Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
(S)-dihydroorotate + 1,4-naphthoquinone
orotate + 1,4-naphthoquinol
(S)-dihydroorotate + 2,3-dimethoxy-5-methyl-1,4-benzoquinone
orotate + 2,3-dimethoxy-5-methyl-1,4-benzoquinol
-
-
-
-
?
(S)-dihydroorotate + 2,3-dimethoxy-5-methyl-6-(3-methyl-2-butenyl)-1,4-benzoquinone
orotate + reduced 2,3-dimethoxy-5-methyl-6-(3-methyl-2-butenyl)-1,4-benzoquinone
Q02172
-
-
-
?
(S)-dihydroorotate + 2,5-dimethyl-p-benzoquinone
orotate + 2,5-dimethyl-p-benzoquinol
(S)-dihydroorotate + 2,6-dichlorophenolindophenol
orotate + reduced 2,6-dichlorophenolindophenol
(S)-dihydroorotate + 2,6-dihydrophenolindophenol
orotate + reduced 2,6-dihydrophenolindophenol
(S)-dihydroorotate + 5,8-dihydroxy-1,4-naphthoquinone
orotate + 5,8-dihydroxy-1,4-naphthoquinol
78% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + acceptor
orotate + reduced acceptor
(S)-dihydroorotate + coenzyme Q
orotate + reduced coenzyme Q
-
-
-
-
?
(S)-dihydroorotate + coenzyme Q0
orotate + reduced coenzyme Q0
(S)-dihydroorotate + coenzyme Q1
orotate + reduced coenzyme Q1
(S)-dihydroorotate + coenzyme Q10
orotate + reduced coenzyme Q10
(S)-dihydroorotate + coenzyme Q2
orotate + reduced coenzyme Q2
123% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + coenzyme Q6
orotate + reduced coenzyme Q6
(S)-dihydroorotate + coenzyme Q7
orotate + reduced coenzyme Q7
-
-
-
-
r
(S)-dihydroorotate + coenzyme Q9
orotate + reduced coenzyme Q9
(S)-dihydroorotate + coenzyme Qd
orotate + reduced coenzyme Qd
(S)-dihydroorotate + decylubiquinone
orotate + decylubiquinol
(S)-dihydroorotate + decylubiquinone
orotate + reduced decylubiquinone
(S)-dihydroorotate + menadione
orotate + menadiol
-
-
-
-
r
(S)-dihydroorotate + oxidized 2,6-dichloroindophenol
orotate + reduced 2,6-dichloroindophenol
-
-
-
-
?
(S)-dihydroorotate + ubiquinone
orotate + reduced ubiquinone
-
-
-
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
(S)-dihydroorotate + ubiquinone-0
orotate + ubiquinol
(S)-dihydroorotate + ubiquinone-30
orotate + ubiquinol-30
-
-
-
-
?
(S)-dihydroorotate + ubiquinone-50
orotate + ubiquinol-50
benzyl-(S)-dihydroorotate + acceptor
benzyl orotate + reduced acceptor
-
-
-
-
?
dihydroorotate + 2,3-dimethoxy-5-methyl-1,4-benzoquinone
orotate + reduced 2,3-dimethoxy-5-methyl-1,4-benzoquinone
-
-
-
?
dihydroorotate + 2,5-dimethyl-p-benzoquinone
orotate + reduced 2,5-dimethyl-p-benzoquinone
95% the rate of decylubiquinone, wild-type, 75% the rate of decylubiquinone, DELTA1-75 mutant
-
-
?
dihydroorotate + 2,5-dimethylbenzoquinone
orotate + reduced 2,5-dimethylbenzoquinone
-
84% of the rate with decylubiquinone
-
-
?
dihydroorotate + 2,6-dichloroindophenol
orotate + reduced 2,6-dichloroindophenol
-
-
-
?
dihydroorotate + 2,6-dichlorophenolindophenol
orotate + reduced 2,6-dichlorophenolindophenol
dihydroorotate + acceptor
orotate + reduced acceptor
dihydroorotate + coenzyme Q
orotate + reduced coenzyme Q
coenzyme OD possesses a decyl tail
-
-
?
dihydroorotate + coenzyme Q0
orotate + reduced coenzyme Q0
dihydroorotate + coenzyme Q1
orotate + reduced coenzyme Q1
coenzyme Q1 possesses a prenyl tail
-
-
?
dihydroorotate + coenzyme QD
orotate + reduced coenzyme QD
coenzyme QD possesses a decyl tail
-
-
?
dihydroorotate + CoQ0
orotate + reduced CoQo
102% the rate of decylubiquinone, wild-type, 67% the rate of decylubiquinone, DELTA1-75 mutant
-
-
?
dihydroorotate + decylplastoquinone
orotate + reduced decylplastoquinone
dihydroorotate + decylubiquinone
orotate + decylubiquinol
-
-
-
?
dihydroorotate + decylubiquinone
orotate + reduced decylubiquinone
dihydroorotate + menadione
orotate + reduced menadione
dihydroorotate + O2
orotate + H2O2
-
-
-
?
dihydroorotate + potassium hexacyanoferrate(III)
orotate + reduced potassium hexacyanoferrate(III)
-
-
-
?
dihydroorotate + ubiquinone 30
orotate + reduced ubiquinone 30
-
-
-
?
dihydroorotate + ubiquinone 50
orotate + reduced ubiquinone 50
-
-
-
?
dihydroorotate + ubiquinone-0
orotate + reduced ubiquinone-0
-
80% of the rate with decylubiquinone
-
-
?
dihydroorotate + ubiquinone-10
orotate + reduced ubiquinone-10
-
59% of the rate with decylubiquinone
-
-
?
dihydroorotate + ubiquinone-50
orotate + reduced ubiquinone-50
83% the rate of decylubiquinone, wild-type, 76% the rate of decylubiquinone, DELTA1-75 mutant
-
-
?
ethyl-dihydroorotate + acceptor
ethyl-orotate + reduced acceptor
-
-
-
-
?
L-dihydroorotate + 2,6-dichloroindophenol
orotate + ?
-
-
-
-
?
L-dihydroorotate + 2,6-dichlorophenolindophenol
orotate + reduced 2,6-dichlorophenolindophenol
-
-
-
-
?
L-dihydroorotate + 2,6-dihydrophenolindophenol
orotate + reduced 2,6-dihydrophenolindophenol
-
-
-
-
r
L-dihydroorotate + decylubiquinone
orotate + ?
-
-
-
-
?
L-dihydroorotate + decylubiquinone
orotate + reduced decylubiquinone
L-dihydroorotate + FMN
orotate + FMNH2
L-dihydroorotate + ubiquinone-0
orotate + reduced ubiquinone-0
-
-
-
?
L-dihydroorotate + ubiquinone-4
orotate + reduced ubiquinone-4
-
-
-
?
L-dihydroorotate + ubiquinone-6
orotate + reduced ubiquinone-6
L-dihydroorotate + vitamin K3
orotate + reduced vitamin K3
-
-
-
?
methyl-dihydroorotate + acceptor
methyl-orotate + reduced acceptor
-
-
-
-
?
methyl-S-dihydroorotate + 2,6-dichlorophenolindophenol
methylorotate + reduced 2,6-dichlorophenolindophenol
-
-
-
-
r
tert-butyl-dihydroorotate + acceptor
tert-butyl-orotate + reduced acceptor
-
-
-
-
?
additional information
?
-
(S)-dihydroorotate + 1,4-naphthoquinone
orotate + 1,4-naphthoquinol
50% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + 1,4-naphthoquinone
orotate + 1,4-naphthoquinol
78% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + 1,4-naphthoquinone
orotate + 1,4-naphthoquinol
-
-
-
-
?
(S)-dihydroorotate + 2,5-dimethyl-p-benzoquinone
orotate + 2,5-dimethyl-p-benzoquinol
48% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + 2,5-dimethyl-p-benzoquinone
orotate + 2,5-dimethyl-p-benzoquinol
67% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + 2,5-dimethyl-p-benzoquinone
orotate + 2,5-dimethyl-p-benzoquinol
-
-
-
-
?
(S)-dihydroorotate + 2,6-dichlorophenolindophenol
orotate + reduced 2,6-dichlorophenolindophenol
-
-
-
?
(S)-dihydroorotate + 2,6-dichlorophenolindophenol
orotate + reduced 2,6-dichlorophenolindophenol
Q02172
-
-
-
?
(S)-dihydroorotate + 2,6-dichlorophenolindophenol
orotate + reduced 2,6-dichlorophenolindophenol
-
-
-
-
?
(S)-dihydroorotate + 2,6-dichlorophenolindophenol
orotate + reduced 2,6-dichlorophenolindophenol
-
-
-
-
?
(S)-dihydroorotate + 2,6-dihydrophenolindophenol
orotate + reduced 2,6-dihydrophenolindophenol
-
-
-
-
r
(S)-dihydroorotate + 2,6-dihydrophenolindophenol
orotate + reduced 2,6-dihydrophenolindophenol
-
-
-
?
(S)-dihydroorotate + 2,6-dihydrophenolindophenol
orotate + reduced 2,6-dihydrophenolindophenol
-
-
-
?
(S)-dihydroorotate + acceptor
orotate + reduced acceptor
-
fumarate and menadione as electron acceptors
-
?
(S)-dihydroorotate + acceptor
orotate + reduced acceptor
-
reduction of a number of substrates: fumatate, coenzyme ubiquinone-0 and menadione
-
?
(S)-dihydroorotate + acceptor
orotate + reduced acceptor
-
uses ubiquinone as electron acceptor
-
-
?
(S)-dihydroorotate + acceptor
orotate + reduced acceptor
-
with ubiquinone-0, 2,6-dichlorophenolindophenol, menadione, decylubiquinone, fumarate and O2 as electron acceptor
-
?
(S)-dihydroorotate + acceptor
orotate + reduced acceptor
-
fourth step in synthesis of pyrimidine nucleotides
-
?
(S)-dihydroorotate + acceptor
orotate + reduced acceptor
-
fourth step in synthesis of pyrimidine nucleotides
-
?
(S)-dihydroorotate + acceptor
orotate + reduced acceptor
-
fourth step in synthesis of pyrimidine nucleotides
-
?
(S)-dihydroorotate + acceptor
orotate + reduced acceptor
-
ubiquinone-6 tested as electron acceptor
-
?
(S)-dihydroorotate + acceptor
orotate + reduced acceptor
-
with ubiquinone-0, 2,6-dichlorophenolindophenol, menadione, decylubiquinone, fumarate and O2 as electron acceptor
-
?
(S)-dihydroorotate + acceptor
orotate + reduced acceptor
-
fourth step in synthesis of pyrimidine nucleotides
-
?
(S)-dihydroorotate + coenzyme Q0
orotate + reduced coenzyme Q0
56% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + coenzyme Q0
orotate + reduced coenzyme Q0
96% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + coenzyme Q1
orotate + reduced coenzyme Q1
111% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + coenzyme Q1
orotate + reduced coenzyme Q1
124% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + coenzyme Q10
orotate + reduced coenzyme Q10
30% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + coenzyme Q10
orotate + reduced coenzyme Q10
19% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + coenzyme Q6
orotate + reduced coenzyme Q6
144% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + coenzyme Q6
orotate + reduced coenzyme Q6
102% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + coenzyme Q9
orotate + reduced coenzyme Q9
66% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + coenzyme Q9
orotate + reduced coenzyme Q9
111% of the activity with coenzyme Qd
-
-
?
(S)-dihydroorotate + coenzyme Qd
orotate + reduced coenzyme Qd
-
-
-
?
(S)-dihydroorotate + coenzyme Qd
orotate + reduced coenzyme Qd
-
-
-
?
(S)-dihydroorotate + decylubiquinone
orotate + decylubiquinol
-
-
-
-
r
(S)-dihydroorotate + decylubiquinone
orotate + decylubiquinol
-
-
-
?
(S)-dihydroorotate + decylubiquinone
orotate + decylubiquinol
-
-
-
-
r
(S)-dihydroorotate + decylubiquinone
orotate + decylubiquinol
-
-
-
-
?
(S)-dihydroorotate + decylubiquinone
orotate + reduced decylubiquinone
-
-
-
?
(S)-dihydroorotate + decylubiquinone
orotate + reduced decylubiquinone
Q02172
-
-
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
-
-
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
-
-
ir
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
-
-
ir
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
reaction studied with menadione, O2 and ferricyanide
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
-
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
-
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
-
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
decylubiquinone as electron acceptor
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
fourth enzyme in pyrimidine synthesis
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
fourth enzyme in pyrimidine synthesis
-
ir
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
six-step biosynthesis of pyrimidine uridine monophosphate
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
fourth step in synthesis of uridine 5'-monophosphate
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
-
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
fourth enzyme in pyrimidine synthesis
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
fourth enzyme in pyrimidine synthesis
-
ir
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
ubiquinone-6, ubiquinone-7, ubiquinone-9 and ubiquinone-10 maximize enzyme activity
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
fourth step in synthesis of uridine 5'-monophosphate
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
-
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
-
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
-
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
fourth enzyme in pyrimidine synthesis
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
fourth enzyme in pyrimidine synthesis
-
ir
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
six-step biosynthesis of pyrimidine uridine monophosphate
-
?
(S)-dihydroorotate + ubiquinone
orotate + ubiquinol
-
-
-
ir
(S)-dihydroorotate + ubiquinone-0
orotate + ubiquinol
-
-
-
-
r
(S)-dihydroorotate + ubiquinone-0
orotate + ubiquinol
-
-
-
-
r
(S)-dihydroorotate + ubiquinone-50
orotate + ubiquinol-50
-
-
-
-
r
(S)-dihydroorotate + ubiquinone-50
orotate + ubiquinol-50
-
-
-
-
?
dihydroorotate + 2,6-dichlorophenolindophenol
orotate + reduced 2,6-dichlorophenolindophenol
-
33% of the rate with decylubiquinone
-
-
?
dihydroorotate + 2,6-dichlorophenolindophenol
orotate + reduced 2,6-dichlorophenolindophenol
-
-
-
?
dihydroorotate + 2,6-dichlorophenolindophenol
orotate + reduced 2,6-dichlorophenolindophenol
-
-
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: quinones
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: coenzyme Q6
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
not acceptor: oxygen
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: menadione
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor coenzyme Q7
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: menadione
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: fumarate, coenzyme Q10
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
mechanism and pH-dependence of reaction
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
-
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: 2,6-dichlorophenolindophenol
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: menaquinone
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: ubiquinone
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
reaction intermediates, mechanism, pH-dependence of reaction
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
physiological electron acceptor: ubiquinone (aerobic conditions), menaquinone (anaerobic conditions)
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
-
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor (low activity): 1,4-naphthoquinone, 5,8-hydroxy-naphthoquinone, juglon, plumbagin, polyporic acid
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: ubiquinone
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
-
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: 2,6-dichlorophenolindophenol
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: quinones
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
not acceptor: oxygen
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
cytochrome b, cytochrome c, pyridine nucleotides (NAD+, NADP+) cannot serve as electron acceptors
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: quinones
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
-
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: 2,6-dichlorophenolindophenol
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptors: e.g. phenazine methosulfate
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor (low activity): 1,4-naphthoquinone, 5,8-hydroxy-naphthoquinone, juglon, plumbagin, polyporic acid
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: ubiquinone
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: oxygen, slowly
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
fourth step in pyrimidine biosynthesis
-
-
?
dihydroorotate + acceptor
orotate + reduced acceptor
-
acceptor: ubiquinone
-
-
?
dihydroorotate + coenzyme Q0
orotate + reduced coenzyme Q0
-
-
-
?
dihydroorotate + coenzyme Q0
orotate + reduced coenzyme Q0
-
-
-
-
?
dihydroorotate + coenzyme Q0
orotate + reduced coenzyme Q0
-
-
-
?
dihydroorotate + coenzyme Q0
orotate + reduced coenzyme Q0
-
-
-
-
?
dihydroorotate + decylplastoquinone
orotate + reduced decylplastoquinone
95% the rate of decylubiquinone, wild-type, 104% the rate of decylubiquinone, DELTA1-75 mutant
-
-
?
dihydroorotate + decylplastoquinone
orotate + reduced decylplastoquinone
-
78% of the rate with decylubiquinone
-
-
?
dihydroorotate + decylubiquinone
orotate + reduced decylubiquinone
-
-
-
?
dihydroorotate + decylubiquinone
orotate + reduced decylubiquinone
-
-
-
?
dihydroorotate + decylubiquinone
orotate + reduced decylubiquinone
-
-
-
-
?
dihydroorotate + menadione
orotate + reduced menadione
82% the rate of decylubiquinone, wild-type, 78% the rate of decylubiquinone, DELTA1-75 mutant
-
-
?
dihydroorotate + menadione
orotate + reduced menadione
-
39% of the rate with decylubiquinone
-
-
?
L-dihydroorotate + decylubiquinone
orotate + reduced decylubiquinone
-
-
-
-
?
L-dihydroorotate + decylubiquinone
orotate + reduced decylubiquinone
-
-
-
?
L-dihydroorotate + decylubiquinone
orotate + reduced decylubiquinone
-
-
-
-
?
L-dihydroorotate + FMN
orotate + FMNH2
-
-
-
-
?
L-dihydroorotate + FMN
orotate + FMNH2
-
DHODH catalyzes the FMN-dependent oxidation of dihydroorotate to produce orotic acid. Two separate half reactions are required to complete the catalytic cycle: 1. oxidation of dihydroorotate driven by the reduction of FMN and, 2. reoxidation of FMNH2 to regenerate the active enzyme
-
-
?
L-dihydroorotate + FMN
orotate + FMNH2
-
-
-
?
L-dihydroorotate + FMN
orotate + FMNH2
-
-
-
-
?
L-dihydroorotate + FMN
orotate + FMNH2
DHODH catalyzes the FMN-dependent oxidation of dihydroorotate to produce orotic acid. Two separate half reactions are required to complete the catalytic cycle: 1. oxidation of dihydroorotate driven by the reduction of FMN and, 2. reoxidation of FMNH2 to regenerate the active enzyme
-
-
?
L-dihydroorotate + ubiquinone-6
orotate + reduced ubiquinone-6
-
-
-
-
?
L-dihydroorotate + ubiquinone-6
orotate + reduced ubiquinone-6
-
-
-
-
?
L-dihydroorotate + ubiquinone-6
orotate + reduced ubiquinone-6
-
-
-
-
?
L-dihydroorotate + ubiquinone-6
orotate + reduced ubiquinone-6
-
-
-
?
additional information
?
-
-
not substrate: 1-methyl-(S)-dihydroorotate, 3-methyl-dihydroorotate, 1,3-dimethyldihydroorotate
-
-
?
additional information
?
-
fumarate and NAD are inadequate electron acceptors for full-length DHODH and N-terminally truncated DHODH
-
-
?
additional information
?
-
-
fumarate and NAD are inadequate electron acceptors for full-length DHODH and N-terminally truncated DHODH
-
-
?
additional information
?
-
computational method to investigate potential proton relay pathways in the active site of the enzyme
-
-
?
additional information
?
-
-
computational method to investigate potential proton relay pathways in the active site of the enzyme
-
-
?
additional information
?
-
reduction of decylubiquinone (DUQ) is stoichiometrically equivalent to reduction of 2,6-ichloroindophenol (DCIP) resulting in the decrease in absorbance at 610 nm, which is measured
-
-
-
additional information
?
-
-
reduction of decylubiquinone (DUQ) is stoichiometrically equivalent to reduction of 2,6-ichloroindophenol (DCIP) resulting in the decrease in absorbance at 610 nm, which is measured
-
-
-
additional information
?
-
-
fumarate is a poor electron acceptor
-
-
?
additional information
?
-
-
enzyme has methylviologen-fumarate reductase activity
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
(1-(5-cyclopropylpyrimidin-2-yl)-3-isopropoxy-5-methyl-1H-pyrazol-4-yl)(phenyl)methanol
Q02172
-
(2,3-difluoro-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(2,5-difluoro-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(2,6-difluoro-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(2-chloro-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(2-fluoro-4-methyl-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(2E)-2-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]but-2-enamide
-
50% inhibition at 0.000435 mM
(2E)-2-cyano-N-(2',3-dichloro[1,1'-biphenyl]-4-yl)-3-hydroxybut-2-enamide
-
-
(2E)-N-(3-chloro-2'-methoxy[1,1'-biphenyl]-4-yl)-2-cyano-3-hydroxybut-2-enamide
-
-
(2E)-N-[2'-chloro-3-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-2-cyano-3-hydroxybut-2-enamide
-
-
(2Z)-2-cyano-3-cyclopropyl-3-hydroxy-N-[4-(trifluoromethyl)phenyl]prop-2-enamide
-
(2Z)-2-cyano-N-(2',3-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
-
(2Z)-2-cyano-N-(2,2'-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
-
(2Z)-2-cyano-N-(2,3'-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
-
(2Z)-2-cyano-N-(3'-ethoxybiphenyl-4-yl)-3-hydroxybut-2-enamide
-
(2Z)-N-(2'-chlorobiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
-
(2Z)-N-(3-chloro-2'-methoxybiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
-
(2Z)-N-(biphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
(2Z)-N-[2'-chloro-3-(trifluoromethyl)biphenyl-4-yl]-2-cyano-3-hydroxybut-2-enamide
-
(3,4-difluoro-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(3,4-dimethyl-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(3,5-bis-trifluoromethyl-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(3,5-difluoro-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(3-chloro-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(3-fluoro-4-methyl-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(3-fluoro-4-trifluoromethyl-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(3-fluoro-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(4-benzyl-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(4-bromo-3-trifluoromethyl-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(4-bromo-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(4-chloro-3-trifluoromethyl-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(4-chloro-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(4-difluoromethoxy-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(4-fluoro-3-methyl-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(4-fluoro-phenyl)-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(4-methoxyphenyl)(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-(2,3,4,5,6-pentafluorophenyl)-amine
-
-
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-(2,3,4-trifluoro-phenyl)-amine
-
-
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-(2,3,5,6-tetrafluoro-phenyl)-amine
-
-
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-(2,4,5-trifluoro-phenyl)-amine
-
-
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-(2,4,6-trifluoro-phenyl)-amine
-
-
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-(2-trifluoromethyl-phenyl)-amine
-
-
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-(3-trifluoromethyl-phenyl)-amine
-
-
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-(4-methyl-3-trifluoromethylphenyl)-amine
-
-
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-(4-nitro-phenyl)-amine
-
-
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-(4-trifluoromethoxy-phenyl)-amine
-
-
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-(4-trifluoromethyl-phenyl)-amine
-
DSM74
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-m-tolyl-amine
-
-
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-naphthalen-2-yl-amine
-
DSM1, a potent triazolopyrimidine-based inhibitor of PfDHODH that shows greater than 4000fold selectivity for the malarial enzyme when compared to human DHODH
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-o-tolyl-amine
-
-
(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-p-tolyl-amine
-
-
1-(1-naphthyl)-3-[2-(trifluoromethyl)phenyl]urea
-
50% inhibition at 0.0004 mM, wild type, 0.00034 mM, mutant R265A, above 0.2, mutant H185A
1-(2-((3,4-dimethylphenyl)amino)-4-methylthiazol-5-yl)-ethanone
Q02172
-
1-(2-((3-chloro-4-methylphenyl)amino)-4-methylthiazol-5-yl)ethanone
Q02172
-
1-(2-((3-fluoro-4-methylphenyl)amino)-4-methylthiazol-5-yl)ethanone
Q02172
-
1-(2-((4-(tert-butyl)phenyl)amino)-4-methylthiazol-5-yl)-ethanone
Q02172
-
1-(2-((4-bromo-3-(trifluoromethyl)phenyl)amino)-4-methylthiazol-5-yl)ethanone
Q02172
-
1-(2-((4-bromophenyl)amino)-4-methylthiazol-5-yl)-ethanone
Q02172
-
1-(2-((4-chloro-3-(trifluoromethyl)phenyl)amino)-4-methylthiazol-5-yl)ethanone
Q02172
-
1-(2-(anthracen-2-ylamino)-4-methylthiazol-5-yl)ethan-1-one
Q02172
-
1-(2-methoxyphenyl)-3-(1-naphthyl)urea
-
50% inhibition at 0.00023 mM, wild type, 0.00024 mM, mutant R265A, 0.140, mutant H185A
1-(2-methoxyphenyl)-3-naphthalen-1-ylurea
1-(4-chlorophenyl)-3-quinolin-8-ylurea
-
50% inhibition at 0.00078 mM, wild type, 0.002 mM, mutant R265A, above 0.4, mutant H185A
1-(4-methyl-2-(naphthalen-2-ylamino)thiazol-5-yl)ethan-1-one
Q02172
-
1-(4-methyl-2-(phenylamino)thiazol-5-yl)ethanone
Q02172
-
1-hydroxy-2-dodecyl-4(1)quinolone
-
competitive with regard to decylubiquinone, uncompetitive with regard to dihydroorotate
10-phenyl-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
IC50 value for human enzyme above 0.0045 mM
-
2,8-dimethyl-N-[4-(trifluoromethyl)phenyl]pyrrolo[1,2-a]pyrimidin-4-amine
-
-
2-(1,1-difluoroethyl)-5-methyl-N-[4-(pentafluoro-lambda6-sulfanyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
2-(2'-fluoro-[1,1'-biphenyl]-4-yl)-3-methyl-6-(trifluoromethyl)-1,7-naphthyridine-4-carboxylic acid
-
-
2-(2'-methoxy-[1,1'-biphenyl]-4-yl)quinoline-4-carboxylic acid
-
-
2-(2,3-bis(benzyloxy)phenyl)quinoline-4-carboxylic acid
-
-
2-(2,3-dichloroanilino)-3-hydroxynaphthalene-1,4-dione
-
2-(2,4-bis(benzyloxy)phenyl)quinoline-4-carboxylic acid
-
-
2-(2,4-dimethoxyphenyl)quinoline-4-carboxylic acid
-
-
2-(2,6-dimethylanilino)-3-hydroxynaphthalene-1,4-dione
-
2-(2-chloroanilino)-3-hydroxynaphthalene-1,4-dione
-
2-(3,4-bis(benzyloxy)phenyl)quinoline-4-carboxylic acid
-
-
2-(3,4-dibutoxyphenyl)quinoline-4-carboxylic acid
-
-
2-(3,4-dihydroxyphenyl)quinoline-4-carboxylic acid
-
-
2-(3,4-diisobutoxyphenyl)quinoline-4-carboxylic acid
-
-
2-(3,4-dimethoxyphenyl)quinoline-4-carboxylic acid
-
-
2-(3,4-dipropoxyphenyl)quinoline-4-carboxylic acid
-
-
2-(3-chloroanilino)-3-hydroxynaphthalene-1,4-dione
-
2-(3-ethoxy-4-(2-fluorophenoxy)-5-methyl-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(3-ethoxy-5-methyl-4-(2-(trifluoromethyl)phenoxy)-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(3-ethoxy-5-methyl-4-(3-(trifluoromethyl)phenoxy)-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(3-ethoxy-5-methyl-4-(4-(trifluoromethyl)phenoxy)-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(3-ethoxy-5-methyl-4-phenoxy-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(3-methoxy-4-propoxyphenyl)quinoline-4-carboxylic acid
-
-
2-(4'-tert-butyl-2-chloro-biphenyl-4-ylcarbamoyl)-cyclopent-1-enecarboxylic acid
-
50% inhibition at 0.000080 mM
2-(4-(1H-imidazol-1-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(2,3-dichlorophenoxy)-3-ethoxy-5-methyl-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(4-(2,3-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(4-(2,4-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(4-(2,5-dichlorophenoxy)-3-ethoxy-5-methyl-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(4-(2,5-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-5-ethylpyrimidin-4-ol
Q02172
-
2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-5-fluoropyrimidine
Q02172
-
2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-5-methoxypyrimidine
Q02172
-
2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-5-methylpyrimidin-4-ol
Q02172
-
2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-5-propylpyrimidin-4-ol
Q02172
-
2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-5-propylpyrimidine
Q02172
-
2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-pyrimidine
Q02172
-
2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)pyrimidin-4-ol
Q02172
-
2-(4-(2-(trifluoromethyl)pyridin-3-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(2-bromophenoxy)-3-ethoxy-5-methyl-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(4-(2-chloro-6-methylpyridin-3-yl)phenyl)-3-methyl-1,7-naphthyridine-4-carboxylic acid
-
-
2-(4-(2-chloro-6-methylpyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
-
-
2-(4-(2-chloro-6-methylpyridin-3-yl)phenyl)-6-fluoro-3-methylquinoline-4-carboxylic acid
-
-
2-(4-(2-chloro-6-methylpyridin-3-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(2-chlorophenoxy)-3-ethoxy-5-methyl-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(4-(2-chloropyridin-3-yl)phenyl)-3,6-dimethylquinoline-4-carboxylic acid
-
-
2-(4-(2-chloropyridin-3-yl)phenyl)-3-methyl-1,7-naphthyridine-4-carboxylic acid
-
-
2-(4-(2-chloropyridin-3-yl)phenyl)-3-methyl-6-(trifluoromethyl)-1,7-naphthyridine-4-carboxylic acid
-
-
2-(4-(2-chloropyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
-
-
2-(4-(2-chloropyridin-3-yl)phenyl)-6-fluoro-3-methylquinoline-4-carboxylic acid
the compound possesses significant oral bioavailability (F = 56%) and an elimination t1/2 = 2.78 h, pharmacokinetic parameters, overview
-
2-(4-(2-chloropyridin-3-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(2-fluoro-6-methylpyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
-
-
2-(4-(2-fluoropyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
-
-
2-(4-(2-fluoropyridin-3-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(2-methoxypyridin-3-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(2-methylpyridin-3-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(3,5-dichlorophenoxy)-3-ethoxy-5-methyl-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(4-(4-(trifluoromethyl)pyridin-3-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(4-methylpyridin-3-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(6-fluoropyridin-3-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(benzyloxy)-3-methoxyphenyl)quinoline-4-carboxylic acid
-
-
2-(4-(piperidin-1-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(pyridazin-3-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(pyridin-2-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(pyridin-3-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(pyridin-4-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-(pyrimidin-2-yl)phenyl)quinoline-4-carboxylic acid
-
-
2-(4-benzyl-1-(5-ethylpyrimidin-2-yl)-5-methyl-1H-pyrazol-3-yloxy)ethanol
Q02172
-
2-(4-benzyl-3-(2-(benzyloxy)ethoxy)-5-methyl-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(4-benzyl-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-5-cyclopropylpyrimidine
Q02172
-
2-(4-benzyl-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)-5-ethylpyrimidine
Q02172
-
2-(4-benzyl-3-methoxy-5-methyl-1H-pyrazol-1-yl)-5-cyclopropylpyrimidine
Q02172
-
2-(4-benzyl-3-sec-butoxy-5-methyl-1H-pyrazol-1-yl)-5-cyclopropylpyrimidine
Q02172
-
2-(4-benzyl-5-methyl-3-(pentan-3-yloxy)-1H-pyrazol-1-yl)-5-cyclopropylpyrimidine
Q02172
-
2-(4-biphenylylcarbamoyl)-1-cyclopentene-1-carboxylic acid
-
2-(4-biphenylylcarbamoyl)-2-benzoic acid
i.e. MD 129, 0.5 mM, 95% of initial activity
-
2-(4-butoxy-3-methoxyphenyl)quinoline-4-carboxylic acid
-
-
2-(4-chloroanilino)-3-hydroxynaphthalene-1,4-dione
-
2-(4-cyclohexylphenyl)quinoline-4-carboxylic acid
-
-
2-(4-fluoroanilino)-3-hydroxynaphthalene-1,4-dione
-
2-(4-hydroxy-3-methoxyphenyl)quinoline-4-carboxylic acid
-
-
2-(4-isobutoxy-3-methoxyphenyl)quinoline-4-carboxylic acid
-
-
2-(4-isobutylphenyl)quinoline-4-carboxylic acid
-
-
2-(4-isopropylphenyl)quinoline-4-carboxylic acid
-
-
2-(4-methylphenyl)quinoline-4-carboxylic acid
-
-
2-(4-morpholinophenyl)quinoline-4-carboxylic acid
-
-
2-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-ylamino)-benzonitrile
-
-
2-([1,1'-biphenyl]-4-yl)-3-methyl-1,6-naphthyridine-4-carboxylic acid
-
-
2-([1,1'-biphenyl]-4-yl)-3-methyl-1,7-naphthyridine-4-carboxylic acid
-
-
2-([1,1'-biphenyl]-4-yl)-3-methyl-1,8-naphthyridine-4-carboxylic acid
-
-
2-([1,1'-biphenyl]-4-yl)-3-methyl-6-(trifluoromethyl)-1,7-naphthyridine-4-carboxylic acid
-
-
2-([1,1'-biphenyl]-4-yl)-3-methylquinoline-4-carboxylic acid
-
-
2-([1,1'-biphenyl]-4-yl)quinoline-4-carboxylic acid
-
-
2-([[2,3,5,6-tetrafluoro-3'-(trifluoromethoxy)biphenyl-4-yl]amino]carbonyl)cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000007 mM
2-([[2-chloro-3'-(trifluoromethoxy)biphenyl-4-yl]amino]carbonyl)cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000020 mM
2-([[2-chloro-4'-(dimethylamino)biphenyl-4-yl]amino]carbonyl)cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.00005 mM
2-([[3'-(trifluoromethoxy)-3-(trifluoromethyl)biphenyl-4-yl]amino]carbonyl)cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000840 mM
2-([[3,5-difluoro-3'-(trifluoromethoxy)biphenyl-4-yl]amino]carbonyl)cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000033 mM
2-([[3-chloro-3'-(trifluoromethoxy)biphenyl-4-yl]amino]carbonyl)cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000290 mM
2-([[3-cyano-3'-(trifluoromethoxy)biphenyl-4-yl]amino]carbonyl)cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000370 mM
2-([[3-fluoro-3'-(trifluoromethoxy)biphenyl-4-yl]amino]carbonyl)cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.00028 mM
2-([[3-fluoro-4'-(trifluoromethoxy)biphenyl-4-yl]amino]carbonyl)cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.00570 mM
2-([[3-methyl-3'-(trifluoromethoxy)biphenyl-4-yl]amino]carbonyl)cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000150 mM
2-([[3-nitro-3'-(trifluoromethoxy)biphenyl-4-yl]amino]carbonyl)cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000390 mM
2-([[4'-(dimethylamino)-3,5-difluorobiphenyl-4-yl]amino]carbonyl)cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.00061 mM
2-([[4-(1-naphthyl)-2-(trifluoromethyl)phenyl]amino]carbonyl)cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000180 mM
2-anilino-3-hydroxynaphthalene-1,4-dione
-
2-chloro-3-(methylamino)naphthalene-1,4-dione
-
2-cyano-3-(9-ethyl-9H-carbazol-3-ylamino)acrylic acid ethyl ester
2-cyano-3-cyclopropyl-3-hydroxy-N-[4'-(cyano)phenyl]-propenamide
2-cyano-3-cyclopropyl-3-hydroxy-N-[4'-(nitro)phenyl]-propenamide
2-cyano-3-cyclopropyl-3-hydroxy-N-[4'-(trifluoromethyl)phenyl]-propenamide
2-cyano-3-hydroxy-N-(2',3,3'-trichlorobiphenyl-4-yl)but-2-enamide
-
-
2-hydroxy-3-(3-methylbutyl)naphthalene-1,4-dione
-
2-hydroxy-3-(4-methoxyanilino)naphthalene-1,4-dione
-
2-hydroxy-3-(4-phenylpiperazin-1-yl)naphthalene-1,4-dione
-
2-hydroxy-3-[3-(trifluoromethyl)anilino]naphthalene-1,4-dione
-
2-hydroxy-3-[4-(4-nitrophenyl)piperazin-1-yl]naphthalene-1,4-dione
-
2-hydroxyethylidene-cyano acetic acid 4-trifluoromethyl anilide
-
A177-1726, active derivative of human inhibitor leflunomide
2-hydroxyethylidene-cyanoacetic acid 4-trifluoromethyl anilide
2-methyl-3-nitro-N-[3-(trifluoromethyl)phenyl]benzamide
-
50% inhibition at 0.00008 mM, wild type, 0.00037 mM, mutant R265A, 0.120, mutant H185A
2-methyl-N-1-naphthyl-3-nitrobenzamide
-
50% inhibition at 0.00008 mM, wild type, 0.00048 mM, mutant R265A, 0.180, mutant H185A
2-methylcyclohexa-2,5-diene-1,4-dione
-
2-tert-butylcyclohexa-2,5-diene-1,4-dione
-
-
2-[(2,3-dihydro-1,4-benzodioxin-6-yl)amino]-3-hydroxynaphthalene-1,4-dione
-
2-[(2,5-dichlorophenyl)sulfanyl]-5-ethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
2-[(2,5-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
2-[(2H-1,3-benzodioxol-5-yl)amino]-3-hydroxynaphthalene-1,4-dione
-
2-[(3,4-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
2-[(4-chlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
2-[(biphenyl-4-ylamino)carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.00041 mM
2-[(E)-2-(2-methylphenyl)ethenyl]quinolin-4-ol
2-[4-(2,3-dichlorophenyl)piperazin-1-yl]-3-hydroxynaphthalene-1,4-dione
-
2-[4-(4-chlorophenyl)piperazin-1-yl]-3-hydroxynaphthalene-1,4-dione
-
2-[[(2',3,5-trifluorobiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000045 mM
2-[[(2'-chloro-3,5-difluorobiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000018 mM
2-[[(2'-chlorobiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000225 mM
2-[[(2,3,5,6-tetrafluoro-2'-methoxybiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000008 mM
2-[[(3'-ethoxy-3,5-difluorobiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000017 mM
2-[[(3,3'-dimethoxybiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000170 mM
2-[[(3,5-difluoro-2',4'-dimethoxybiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000090 mM
2-[[(3,5-difluoro-2'-methoxybiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000042 mM
2-[[(3-chloro-2'-methoxybiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000310 mM
2-[[(3-chloro-4'-methoxybiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.00840 mM
2-[[(3-fluoro-3'-hydroxybiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000610 mM
2-[[(3-fluoro-4'-methoxybiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.00170 mM
2-[[(4'-bromo-2-chlorobiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000070 mM
2-[[(4'-bromo-3-chlorobiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.002900 mM
2-[[(4'-bromo-3-fluorobiphenyl-4-yl)amino]carbonyl]cyclopent-1-ene-1-carboxylic acid
-
50% inhibition at 0.000735 mM
2-[[(4-chlorophenyl)methyl]sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7(4H)-one
-
-
3-(3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazol-9-yl)phenol
IC50 value for human enzyme above 0.0045 mM
-
3-(3-methylbut-2-en-1-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl 4-methylbenzene-1-sulfonate
-
3-(4-benzyl-1-(5-ethylpyrimidin-2-yl)-5-methyl-1H-pyrazol-3-yloxy)-N,N-dimethylpropan-1-amine
Q02172
-
3-hydroxy-2-(3,3-dichloroallyl)-1,4-naphthoquinone
4-(3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazol-9-yl)phenol
IC50 value for human enzyme above 0.0045 mM
-
4-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-ylamino)-2-trifluoromethylbenzonitrile
-
-
4-(6-imino-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-9-yl)benzamide
IC50 value for human enzyme above 0.0045 mM
-
4-benzyl-1-(5-cyclopropylpyrimidin-2-yl)-5-methyl-1H-pyrazol-3-ol
Q02172
-
4-benzyl-1-(5-ethylpyrimidin-2-yl)-5-methyl-1H-pyrazol-3-ol
Q02172
-
4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
4-[(5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)amino]-2-(trifluoromethyl)benzonitrile
-
5,6-dimethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
5-(1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
5-(1H-indol-1-yl)-N-propylthiophene-2-carboxamide
5-(2-methyl-1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
5-(4-cyano-2-methyl-1H-benzimidazol-1-yl)-N-cyclopropylthiophene-2-carboxamide
-
-
5-(4-methylpiperazin-1-yl)-N-propylthiophene-2-carboxamide
5-(piperidin-1-yl)-N-propylthiophene-2-carboxamide
5-bromo-2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)pyrimidine
Q02172
-
5-cyclopropyl-2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)pyrimidine
Q02172
-
5-cyclopropyl-2-(4-(2-fluorobenzyl)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)pyrimidine
Q02172
-
5-ethyl-2-(3-isopropoxy-4-(2-methoxybenzyl)-5-methyl-1H-pyrazol-1-yl)pyrimidine
Q02172
-
5-ethyl-2-(3-isopropoxy-4-(3-methoxybenzyl)-5-methyl-1H-pyrazol-1-yl)pyrimidine
Q02172
-
5-ethyl-2-(3-isopropoxy-4-(4-methoxybenzyl)-5-methyl-1H-pyrazol-1-yl)pyrimidine
Q02172
-
5-ethyl-2-(4-(2-fluorobenzyl)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)pyrimidine
Q02172
-
5-ethyl-2-(4-(2-fluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)pyrimidine
Q02172
-
5-ethyl-2-(4-(3-fluorobenzyl)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)pyrimidine
Q02172
-
5-ethyl-2-(4-(3-fluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)pyrimidine
Q02172
-
5-ethyl-2-(4-(4-fluorobenzyl)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)pyrimidine
Q02172
-
5-ethyl-2-(4-(4-fluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)pyrimidine
Q02172
-
5-ethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
5-methoxy-2-[(4-phenoxyphenyl)amino]benzoic acid
-
5-methyl-2-(4-(2,6-difluorophenoxy)-3-isopropoxy-5-methyl-1H-pyrazol-1-yl)pyrimidine
Q02172
-
5-methyl-7-(naphthalen-2-yloxy)[1,2,4]triazolo[1,5-a]pyrimidine
5-methyl-7-(naphthalen-2-ylsulfanyl)[1,2,4]triazolo[1,5-a]pyrimidine
5-methyl-N-(2,3,4-trifluorophenyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
5-methyl-N-(2,4,5-trifluorophenyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
5-methyl-N-(3-methylphenyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
5-methyl-N-(4-methylphenyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
5-methyl-N-(4-nitrophenyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
5-methyl-N-[3-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
5-methyl-N-[4-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
5-methyl-N-[4-(trifluoromethyl)phenyl]-1,2-oxazole-4-carboxamide
-
5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
5-methyl-N-[4-methyl-3-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
6-chloro-2-(2'-fluorobiphenyl-4-yl)quinoline-4-carboxylic acid
-
6-chloro-2-(4-(2-chloro-6-methylpyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
-
-
6-chloro-2-(4-(2-chloropyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
-
-
6-chloro-2-(4-(2-fluoropyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
-
-
6-fluoro-2-(2'-fluoro[1,1'-biphenyl]-4-yl)-3-methylquinoline-4-carboxylic acid
-
6-fluoro-2-(4-(2-fluoro-6-methylpyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
-
-
6-fluoro-2-(4-(2-fluoropyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
-
-
6-fluoro-2-[2-methyl-4-phenoxy-5-(propan-2-yl)phenyl]quinoline-4-carboxylic acid
i.e. C44
-
6-methyl-N-phenyl-3aH-inden-4-amine
7-methyl-N-(naphthalen-2-yl)imidazo[1,2-a]pyrimidin-5-amine
-
-
7-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyridin-5-amine
-
-
8-(1,3,3a,4-tetrahydro-2-benzofuran-4-yl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
IC50 value for human enzyme above 0.0045 mM
-
8-(1,8a-dihydronaphthalen-1-yl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
IC50 value for human enzyme above 0.0045 mM
-
8-(oxolan-2-yl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
IC50 value for human enzyme above 0.0045 mM
-
8-(pyridin-3-yl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
IC50 value for human enzyme above 0.0045 mM
-
8-(thiolan-3-yl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
IC50 value for human enzyme above 0.0045 mM
-
9-(1-benzofuran-2-yl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
IC50 value for human enzyme above 0.0045 mM
-
9-(2,3-dihydro-1,4-benzodioxin-6-yl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
IC50 value for human enzyme above 0.0045 mM
-
9-(2-methoxyphenyl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
IC50 value for human enzyme above 0.0045 mM
-
9-(2-nitrophenyl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
IC50 value for human enzyme above 0.0045 mM
-
9-(2H-1,3-benzodioxol-5-yl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
IC50 value for human enzyme above 0.0045 mM
-
9-(3-ethylphenyl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
IC50 value for human enzyme above 0.0045 mM
-
9-(4-nitrophenyl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
IC50 value for human enzyme above 0.0045 mM
-
9-(4-phenoxyphenyl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
IC50 value for human enzyme above 0.0045 mM
-
9-(isoquinolin-6-yl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
IC50 value for human enzyme above 0.0045 mM
-
9-(naphthalen-1-yl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
IC50 value for human enzyme above 0.0045 mM
-
9-(naphthalen-2-yl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
IC50 value for human enzyme above 0.0045 mM
-
9-phenyl-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
IC50 value for human enzyme above 0.0045 mM
-
9-phenyl-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
IC50 value for human enzyme above 0.0045 mM
-
9-[(E)-2-phenylethenyl]-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
IC50 value for human enzyme above 0.0045 mM
-
9-[3-[(propan-2-yl)oxy]phenyl]-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
IC50 value for human enzyme above 0.0045 mM
-
9-[4-(methylsulfanyl)phenyl]-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
IC50 value for human enzyme above 0.0045 mM
-
9-[4-(trifluoromethoxy)phenyl]-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
IC50 value for human enzyme above 0.0045 mM
-
alloxan
0.5 mM, 74% of initial activity
benzoquinones
-
ubiquinone-0 and decylubiquinone
biphenyl-4-yl-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)-amine
-
-
cis-5-methyldihydroorotate
-
-
diethyl [(1H-benzimidazol-5-ylamino)methylidene]propanedioate
-
diethyl [(1H-indazol-5-ylamino)methylidene]propanedioate
-
diethyl [(5a,9a-dihydrodibenzo[b,d]thiophen-2-ylamino)methylidene]propanedioate
-
diethyl [(biphenyl-3-ylamino)methylidene]propanedioate
-
diethyl [(biphenyl-4-ylamino)methylidene]propanedioate
-
diethyl [(dibenzo[b,d]thiophen-2-ylamino)methylidene]propanedioate
diethyl {[(2-methylphenyl)amino]methylidene}propanedioate
-
diethyl {[(4-methylphenyl)amino]methylidene}propanedioate
-
ethyl (2Z)-3-(biphenyl-3-ylamino)-2-cyanoprop-2-enoate
-
ethyl (2Z)-3-(biphenyl-4-ylamino)-2-cyanoprop-2-enoate
-
ethyl 2-((2,3-dihydro-1h-inden-5-yl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3,4-dichlorophenyl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3,4-dimethylphenyl)amino)-4-methylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3,4-dimethylphenyl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3,5-dichlorophenyl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3,5-difluoro-3'-methoxy-[1,1'-biphenyl]-4-yl)-amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3-chloro-4-((2-chloro-6-fluorobenzyl)oxy)phenyl)-amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3-chloro-4-methylphenyl)amino)-4-cyclopropylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3-chloro-4-methylphenyl)amino)-4-methylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3-chloro-4-methylphenyl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3-chloro-4-phenoxyphenyl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3-fluoro-3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3-fluoro-4-methylphenyl)amino)-4-methylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3-fluoro-4-methylphenyl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((3-fluoro-[1,1'-biphenyl]-4-yl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((4-(benzyloxy)-3-chlorophenyl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((4-(tert-butyl)phenyl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((4-bromo-2-methylphenyl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((4-bromo-3-(trifluoromethyl)phenyl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((4-bromophenyl)amino)-4-methylthiazole-5-carboxylate
Q02172
-
ethyl 2-((4-chloro-3-(trifluoromethyl)phenyl)amino)-4-(cyclopropanecarboxamido)thiazole-5-carboxylate
Q02172
-
ethyl 2-((4-chloro-3-(trifluoromethyl)phenyl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((4-chlorophenyl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-((4-methoxyphenyl)amino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-(anthracen-2-ylamino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-(benzo[d][1,3]dioxol-5-ylamino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-(naphthalen-2-ylamino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 2-([1,1'-biphenyl]-4-ylamino)-4-phenylthiazole-5-carboxylate
Q02172
-
ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
ethyl 4-(cyclopropanecarboxamido)-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
Q02172
-
ethyl 4-(tert-butyl)-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
Q02172
-
ethyl 4-(tert-butyl)-2-((3-chloro-4-methylphenyl)amino)-thiazole-5-carboxylate
Q02172
-
ethyl 4-(tert-butyl)-2-((3-fluoro-4-methylphenyl)amino)-thiazole-5-carboxylate
Q02172
-
ethyl 4-amino-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
Q02172
-
ethyl 4-amino-2-((4-chloro-3-(trifluoromethyl)phenyl)-amino)thiazole-5-carboxylate
Q02172
-
ethyl 4-benzamido-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
Q02172
-
ethyl 4-benzamido-2-((4-chloro-3-(trifluoromethyl)phenyl)-amino)thiazole-5-carboxylate
Q02172
-
ethyl 4-cyclopropyl-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
Q02172
-
ethyl 4-cyclopropyl-2-((4-fluoro-3-methylphenyl)amino)-thiazole-5-carboxylate
Q02172
-
ethyl 4-methyl-2-(naphthalen-2-ylamino)thiazole-5-carboxylate
Q02172
-
ethyl 4-phenyl-2-((4-(trifluoromethyl)phenyl)amino)-thiazole-5-carboxylate
Q02172
-
ethyl 4-phenyl-2-((5,6,7,8-tetrahydronaphthalen-2-yl)-amino)thiazole-5-carboxylate
Q02172
-
ethyl 4-phenyl-2-(phenylamino)thiazole-5-carboxylate
Q02172
-
H2O2
-
byproduct, tends to inactivate enzyme
HR325
-
structural analogue of A77 1726
methyl 2-(4-(4-(trifluoromethyl)pyridin-3-yl)phenyl)quinoline-4-carboxylate
-
-
methyl 2-(4-(piperidin-1-yl)phenyl)quinoline-4-carboxylate
-
-
methyl 2-(4-(pyridin-3-yl)phenyl)quinoline-4-carboxylate
-
-
methyl 2-(4-cyclohexylphenyl)quinoline-4-carboxylate
-
-
methyl 2-([1,1'-biphenyl]-4-yl)quinoline-4-carboxylate
-
-
methyl 3-(3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazol-9-yl)benzoate
IC50 value for human enzyme above 0.0045 mM
-
methyl 4-(3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazol-9-yl)benzoate
IC50 value for human enzyme above 0.0045 mM
-
methyl 4-(6-imino-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-9-yl)benzoate
IC50 value for human enzyme above 0.0045 mM
-
N-(2,3-difluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(2,4-dichlorophenyl)-2-naphthamide
-
50% inhibition at 0.00005 mM, wild type, 0.00008 mM, mutant R265A, above 0.05, mutant H185A
N-(2,4-dichlorophenyl)naphthalene-2-carboxamide
N-(2-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
N-(2-fluoro-4-methylphenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(2-fluorophenyl)-2-naphthamide
-
50% inhibition at 0.00047 mM, wild type, 0.00030 mM, mutant R265A, 0.21, mutant H185A
N-(2-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
N-(3,4-dichlorophenyl)-2-methyl-3-nitrobenzamide
-
50% inhibition at 0.00008 mM, wild type, 0.0028 mM, mutant R265A, 0.06, mutant H185A
N-(3,4-difluorophenyl)-2-methyl-3-nitrobenzamide
-
50% inhibition at 0.00026 mM, wild type, 0.00082 mM, mutant R265A, 0.25, mutant H185A
N-(3,4-difluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(3,4-dimethylphenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(3,5-dichloro-phenyl)-2-methyl-3-nitro-benzamide
-
N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide
N-(3,5-difluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(3-bromophenyl)-2-methyl-3-nitrobenzamide
-
50% inhibition at 0.00006 mM, wild type, 0.0012 mM, mutant R265A, 0.140, mutant H185A
N-(3-chloro-2'-methoxybiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
-
-
N-(3-chloro-2-methoxybiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
-
N-(3-chloro-4-fluorophenyl)-2-methyl-3-nitrobenzamide
-
50% inhibition at 0.0001 mM, wild type, 0.0005 mM, mutant R265A, 0.13, mutant H185A
N-(3-chlorobiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
-
N-(3-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
N-(3-fluoro-4-methylphenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(3-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
N-(4-benzylphenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(4-bromo-2-methylphenyl)-2-naphthamide
-
50% inhibition at 0.00005 mM, wild type, 0.00005 mM, mutant R265A, 0.57, mutant H185A
N-(4-bromophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
N-(4-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(4-fluoro-3-methylphenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(4-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
N-(4-methoxyphenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(anthracen-2-yl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
N-(anthracen-2-yl)-N,5-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
N-(biphenyl-4-yl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-anthracen-2-yl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
i.e. DSM2
N-cyclopropyl-5-(2,3-dihydro-4H-1,4-benzothiazin-4-yl)thiophene-2-carboxamide
N-cyclopropyl-5-[4-(difluoromethoxy)-2-methyl-1H-benzimidazol-1-yl]thiophene-2-carboxamide
-
-
N-propyl-5-(1H-pyrazol-1-yl)thiophene-2-carboxamide
N-[3,5-difluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-[3-fluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
N-[4-(difluoromethoxy)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-[4-bromo-3-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-[4-chloro-3-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
NSC 277965
0.5 mM, 60% of initial activity
-
NSC 71097
0.5 mM, 70% of initial activity
-
rhodamine 123
-
mitochondrial inhibitor
trifluoromethyl 6-(6-imino-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-9-yl)-1H-indole-3-carboxylate
IC50 value for human enzyme above 0.0045 mM
-
[2-fluoro-2',5'-dimethyl-4'-[6-(3-methyl-2-butenyloxy)pyridin-3-yl]biphenyl-4-yl]-(3-methyl-2-butenyl)amine
[4-(6-imino-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-9-yl)phenyl](4-[[(prop-2-yn-1-yl)oxy]methyl]phenyl)methanone
IC50 value for human enzyme above 0.0045 mM
-
[[3-(3-methylbut-2-en-1-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl]oxy]acetonitrile
-
(2Z)-2-cyano-3-cyclopropyl-3-hydroxy-N-[4-(trifluoromethyl)phenyl]prop-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-2-cyano-3-cyclopropyl-3-hydroxy-N-[4-(trifluoromethyl)phenyl]prop-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-2-cyano-N-(2',3-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-2-cyano-N-(2',3-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-2-cyano-N-(2,2'-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-2-cyano-N-(2,2'-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-2-cyano-N-(2,3'-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-2-cyano-N-(2,3'-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-2-cyano-N-(3'-ethoxybiphenyl-4-yl)-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-2-cyano-N-(3'-ethoxybiphenyl-4-yl)-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-N-(2'-chlorobiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-N-(2'-chlorobiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-N-(3-chloro-2'-methoxybiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-N-(3-chloro-2'-methoxybiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-N-(biphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
(2Z)-N-(biphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
(2Z)-N-[2'-chloro-3-(trifluoromethyl)biphenyl-4-yl]-2-cyano-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
(2Z)-N-[2'-chloro-3-(trifluoromethyl)biphenyl-4-yl]-2-cyano-3-hydroxybut-2-enamide
inhibitor based on the active metabolite of the anti-inflammatory drug leflunomide. Comparison of inhibitory effect and binding to human and Plasmodium falciparum enzyme
-
1,4-benzoquinone
3.9fold selectivity for Schistosoma mansoni over human enzyme
1,4-benzoquinone
3.9fold selectivity for Schistosoma mansoni over human enzyme
1-(2-methoxyphenyl)-3-naphthalen-1-ylurea
-
-
1-(2-methoxyphenyl)-3-naphthalen-1-ylurea
-
2-(1,1-difluoroethyl)-5-methyl-N-[4-(pentafluoro-lambda6-sulfanyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
i.e. DSM265
-
2-(1,1-difluoroethyl)-5-methyl-N-[4-(pentafluoro-lambda6-sulfanyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
i.e. DSM265
-
2-(2,3-dichloroanilino)-3-hydroxynaphthalene-1,4-dione
6.5fold selectivity for Schistosoma mansoni over human enzyme
-
2-(2,3-dichloroanilino)-3-hydroxynaphthalene-1,4-dione
6.5fold selectivity for Schistosoma mansoni over human enzyme
-
2-(2,6-dimethylanilino)-3-hydroxynaphthalene-1,4-dione
-
-
2-(2,6-dimethylanilino)-3-hydroxynaphthalene-1,4-dione
-
-
2-(2-chloroanilino)-3-hydroxynaphthalene-1,4-dione
10.4fold selectivity for Schistosoma mansoni over human enzyme
-
2-(2-chloroanilino)-3-hydroxynaphthalene-1,4-dione
10.4fold selectivity for Schistosoma mansoni over human enzyme
-
2-(3-chloroanilino)-3-hydroxynaphthalene-1,4-dione
7fold selectivity for Schistosoma mansoni over human enzyme
-
2-(3-chloroanilino)-3-hydroxynaphthalene-1,4-dione
7fold selectivity for Schistosoma mansoni over human enzyme
-
2-(4-biphenylylcarbamoyl)-1-cyclopentene-1-carboxylic acid
i.e. MD 108, 0.5 mM, 23% of initial activity
-
2-(4-biphenylylcarbamoyl)-1-cyclopentene-1-carboxylic acid
i.e. MD 108, 0.5 mM, 90% of initial activity
-
2-(4-chloroanilino)-3-hydroxynaphthalene-1,4-dione
2.9fold selectivity for Schistosoma mansoni over human enzyme
-
2-(4-chloroanilino)-3-hydroxynaphthalene-1,4-dione
2.9fold selectivity for Schistosoma mansoni over human enzyme
-
2-(4-fluoroanilino)-3-hydroxynaphthalene-1,4-dione
3fold selectivity for human over Schistosoma mansoni enzyme
-
2-(4-fluoroanilino)-3-hydroxynaphthalene-1,4-dione
3fold selectivity for human over Schistosoma mansoni enzyme
-
2-anilino-3-hydroxynaphthalene-1,4-dione
-
-
2-anilino-3-hydroxynaphthalene-1,4-dione
-
-
2-chloro-3-(methylamino)naphthalene-1,4-dione
-
-
2-chloro-3-(methylamino)naphthalene-1,4-dione
-
-
2-cyano-3-(9-ethyl-9H-carbazol-3-ylamino)acrylic acid ethyl ester
-
IC50: 0.491 mM
2-cyano-3-(9-ethyl-9H-carbazol-3-ylamino)acrylic acid ethyl ester
IC50: 0.00044 mM
2-cyano-3-cyclopropyl-3-hydroxy-N-[4'-(cyano)phenyl]-propenamide
-
50% inhibition at 0.0.00035 mM, N-terminally truncated protein
2-cyano-3-cyclopropyl-3-hydroxy-N-[4'-(cyano)phenyl]-propenamide
50% inhibition at 0.712 mM, N-terminally truncated protein
2-cyano-3-cyclopropyl-3-hydroxy-N-[4'-(nitro)phenyl]-propenamide
-
50% inhibition at 0.00025 mM, N-terminally truncated protein
2-cyano-3-cyclopropyl-3-hydroxy-N-[4'-(nitro)phenyl]-propenamide
50% inhibition at 0.543 mM, N-terminally truncated protein
2-cyano-3-cyclopropyl-3-hydroxy-N-[4'-(trifluoromethyl)phenyl]-propenamide
-
50% inhibition at 0.00019 mM, N-terminally truncated protein
2-cyano-3-cyclopropyl-3-hydroxy-N-[4'-(trifluoromethyl)phenyl]-propenamide
50% inhibition at 1.08 mM, N-terminally truncated protein
2-hydroxy-3-(3-methylbutyl)naphthalene-1,4-dione
30.8fold selectivity for Schistosoma mansoni over human enzyme
-
2-hydroxy-3-(3-methylbutyl)naphthalene-1,4-dione
30.8fold selectivity for Schistosoma mansoni over human enzyme
-
2-hydroxy-3-(4-methoxyanilino)naphthalene-1,4-dione
-
-
2-hydroxy-3-(4-methoxyanilino)naphthalene-1,4-dione
-
-
2-hydroxy-3-(4-phenylpiperazin-1-yl)naphthalene-1,4-dione
9.6fold selectivity for Schistosoma mansoni over human enzyme
-
2-hydroxy-3-(4-phenylpiperazin-1-yl)naphthalene-1,4-dione
9.6fold selectivity for Schistosoma mansoni over human enzyme
-
2-hydroxy-3-[3-(trifluoromethyl)anilino]naphthalene-1,4-dione
-
-
2-hydroxy-3-[3-(trifluoromethyl)anilino]naphthalene-1,4-dione
-
-
2-hydroxy-3-[4-(4-nitrophenyl)piperazin-1-yl]naphthalene-1,4-dione
-
-
2-hydroxy-3-[4-(4-nitrophenyl)piperazin-1-yl]naphthalene-1,4-dione
-
-
2-hydroxyethylidene-cyanoacetic acid 4-trifluoromethyl anilide
-
anti-proliferative effect of A77 1726 is mediated by inhibition of enzyme
2-hydroxyethylidene-cyanoacetic acid 4-trifluoromethyl anilide
-
inbibits by interference with the transfer of electrons from flavin to quinone
2-hydroxyethylidene-cyanoacetic acid 4-trifluoromethyl anilide
-
A77 1726, active metabolite of leflumonide
2-hydroxyethylidene-cyanoacetic acid 4-trifluoromethyl anilide
-
noncompetitive versus ubiquinone, uncompetitive versus dihydroorotate, study of kinetics
2-[(2,3-dihydro-1,4-benzodioxin-6-yl)amino]-3-hydroxynaphthalene-1,4-dione
2fold selectivity for human over Schistosoma mansoni enzyme
-
2-[(2,3-dihydro-1,4-benzodioxin-6-yl)amino]-3-hydroxynaphthalene-1,4-dione
2fold selectivity for human over Schistosoma mansoni enzyme
-
2-[(2,5-dichlorophenyl)sulfanyl]-5-ethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
compound has therapeutically relevant activity against human enzyme
2-[(2,5-dichlorophenyl)sulfanyl]-5-ethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
-
no specific inhibition of Plasmodium enzyme, good inhibitor of human enzyme
2-[(2,5-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
compound has therapeutically relevant activity against human enzyme
2-[(2,5-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
-
no specific inhibition of Plasmodium enzyme, good inhibitor of human enzyme
2-[(2H-1,3-benzodioxol-5-yl)amino]-3-hydroxynaphthalene-1,4-dione
-
-
2-[(2H-1,3-benzodioxol-5-yl)amino]-3-hydroxynaphthalene-1,4-dione
-
-
2-[(3,4-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
compound is less active with human enzyme but good inhibitor of Plasmodium falciparum enzyme
2-[(3,4-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
-
-
2-[(4-chlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
compound is less active with human enzyme but good inhibitor of Plasmodium falciparum enzyme
2-[(4-chlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
-
-
2-[(E)-2-(2-methylphenyl)ethenyl]quinolin-4-ol
-
-
2-[(E)-2-(2-methylphenyl)ethenyl]quinolin-4-ol
-
2-[4-(2,3-dichlorophenyl)piperazin-1-yl]-3-hydroxynaphthalene-1,4-dione
4.1fold selectivity for Schistosoma mansoni over human enzyme
-
2-[4-(2,3-dichlorophenyl)piperazin-1-yl]-3-hydroxynaphthalene-1,4-dione
4.1fold selectivity for Schistosoma mansoni over human enzyme
-
2-[4-(4-chlorophenyl)piperazin-1-yl]-3-hydroxynaphthalene-1,4-dione
20.3fold selectivity for Schistosoma mansoni over human enzyme
-
2-[4-(4-chlorophenyl)piperazin-1-yl]-3-hydroxynaphthalene-1,4-dione
20.3fold selectivity for Schistosoma mansoni over human enzyme
-
3-(3-methylbut-2-en-1-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl 4-methylbenzene-1-sulfonate
4.0fold selectivity for human over Schistosoma mansoni enzyme
-
3-(3-methylbut-2-en-1-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl 4-methylbenzene-1-sulfonate
4.0fold selectivity for human over Schistosoma mansoni enzyme
-
3-hydroxy-2-(3,3-dichloroallyl)-1,4-naphthoquinone
-
50% inhibition at 0.000065 mM, i. e. dichloroallyl lawsone, N-terminally truncated protein
3-hydroxy-2-(3,3-dichloroallyl)-1,4-naphthoquinone
50% inhibition at 0.220 mM, i. e. dichloroallyl lawsone, N-terminally truncated protein
4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
-
-
4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
-
-
4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
-
4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
-
-
4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
-
-
5,6-dimethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
5,6-dimethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
5-(1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
-
-
5-(1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
-
5-(1H-indol-1-yl)-N-propylthiophene-2-carboxamide
-
-
5-(1H-indol-1-yl)-N-propylthiophene-2-carboxamide
-
5-(2-methyl-1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
-
-
5-(2-methyl-1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
-
5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
-
-
5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
-
-
5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
-
5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
-
-
5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
-
-
5-(4-methylpiperazin-1-yl)-N-propylthiophene-2-carboxamide
-
-
5-(4-methylpiperazin-1-yl)-N-propylthiophene-2-carboxamide
-
5-(piperidin-1-yl)-N-propylthiophene-2-carboxamide
-
-
5-(piperidin-1-yl)-N-propylthiophene-2-carboxamide
-
5-ethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
5-ethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
5-methyl-7-(naphthalen-2-yloxy)[1,2,4]triazolo[1,5-a]pyrimidine
-
-
5-methyl-7-(naphthalen-2-yloxy)[1,2,4]triazolo[1,5-a]pyrimidine
-
5-methyl-7-(naphthalen-2-ylsulfanyl)[1,2,4]triazolo[1,5-a]pyrimidine
-
-
5-methyl-7-(naphthalen-2-ylsulfanyl)[1,2,4]triazolo[1,5-a]pyrimidine
-
5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
i.e. DSM1
5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
i.e. DSM74
5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
5-Methylorotate
-
-
6-methyl-N-phenyl-3aH-inden-4-amine
-
-
6-methyl-N-phenyl-3aH-inden-4-amine
-
A77 1726
-
active metabolite of leflunomide
A77 1726
-
malononitrilamide, 50% inhibition at 18-773 nM
A77 1726
-
active metabolite of the anti-rheumatic drug leflunomide
A77 1726
-
inhibits cell growth in multiple myeloma cell lines at clinically achievable concentrations by induction of apoptosis. Inhibition of cell growth is partly due to inhibition of multiple myeloma cell proliferation. A77 1726 shows synergistic and additive activity together with genotoxic agents melphalan, treosulfan, and doxorubicin
A77 1726
-
malononitrilamide, 50% inhibition at 18-773 nM
A77 1726
-
active metabolite of the anti-rheumatic drug leflunomide
A77 1726
-
malononitrilamide, 50% inhibition at 18-773 nM
A77-1726
-
50% inhibition at 0.00045 mM, wild-type, 0.00033 mM, DELTA2-21 mutant, 0.00031 mM, DELTA22-37 mutant, 0.00036 mM, DELTA2-37 mutant
A77-1726
0.5 mM, 14% of initial activity, inhibits the growth of Phytophthora infestans
A77-1726
-
potent inhibitor
A77-1726
0.5 mM, 97% of initial activity
ametoctradin
0.5 mM, 41% of initial activity
-
ametoctradin
0.5 mM,102% of initial activity
-
atovaquone
-
competitive to quinone
atovaquone
6.3fold selectivity for Schistosoma mansoni over human enzyme
atovaquone
0.5 mM, 127% of initial activity
atovaquone
-
competitive to quinone
atovaquone
-
50% inhibition at 0.000698 mM, wild-type enzyme, 0.000904 mM, DELTA1-29 mutant
atovaquone
6.3fold selectivity for Schistosoma mansoni over human enzyme
atovaquone
0.5 mM, 75% of initial activity
Barbituric acid
-
-
Barbituric acid
-
competitive to dihydroorotate, dead-end inhibitor
brequinar
-
50% inhibition at 0.567 mM, wild-type, 0.528 mM, DELTA2-21 mutant, 0.615 mM, DELTA22-37 mutant, 0.662 mM, DELTA2-37 mutant
brequinar
sensitive to brequinar at a 0.01 mM concentration
brequinar
540fold selectivity for human over Schistosoma mansoni enzyme
brequinar
0.5 mM, 98% of initial activity
brequinar
-
poor inhibitor
brequinar
-
50% inhibition at 0.000367 mM, wild-type enzyme, 0.000127 mM, DELTA1-29 mutant
brequinar
540fold selectivity for human over Schistosoma mansoni enzyme
brequinar
0.5 mM, 49% of initial activity
brequinar sodium
-
complete activity termination in all tissues at 0.01 mM
brequinar sodium
1 mM reduces the activity by more than 50% of the full-length enzyme
brequinar sodium
-
complete activity termination in all tissues at 0.01 mM
brequinar sodium
-
tight binding, most potent inhibitor, mutant H26A is insensitive, wild-type and other mutants are inhibited by 50% at concentrations between 6 and 10 nM
brequinar sodium
-
potent, noncompetitive inhibitor
brequinar sodium
-
more active than A77 1726 and HR325
brequinar sodium
-
50% inhibition at 6-127 nM
brequinar sodium
-
complete activity termination in all tissues at 0.01 mM
brequinar sodium
-
inbibits by interference with the transfer of electrons from flavin to quinone
brequinar sodium
-
competitive versus ubiquinone, uncompetitive versus dihydroorotate, study of kinetics
brequinar sodium
-
50% inhibition at 6-127 nM
brequinar sodium
-
complete activity termination in all tissues at 0.01 mM
brequinar sodium
-
50% inhibition at 6-127 nM
brequinar sodium
complete activity termination in all tissues at 0.01 mM
brequinar sodium
-
complete activity termination in all tissues at 0.01 mM
dichloroallyl lawsone
-
50% inhibition at 0.00051 mM, wild-type, 0.00031 mM, DELTA2-21 mutant, 0.00020 mM, DELTA22-37 mutant, 0.00021 mM, DELTA2-37 mutant
dichloroallyl lawsone
0.5 mM, 30% of initial activity
dichloroallyl lawsone
0.5 mM, 39% of initial activity
dichloroallyl-lawsone
-
competitive to quinone
dichloroallyl-lawsone
-
competitive to quinone
diethyl [(dibenzo[b,d]thiophen-2-ylamino)methylidene]propanedioate
-
-
diethyl [(dibenzo[b,d]thiophen-2-ylamino)methylidene]propanedioate
-
diethyldicarbonate
-
histidine-selective covalent modifier
diethyldicarbonate
-
histidine-selective covalent modifier; histidine-selective modifying agent, dose-dependent
ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
-
-
ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
-
-
ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
-
ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
-
-
ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
-
-
fatty acids
-
-
fatty acids
-
noncompetitive with respect to ubiquinone
Genz-667348
-
-
Genz-668857
-
-
Genz-669178
-
-
isolapachol
8.3fold selectivity for Schistosoma mansoni over human enzyme
-
isolapachol
8.3fold selectivity for Schistosoma mansoni over human enzyme
-
Lapachol
-
-
Lapachol
5.3fold selectivity for Schistosoma mansoni over human enzyme
Lapachol
5.3fold selectivity for Schistosoma mansoni over human enzyme
Lawsone
-
-
leflunomide
-
-
leflunomide
-
poor inhibitor
MNA 279
-
malononitrilamide, 50% inhibition at 22-715 nM
MNA 279
-
malononitrilamide, 50% inhibition at 22-715 nM
MNA 279
-
malononitrilamide, 50% inhibition at 22-715 nM
MNA 715
-
malononitrilamide, 50% inhibition at 41-109 nM
MNA 715
-
malononitrilamide, 50% inhibition at 41-109 nM
MNA 715
-
malononitrilamide, 50% inhibition at 41-109 nM
N-(2,4-dichlorophenyl)naphthalene-2-carboxamide
-
-
N-(2,4-dichlorophenyl)naphthalene-2-carboxamide
-
N-(2-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
N-(2-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(2-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
N-(2-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide
-
-
N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide
-
50% inhibition at 0.00002 mM, wild type, 0.0004 mM, mutant R265A, 0.13, mutant H185A
N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide
-
N-(3-chloro-2-methoxybiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
i.e. MD 209, 0.5 mM, 2% of initial activity
-
N-(3-chloro-2-methoxybiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
i.e. MD 209, 0.5 mM, 0% of initial activity
-
N-(3-chlorobiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
i.e. MD 241, 0.5 mM, 1% of initial activity
-
N-(3-chlorobiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
i.e. MD 241, 0.5 mM, 87% of initial activity
-
N-(3-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
N-(3-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(3-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
N-(3-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
N-(3-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(3-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
N-(4-bromophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
N-(4-bromophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(4-bromophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
N-(4-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
N-(4-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(4-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
N-(anthracen-2-yl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
N-(anthracen-2-yl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-(anthracen-2-yl)-N,5-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
N-(anthracen-2-yl)-N,5-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-cyclopropyl-5-(2,3-dihydro-4H-1,4-benzothiazin-4-yl)thiophene-2-carboxamide
-
-
N-cyclopropyl-5-(2,3-dihydro-4H-1,4-benzothiazin-4-yl)thiophene-2-carboxamide
-
N-cyclopropyl-5-(2,3-dihydro-4H-1,4-benzothiazin-4-yl)thiophene-2-carboxamide
-
-
N-propyl-5-(1H-pyrazol-1-yl)thiophene-2-carboxamide
-
-
N-propyl-5-(1H-pyrazol-1-yl)thiophene-2-carboxamide
-
N-[3,5-difluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
i.e. DSM190, 0.5 mM, 36% of initial activity
-
N-[3,5-difluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
i.e. DSM190, 0.5 mM, 38% of initial activity
-
N-[3-fluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
N-[3-fluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
N-[3-fluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
NSC 61890
0.5 mM, 93% of initial activity
-
NSC 61890
0.5 mM, 36% of initial activity
-
Orotate
-
-
Orotate
-
competitive to dihydroorotate
Orotate
-
competitive to dihydroorotate
Orotate
-
also inhibitors: 5-substituted orotates; competitive to dihydroorotate; strong competitive inhibitor
redoxal
0.5 mM exhibit an inhibitory effect of more than 50% on full-length DHODH and N-terminally truncated DHODH compared with the noninhibited reaction
redoxal
-
50% inhibition at 0.029 mM, wild-type, 0.057 mM, DELTA2-21 mutant, 0.040 mM, DELTA22-37 mutant, 0.056 mM, DELTA2-37 mutant
redoxal
-
50% inhibition at 45-88 nM
redoxal
-
50% inhibition at 0.000013 mM, N-terminally truncated protein
redoxal
-
50% inhibition at 45-88 nM
redoxal
0.5 mM, 31% of initial activity
redoxal
50% inhibition at 0.071 mM, N-terminally truncated protein
redoxal
-
50% inhibition at 45-88 nM
redoxal
0.5 mM, 39% of initial activity
teriflunomide
-
a redox-silent coenzyme Q antagonist of DHODH
teriflunomide
160fold selectivity for human over Schistosoma mansoni enzyme
teriflunomide
160fold selectivity for human over Schistosoma mansoni enzyme
Thenoyltrifluoroacetone
-
-
Thenoyltrifluoroacetone
-
-
toltrazuril
-
50% inhibition at 0.1 mM
toltrazuril
-
50% inhibition at 0.1 mM
toltrazuril
-
50% inhibition at 0.1 mM
toltrazuril
-
50% inhibition at 0.1 mM
toltrazuril
1 mM, 67% of initial activity
toltrazuril
50% inhibition at 0.1 mM
toltrazuril
1 mM, 0% of initial activity
toltrazuril
-
50% inhibition at 0.1 mM
[2-fluoro-2',5'-dimethyl-4'-[6-(3-methyl-2-butenyloxy)pyridin-3-yl]biphenyl-4-yl]-(3-methyl-2-butenyl)amine
-
i.e. S-2678, suppresses immunoglobulin production in human peripheral blood mononuclear cells in vitro, with little or no inhibition of cell proliferation
[2-fluoro-2',5'-dimethyl-4'-[6-(3-methyl-2-butenyloxy)pyridin-3-yl]biphenyl-4-yl]-(3-methyl-2-butenyl)amine
-
i.e. S-2678, suppresses immunoglobulin production in mouse B cells in vitro, with little or no inhibition of cell proliferation, probably through inhibition of class switch recombination in the immunoglobulin heavy chain loci in B cells. In vivo antibody production induced by systemic immunization with ovalbumin is dramatically suppressed by oral administration of S-2678, without any toxicological signs. S-2678 does not affect T-cell activation in vitro, and cytokine production induced by intravenous anti-CD3 antibody in mice. S-2678 does not affect host defense in a mouse model of Candida infection, whereas leflunomide severely impaires it
[[3-(3-methylbut-2-en-1-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl]oxy]acetonitrile
-
-
[[3-(3-methylbut-2-en-1-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl]oxy]acetonitrile
-
-
additional information
-
kinetics of inhibition
-
additional information
competitive nature of small molecule inhibitors toward the putative ubiquinone binding site
-
additional information
-
competitive nature of small molecule inhibitors toward the putative ubiquinone binding site
-
additional information
-
DHODH-specific inhibitors with low nanomolar binding affinities bind in the N-terminal hydrophobic channel of dihydroorotate dehydrogenase, the presumed site of ubiquinone binding during oxidation of dihydroorotate to orotate
-
additional information
-
screening for potent inhibitors of PfDHODH and effect on the human enzyme, overview. The compiunds show strong selectivity for the malarial enzyme over that from the human host, inhibition mechanism, overview
-
additional information
synthesis of a series of 2-substituted quinoline-4-carboxylic acids by Doebner reaction starting from freely available protocatechuic aldehyde and vanillin precursors. Human dihydroorotate dehydrogenase (hDHODH) is recognised as a clear molecular target for these heterocycles. All compounds are also tested for their antiproliferative potential against three cancer cells (MCF-7, A549, A375) and one normal cell line (HaCaT) to evaluate the selective cytotoxicity, overview. IC50 for cytotoxicity in in vivo assays. Molecular docking studies
-
additional information
-
synthesis of a series of 2-substituted quinoline-4-carboxylic acids by Doebner reaction starting from freely available protocatechuic aldehyde and vanillin precursors. Human dihydroorotate dehydrogenase (hDHODH) is recognised as a clear molecular target for these heterocycles. All compounds are also tested for their antiproliferative potential against three cancer cells (MCF-7, A549, A375) and one normal cell line (HaCaT) to evaluate the selective cytotoxicity, overview. IC50 for cytotoxicity in in vivo assays. Molecular docking studies
-
additional information
two potential residues, T63 and Y356, suitable for H-bonding interactions, are identified in the brequinar-binding pocket, design, synthesis, and biological evaluation of 4-quinoline carboxylic acids as inhibitors of dihydroorotate dehydrogenase, overview. Cytotoxicity and bioavalability assays using HCT-116 and MIA PaCa-2 canvcer cells
-
additional information
-
drug screening and identification of a series of N-alkyl-5-(1H-benzimidazol-1-yl)thiophene-2-carboxamides with low nanomolar in vitro potency against DHODH, selective for the parasite enzymes over human DHODH, tolerability in the mouse, overview
-
additional information
DHODH-specific inhibitors with low nanomolar binding affinities bind in the N-terminal hydrophobic channel of dihydroorotate dehydrogenase, the presumed site of ubiquinone binding during oxidation of dihydroorotate to orotate
-
additional information
-
DHODH-specific inhibitors with low nanomolar binding affinities bind in the N-terminal hydrophobic channel of dihydroorotate dehydrogenase, the presumed site of ubiquinone binding during oxidation of dihydroorotate to orotate
-
additional information
development and evaluation of triazolopyrimidine-based DHODH inhibitors, overview. Detailed quantitative structure-activity relationship study and molecular docking studies, the 2-methyltriazolopyrimidine ring interacts with some polar and some nonpolar amino acids whereas the substituted phenyl ring binds with a hydrophobic pocket of the enzyme formed by some nonpolar amino acid residues, overview
-
additional information
screening for potent inhibitors of PfDHODH that show strong selectivity for the malarial enzyme over that from the human host. Lead optimization of a triazolopyrimidine-based series, inhibition mechanism, overview
-
additional information
-
screening for potent inhibitors of PfDHODH that show strong selectivity for the malarial enzyme over that from the human host. Lead optimization of a triazolopyrimidine-based series, inhibition mechanism, overview
-
additional information
drug screening and identifictaion of a series of N-alkyl-5-(1H-benzimidazol-1-yl)thiophene-2-carboxamides with low nanomolarin vitro potency against DHODH, selective for the parasite enzymes over human DHODH, tolerability in the mouse, overview
-
additional information
-
drug screening and identifictaion of a series of N-alkyl-5-(1H-benzimidazol-1-yl)thiophene-2-carboxamides with low nanomolarin vitro potency against DHODH, selective for the parasite enzymes over human DHODH, tolerability in the mouse, overview
-
additional information
-
identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice, overview
-
additional information
-
drug screening and identification of a series of N-alkyl-5-(1H-benzimidazol-1-yl)thiophene-2-carboxamides with low nanomolar in vitro potency against DHODH, selective for the parasite enzymes over human DHODH, tolerability in the mouse, overview
-
additional information
-
not: bathophenathroline, sulfonate, ethylendiaminetetraacetate, cyanide, azide
-
additional information
-
kinetics of inhibition
-
additional information
-
not inhibitory: brequinar, atovaquone, N-(3,5-difluoro-4-(trifluoromethyl)phenyl)-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.000117 - 0.0925
(2Z)-2-cyano-3-cyclopropyl-3-hydroxy-N-[4-(trifluoromethyl)phenyl]prop-2-enamide
-
0.00018 - 0.004
(2Z)-2-cyano-N-(2',3-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
-
0.000022 - 0.165
(2Z)-2-cyano-N-(2,2'-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
-
0.00019 - 0.2366
(2Z)-2-cyano-N-(2,3'-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
-
0.00013 - 0.182
(2Z)-2-cyano-N-(3'-ethoxybiphenyl-4-yl)-3-hydroxybut-2-enamide
-
0.00013 - 0.0474
(2Z)-N-(2'-chlorobiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
-
0.0002 - 0.0086
(2Z)-N-(3-chloro-2'-methoxybiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
-
0.00009 - 0.0257
(2Z)-N-(biphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
0.00017 - 0.0062
(2Z)-N-[2'-chloro-3-(trifluoromethyl)biphenyl-4-yl]-2-cyano-3-hydroxybut-2-enamide
-
0.0088 - 0.034
1,4-benzoquinone
0.00385
1-(2-((3,4-dimethylphenyl)amino)-4-methylthiazol-5-yl)-ethanone
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.00394
1-(2-((3-chloro-4-methylphenyl)amino)-4-methylthiazol-5-yl)ethanone
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.01
1-(2-((3-fluoro-4-methylphenyl)amino)-4-methylthiazol-5-yl)ethanone
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.00365
1-(2-((4-(tert-butyl)phenyl)amino)-4-methylthiazol-5-yl)-ethanone
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.00193
1-(2-((4-bromo-3-(trifluoromethyl)phenyl)amino)-4-methylthiazol-5-yl)ethanone
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.01
1-(2-((4-bromophenyl)amino)-4-methylthiazol-5-yl)-ethanone
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.00235
1-(2-((4-chloro-3-(trifluoromethyl)phenyl)amino)-4-methylthiazol-5-yl)ethanone
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.01
1-(2-(anthracen-2-ylamino)-4-methylthiazol-5-yl)ethan-1-one
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.00023 - 0.11
1-(2-methoxyphenyl)-3-naphthalen-1-ylurea
0.000562
1-(4-methyl-2-(naphthalen-2-ylamino)thiazol-5-yl)ethan-1-one
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.01
1-(4-methyl-2-(phenylamino)thiazol-5-yl)ethanone
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000554 - 1.635
1-hydroxy-2-dodecyl-4(1)quinolone
0.00076
10-phenyl-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.000077
2,8-dimethyl-N-[4-(trifluoromethyl)phenyl]pyrrolo[1,2-a]pyrimidin-4-amine
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.007 - 0.021
2-(1,1-difluoroethyl)-5-methyl-N-[4-(pentafluoro-lambda6-sulfanyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
0.0000118
2-(2'-fluoro-[1,1'-biphenyl]-4-yl)-3-methyl-6-(trifluoromethyl)-1,7-naphthyridine-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000127
2-(2'-methoxy-[1,1'-biphenyl]-4-yl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.268
2-(2,3-bis(benzyloxy)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000123 - 0.00019
2-(2,3-dichloroanilino)-3-hydroxynaphthalene-1,4-dione
-
0.34
2-(2,4-bis(benzyloxy)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
2.549
2-(2,4-dimethoxyphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.0099 - 0.01
2-(2,6-dimethylanilino)-3-hydroxynaphthalene-1,4-dione
-
0.000078 - 0.000808
2-(2-chloroanilino)-3-hydroxynaphthalene-1,4-dione
-
0.27
2-(3,4-bis(benzyloxy)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.153
2-(3,4-dibutoxyphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
1.073
2-(3,4-dihydroxyphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.148
2-(3,4-diisobutoxyphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
1.387
2-(3,4-dimethoxyphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.384
2-(3,4-dipropoxyphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000129 - 0.000911
2-(3-chloroanilino)-3-hydroxynaphthalene-1,4-dione
-
0.449
2-(3-methoxy-4-propoxyphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.0084
2-(4-(1H-imidazol-1-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000148
2-(4-(2-(trifluoromethyl)pyridin-3-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.00526
2-(4-(2-chloro-6-methylpyridin-3-yl)phenyl)-3-methyl-1,7-naphthyridine-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000184
2-(4-(2-chloro-6-methylpyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.0000262
2-(4-(2-chloro-6-methylpyridin-3-yl)phenyl)-6-fluoro-3-methylquinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000235
2-(4-(2-chloro-6-methylpyridin-3-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.0000542
2-(4-(2-chloropyridin-3-yl)phenyl)-3,6-dimethylquinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000259
2-(4-(2-chloropyridin-3-yl)phenyl)-3-methyl-1,7-naphthyridine-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000201
2-(4-(2-chloropyridin-3-yl)phenyl)-3-methyl-6-(trifluoromethyl)-1,7-naphthyridine-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.0000543
2-(4-(2-chloropyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.00000971
2-(4-(2-chloropyridin-3-yl)phenyl)-6-fluoro-3-methylquinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.0000327
2-(4-(2-chloropyridin-3-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.00248
2-(4-(2-fluoro-6-methylpyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000504
2-(4-(2-fluoropyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.00142
2-(4-(2-fluoropyridin-3-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000165
2-(4-(2-methoxypyridin-3-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.0000221
2-(4-(2-methylpyridin-3-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.00143
2-(4-(4-(trifluoromethyl)pyridin-3-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000373
2-(4-(4-methylpyridin-3-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.0125
2-(4-(6-fluoropyridin-3-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.467
2-(4-(benzyloxy)-3-methoxyphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.00807
2-(4-(piperidin-1-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.00801 - 0.2
2-(4-(pyridazin-3-yl)phenyl)quinoline-4-carboxylic acid
-
0.0101
2-(4-(pyridin-2-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000391
2-(4-(pyridin-3-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.00755
2-(4-(pyridin-4-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.2
2-(4-(pyrimidin-2-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.34
2-(4-butoxy-3-methoxyphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000185 - 0.000541
2-(4-chloroanilino)-3-hydroxynaphthalene-1,4-dione
-
0.00025
2-(4-cyclohexylphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.00033 - 0.001
2-(4-fluoroanilino)-3-hydroxynaphthalene-1,4-dione
-
0.944
2-(4-hydroxy-3-methoxyphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.438
2-(4-isobutoxy-3-methoxyphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.00104
2-(4-isobutylphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.00341
2-(4-isopropylphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.144
2-(4-methylphenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.2
2-(4-morpholinophenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.00279
2-([1,1'-biphenyl]-4-yl)-3-methyl-1,6-naphthyridine-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.0000283
2-([1,1'-biphenyl]-4-yl)-3-methyl-1,7-naphthyridine-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.00122
2-([1,1'-biphenyl]-4-yl)-3-methyl-1,8-naphthyridine-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.0000212
2-([1,1'-biphenyl]-4-yl)-3-methyl-6-(trifluoromethyl)-1,7-naphthyridine-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.0000754
2-([1,1'-biphenyl]-4-yl)-3-methylquinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000051
2-([1,1'-biphenyl]-4-yl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.0021 - 0.0026
2-anilino-3-hydroxynaphthalene-1,4-dione
-
0.079
2-chloro-3-(methylamino)naphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.00044 - 0.491
2-cyano-3-(9-ethyl-9H-carbazol-3-ylamino)acrylic acid ethyl ester
0.096
2-cyano-3-hydroxy-N-(2',3,3'-trichlorobiphenyl-4-yl)but-2-enamide
Toxoplasma gondii
-
pH 8.0, 30°C
0.000023 - 0.000709
2-hydroxy-3-(3-methylbutyl)naphthalene-1,4-dione
-
0.0047
2-hydroxy-3-(4-methoxyanilino)naphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.000711 - 0.0068
2-hydroxy-3-(4-phenylpiperazin-1-yl)naphthalene-1,4-dione
-
0.000108 - 0.000111
2-hydroxy-3-[3-(trifluoromethyl)anilino]naphthalene-1,4-dione
-
0.00038
2-hydroxy-3-[4-(4-nitrophenyl)piperazin-1-yl]naphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.091
2-hydroxyethylidene-cyano acetic acid 4-trifluoromethyl anilide
Toxoplasma gondii
-
pH 8.0, 30°C
0.057
2-methylcyclohexa-2,5-diene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
0.768
2-tert-butylcyclohexa-2,5-diene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.00105 - 0.0021
2-[(2,3-dihydro-1,4-benzodioxin-6-yl)amino]-3-hydroxynaphthalene-1,4-dione
-
0.000013 - 0.1
2-[(2,5-dichlorophenyl)sulfanyl]-5-ethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
0.000051 - 0.011
2-[(2,5-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
0.0036 - 0.0055
2-[(2H-1,3-benzodioxol-5-yl)amino]-3-hydroxynaphthalene-1,4-dione
-
0.0019 - 0.0065
2-[(3,4-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
0.001 - 0.039
2-[(4-chlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
0.00093 - 0.03
2-[(E)-2-(2-methylphenyl)ethenyl]quinolin-4-ol
0.00044 - 0.0018
2-[4-(2,3-dichlorophenyl)piperazin-1-yl]-3-hydroxynaphthalene-1,4-dione
-
0.00028 - 0.0046
2-[4-(4-chlorophenyl)piperazin-1-yl]-3-hydroxynaphthalene-1,4-dione
-
0.001
2-[[(4-chlorophenyl)methyl]sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7(4H)-one
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.00144
3-(3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazol-9-yl)phenol
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.0079 - 0.0314
3-(3-methylbut-2-en-1-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl 4-methylbenzene-1-sulfonate
-
0.00181
4-(3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazol-9-yl)phenol
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00182
4-(6-imino-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-9-yl)benzamide
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00011 - 0.03
4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
0.00016
5,6-dimethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.00047 - 0.0007
5-(1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
0.00046 - 0.00071
5-(1H-indol-1-yl)-N-propylthiophene-2-carboxamide
0.00017 - 0.00063
5-(2-methyl-1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
0.000042 - 0.03
5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
0.01 - 0.03
5-(4-methylpiperazin-1-yl)-N-propylthiophene-2-carboxamide
0.01 - 0.03
5-(piperidin-1-yl)-N-propylthiophene-2-carboxamide
0.00019
5-ethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.000081
5-methoxy-2-[(4-phenoxyphenyl)amino]benzoic acid
Homo sapiens
pH 8.0, 22°C
0.0017
5-methyl-7-(naphthalen-2-yloxy)[1,2,4]triazolo[1,5-a]pyrimidine
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.1
5-methyl-7-(naphthalen-2-ylsulfanyl)[1,2,4]triazolo[1,5-a]pyrimidine
Plasmodium falciparum
above, pH not specified in the publication, temperature not specified in the publication
0.000047 - 0.2
5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
0.00028 - 0.025
5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
0.000015
6-chloro-2-(2'-fluorobiphenyl-4-yl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
0.0000744
6-chloro-2-(4-(2-chloro-6-methylpyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000036
6-chloro-2-(4-(2-chloropyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000165
6-chloro-2-(4-(2-fluoropyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.00331
6-fluoro-2-(4-(2-fluoro-6-methylpyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.0000794
6-fluoro-2-(4-(2-fluoropyridin-3-yl)phenyl)-3-methylquinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.1
6-methyl-N-phenyl-3aH-inden-4-amine
Plasmodium falciparum
above, pH not specified in the publication, temperature not specified in the publication
0.00129
8-(1,3,3a,4-tetrahydro-2-benzofuran-4-yl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.0011
8-(1,8a-dihydronaphthalen-1-yl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00153
8-(oxolan-2-yl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00148
8-(pyridin-3-yl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00094
8-(thiolan-3-yl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.0013
9-(1-benzofuran-2-yl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00097
9-(2,3-dihydro-1,4-benzodioxin-6-yl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00118
9-(2-methoxyphenyl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00115
9-(2-nitrophenyl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00118
9-(2H-1,3-benzodioxol-5-yl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00152
9-(3-ethylphenyl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.0013
9-(4-nitrophenyl)-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00107
9-(4-phenoxyphenyl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00096
9-(isoquinolin-6-yl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00085
9-(naphthalen-1-yl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00065
9-(naphthalen-2-yl)-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00068
9-phenyl-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00151
9-phenyl-3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazole
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00107
9-[(E)-2-phenylethenyl]-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00156
9-[3-[(propan-2-yl)oxy]phenyl]-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00096
9-[4-(methylsulfanyl)phenyl]-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00143
9-[4-(trifluoromethoxy)phenyl]-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00043 - 0.0027
atovaquone
0.00016 - 0.03
diethyl [(dibenzo[b,d]thiophen-2-ylamino)methylidene]propanedioate
0.000026
ethyl 2-((2,3-dihydro-1h-inden-5-yl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.01
ethyl 2-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000174
ethyl 2-((3,4-dichlorophenyl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.001358
ethyl 2-((3,4-dimethylphenyl)amino)-4-methylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000058
ethyl 2-((3,4-dimethylphenyl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000393
ethyl 2-((3,5-dichlorophenyl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000311
ethyl 2-((3,5-difluoro-3'-methoxy-[1,1'-biphenyl]-4-yl)-amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.01
ethyl 2-((3-chloro-4-((2-chloro-6-fluorobenzyl)oxy)phenyl)-amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000372
ethyl 2-((3-chloro-4-methylphenyl)amino)-4-cyclopropylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000969
ethyl 2-((3-chloro-4-methylphenyl)amino)-4-methylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000035
ethyl 2-((3-chloro-4-methylphenyl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.01
ethyl 2-((3-chloro-4-phenoxyphenyl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.01
ethyl 2-((3-fluoro-3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.001987
ethyl 2-((3-fluoro-4-methylphenyl)amino)-4-methylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000049
ethyl 2-((3-fluoro-4-methylphenyl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.01
ethyl 2-((3-fluoro-[1,1'-biphenyl]-4-yl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.01
ethyl 2-((4-(benzyloxy)-3-chlorophenyl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000284
ethyl 2-((4-(tert-butyl)phenyl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.01
ethyl 2-((4-bromo-2-methylphenyl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000128
ethyl 2-((4-bromo-3-(trifluoromethyl)phenyl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.00907
ethyl 2-((4-bromophenyl)amino)-4-methylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.00604
ethyl 2-((4-chloro-3-(trifluoromethyl)phenyl)amino)-4-(cyclopropanecarboxamido)thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000131
ethyl 2-((4-chloro-3-(trifluoromethyl)phenyl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000239
ethyl 2-((4-chlorophenyl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.00144
ethyl 2-((4-methoxyphenyl)amino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000453
ethyl 2-(anthracen-2-ylamino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.001108
ethyl 2-(benzo[d][1,3]dioxol-5-ylamino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000029
ethyl 2-(naphthalen-2-ylamino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.01
ethyl 2-([1,1'-biphenyl]-4-ylamino)-4-phenylthiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.00004 - 0.03
ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
0.01
ethyl 4-(cyclopropanecarboxamido)-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000515
ethyl 4-(tert-butyl)-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000552
ethyl 4-(tert-butyl)-2-((3-chloro-4-methylphenyl)amino)-thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000652
ethyl 4-(tert-butyl)-2-((3-fluoro-4-methylphenyl)amino)-thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.00211
ethyl 4-amino-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.01
ethyl 4-amino-2-((4-chloro-3-(trifluoromethyl)phenyl)-amino)thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.00903
ethyl 4-benzamido-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.01
ethyl 4-benzamido-2-((4-chloro-3-(trifluoromethyl)phenyl)-amino)thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000325
ethyl 4-cyclopropyl-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000645
ethyl 4-cyclopropyl-2-((4-fluoro-3-methylphenyl)amino)-thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000887
ethyl 4-methyl-2-(naphthalen-2-ylamino)thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000408
ethyl 4-phenyl-2-((4-(trifluoromethyl)phenyl)amino)-thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000018
ethyl 4-phenyl-2-((5,6,7,8-tetrahydronaphthalen-2-yl)-amino)thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000784
ethyl 4-phenyl-2-(phenylamino)thiazole-5-carboxylate
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000014 - 0.000042
Genz-667348
0.000012 - 0.000044
Genz-668857
0.000015 - 0.00005
Genz-669178
0.0012 - 0.01
isolapachol
-
0.000019 - 0.0001
Lapachol
0.029
Lawsone
Schistosoma mansoni
pH 8.2, 25°C
0.0009
leflunomide
Homo sapiens
pH 8.0, 22°C
0.05
methyl 2-(4-(4-(trifluoromethyl)pyridin-3-yl)phenyl)quinoline-4-carboxylate
Homo sapiens
pH 8.0, 22°C
-
0.2
methyl 2-(4-(piperidin-1-yl)phenyl)quinoline-4-carboxylate, methyl 2-(4-(pyridin-3-yl)phenyl)quinoline-4-carboxylate, methyl 2-(4-cyclohexylphenyl)quinoline-4-carboxylate, methyl 2-([1,1'-biphenyl]-4-yl)quinoline-4-carboxylate
Homo sapiens
pH 8.0, 22°C
-
0.00143
methyl 3-(3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazol-9-yl)benzoate
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00115
methyl 4-(3,4-dihydro-2H-pyrimido[1,2-b][1,2]benzothiazol-9-yl)benzoate
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00122
methyl 4-(6-imino-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-9-yl)benzoate
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00005 - 0.05
N-(2,4-dichlorophenyl)naphthalene-2-carboxamide
0.1
N-(2-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
above, pH not specified in the publication, temperature not specified in the publication
0.1
N-(2-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
above, pH not specified in the publication, temperature not specified in the publication
0.049 - 12
N-(3,5-dichloro-phenyl)-2-methyl-3-nitro-benzamide
0.000016 - 0.2
N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide
0.06
N-(3-chloro-2'-methoxybiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
Toxoplasma gondii
-
pH 8.0, 30°C
0.00068 - 0.0014
N-(3-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
0.0005 - 0.0092
N-(3-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
0.00078
N-(4-bromophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.019
N-(4-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.000056 - 0.0007
N-(anthracen-2-yl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
0.003
N-(anthracen-2-yl)-N,5-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.00021 - 0.0044
N-anthracen-2-yl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
0.00025 - 0.00038
N-cyclopropyl-5-(2,3-dihydro-4H-1,4-benzothiazin-4-yl)thiophene-2-carboxamide
0.01 - 0.03
N-propyl-5-(1H-pyrazol-1-yl)thiophene-2-carboxamide
0.000077 - 0.00021
N-[3-fluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
0.000163 - 0.05
teriflunomide
0.00076
trifluoromethyl 6-(6-imino-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-9-yl)-1H-indole-3-carboxylate
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.00121
[4-(6-imino-3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-9-yl)phenyl](4-[[(prop-2-yn-1-yl)oxy]methyl]phenyl)methanone
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
-
0.0025
[[3-(3-methylbut-2-en-1-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl]oxy]acetonitrile
Schistosoma mansoni
pH 8.2, 25°C
-
additional information
A77 1726
0.000117
(2Z)-2-cyano-3-cyclopropyl-3-hydroxy-N-[4-(trifluoromethyl)phenyl]prop-2-enamide
Homo sapiens
-
-
0.0925
(2Z)-2-cyano-3-cyclopropyl-3-hydroxy-N-[4-(trifluoromethyl)phenyl]prop-2-enamide
Plasmodium falciparum
-
-
0.00018
(2Z)-2-cyano-N-(2',3-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
Homo sapiens
-
-
0.004
(2Z)-2-cyano-N-(2',3-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
Plasmodium falciparum
-
-
0.000022
(2Z)-2-cyano-N-(2,2'-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
Homo sapiens
-
-
0.165
(2Z)-2-cyano-N-(2,2'-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
Plasmodium falciparum
-
-
0.00019
(2Z)-2-cyano-N-(2,3'-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
Homo sapiens
-
-
0.2366
(2Z)-2-cyano-N-(2,3'-dichlorobiphenyl-4-yl)-3-hydroxybut-2-enamide
Plasmodium falciparum
-
-
0.00013
(2Z)-2-cyano-N-(3'-ethoxybiphenyl-4-yl)-3-hydroxybut-2-enamide
Homo sapiens
-
-
0.182
(2Z)-2-cyano-N-(3'-ethoxybiphenyl-4-yl)-3-hydroxybut-2-enamide
Plasmodium falciparum
-
-
0.00013
(2Z)-N-(2'-chlorobiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
Homo sapiens
-
-
0.0474
(2Z)-N-(2'-chlorobiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
Plasmodium falciparum
-
-
0.0002
(2Z)-N-(3-chloro-2'-methoxybiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
Homo sapiens
-
-
0.0086
(2Z)-N-(3-chloro-2'-methoxybiphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
Plasmodium falciparum
-
-
0.00009
(2Z)-N-(biphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
Homo sapiens
-
0.0257
(2Z)-N-(biphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide
Plasmodium falciparum
-
0.00017
(2Z)-N-[2'-chloro-3-(trifluoromethyl)biphenyl-4-yl]-2-cyano-3-hydroxybut-2-enamide
Homo sapiens
-
-
0.0062
(2Z)-N-[2'-chloro-3-(trifluoromethyl)biphenyl-4-yl]-2-cyano-3-hydroxybut-2-enamide
Plasmodium falciparum
-
-
0.0088
1,4-benzoquinone
Schistosoma mansoni
pH 8.2, 25°C
0.034
1,4-benzoquinone
Homo sapiens
pH 8.2, 25°C
0.00023
1-(2-methoxyphenyl)-3-naphthalen-1-ylurea
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.11
1-(2-methoxyphenyl)-3-naphthalen-1-ylurea
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000554
1-hydroxy-2-dodecyl-4(1)quinolone
Toxoplasma gondii
-
wild type enzyme, at pH 8.0 and 25°C
0.001635
1-hydroxy-2-dodecyl-4(1)quinolone
Toxoplasma gondii
-
mutant enzyme N302S, at pH 8.0 and 25°C
0.554
1-hydroxy-2-dodecyl-4(1)quinolone
Toxoplasma gondii
-
wild-type, pH 8.0, 22°C
1.635
1-hydroxy-2-dodecyl-4(1)quinolone
Toxoplasma gondii
-
mutant N302S, pH 8.0, 22°C
0.007
2-(1,1-difluoroethyl)-5-methyl-N-[4-(pentafluoro-lambda6-sulfanyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Homo sapiens
pH 8.2, 25°C
-
0.021
2-(1,1-difluoroethyl)-5-methyl-N-[4-(pentafluoro-lambda6-sulfanyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Schistosoma mansoni
pH 8.2, 25°C
-
0.000123
2-(2,3-dichloroanilino)-3-hydroxynaphthalene-1,4-dione
Homo sapiens
pH 8.2, 25°C
-
0.00019
2-(2,3-dichloroanilino)-3-hydroxynaphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.0099
2-(2,6-dimethylanilino)-3-hydroxynaphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.01
2-(2,6-dimethylanilino)-3-hydroxynaphthalene-1,4-dione
Homo sapiens
pH 8.2, 25°C
-
0.000078
2-(2-chloroanilino)-3-hydroxynaphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.000808
2-(2-chloroanilino)-3-hydroxynaphthalene-1,4-dione
Homo sapiens
pH 8.2, 25°C
-
0.000129
2-(3-chloroanilino)-3-hydroxynaphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.000911
2-(3-chloroanilino)-3-hydroxynaphthalene-1,4-dione
Homo sapiens
pH 8.2, 25°C
-
0.00801
2-(4-(pyridazin-3-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.2
2-(4-(pyridazin-3-yl)phenyl)quinoline-4-carboxylic acid
Homo sapiens
pH 8.0, 22°C
-
0.000185
2-(4-chloroanilino)-3-hydroxynaphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.000541
2-(4-chloroanilino)-3-hydroxynaphthalene-1,4-dione
Homo sapiens
pH 8.2, 25°C
-
0.00033
2-(4-fluoroanilino)-3-hydroxynaphthalene-1,4-dione
Homo sapiens
pH 8.2, 25°C
-
0.001
2-(4-fluoroanilino)-3-hydroxynaphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.0021
2-anilino-3-hydroxynaphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.0026
2-anilino-3-hydroxynaphthalene-1,4-dione
Homo sapiens
pH 8.2, 25°C
-
0.00044
2-cyano-3-(9-ethyl-9H-carbazol-3-ylamino)acrylic acid ethyl ester
Plasmodium falciparum
IC50: 0.00044 mM
0.491
2-cyano-3-(9-ethyl-9H-carbazol-3-ylamino)acrylic acid ethyl ester
Homo sapiens
-
IC50: 0.491 mM
0.000023
2-hydroxy-3-(3-methylbutyl)naphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.000709
2-hydroxy-3-(3-methylbutyl)naphthalene-1,4-dione
Homo sapiens
pH 8.2, 25°C
-
0.000711
2-hydroxy-3-(4-phenylpiperazin-1-yl)naphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.0068
2-hydroxy-3-(4-phenylpiperazin-1-yl)naphthalene-1,4-dione
Homo sapiens
pH 8.2, 25°C
-
0.000108
2-hydroxy-3-[3-(trifluoromethyl)anilino]naphthalene-1,4-dione
Homo sapiens
pH 8.2, 25°C
-
0.000111
2-hydroxy-3-[3-(trifluoromethyl)anilino]naphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.00105
2-[(2,3-dihydro-1,4-benzodioxin-6-yl)amino]-3-hydroxynaphthalene-1,4-dione
Homo sapiens
pH 8.2, 25°C
-
0.0021
2-[(2,3-dihydro-1,4-benzodioxin-6-yl)amino]-3-hydroxynaphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.000013
2-[(2,5-dichlorophenyl)sulfanyl]-5-ethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
Homo sapiens
or above, pH not specified in the publication, temperature not specified in the publication
0.1
2-[(2,5-dichlorophenyl)sulfanyl]-5-ethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
Plasmodium falciparum
-
or above, pH not specified in the publication, temperature not specified in the publication
0.000051
2-[(2,5-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.011
2-[(2,5-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
Plasmodium falciparum
-
pH not specified in the publication, temperature not specified in the publication
0.0036
2-[(2H-1,3-benzodioxol-5-yl)amino]-3-hydroxynaphthalene-1,4-dione
Homo sapiens
pH 8.2, 25°C
-
0.0055
2-[(2H-1,3-benzodioxol-5-yl)amino]-3-hydroxynaphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.0019
2-[(3,4-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
Plasmodium falciparum
-
pH not specified in the publication, temperature not specified in the publication
0.0065
2-[(3,4-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.001
2-[(4-chlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
Plasmodium falciparum
-
pH not specified in the publication, temperature not specified in the publication
0.039
2-[(4-chlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00093
2-[(E)-2-(2-methylphenyl)ethenyl]quinolin-4-ol
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.03
2-[(E)-2-(2-methylphenyl)ethenyl]quinolin-4-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00044
2-[4-(2,3-dichlorophenyl)piperazin-1-yl]-3-hydroxynaphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.0018
2-[4-(2,3-dichlorophenyl)piperazin-1-yl]-3-hydroxynaphthalene-1,4-dione
Homo sapiens
pH 8.2, 25°C
-
0.00028
2-[4-(4-chlorophenyl)piperazin-1-yl]-3-hydroxynaphthalene-1,4-dione
Schistosoma mansoni
pH 8.2, 25°C
-
0.0046
2-[4-(4-chlorophenyl)piperazin-1-yl]-3-hydroxynaphthalene-1,4-dione
Homo sapiens
pH 8.2, 25°C
-
0.0079
3-(3-methylbut-2-en-1-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl 4-methylbenzene-1-sulfonate
Homo sapiens
pH 8.2, 25°C
-
0.0314
3-(3-methylbut-2-en-1-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl 4-methylbenzene-1-sulfonate
Schistosoma mansoni
pH 8.2, 25°C
-
0.00011
4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
Plasmodium berghei
-
pH 8.0
0.00034
4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
Plasmodium falciparum
pH 8.0
0.00034
4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.00051
4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
Plasmodium vivax
-
pH 8.0
0.03
4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00047
5-(1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0007
5-(1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.00046
5-(1H-indol-1-yl)-N-propylthiophene-2-carboxamide
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.00071
5-(1H-indol-1-yl)-N-propylthiophene-2-carboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00017
5-(2-methyl-1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.00063
5-(2-methyl-1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000042
5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
Plasmodium falciparum
pH 8.0
0.000042
5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.00006
5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
Plasmodium berghei
-
pH 8.0
0.00042
5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
Plasmodium vivax
-
pH 8.0
0.03
5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.01
5-(4-methylpiperazin-1-yl)-N-propylthiophene-2-carboxamide
Homo sapiens
-
above, pH not specified in the publication, temperature not specified in the publication
0.03
5-(4-methylpiperazin-1-yl)-N-propylthiophene-2-carboxamide
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.01
5-(piperidin-1-yl)-N-propylthiophene-2-carboxamide
Homo sapiens
-
above, pH not specified in the publication, temperature not specified in the publication
0.03
5-(piperidin-1-yl)-N-propylthiophene-2-carboxamide
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.000047
5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.0013
5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH 8.0, 20°C, mutant F227A
0.0013
5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH 8.0, 20°C, mutant H185A
0.0021
5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH 8.0, 20°C, mutant F188A
0.0021
5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH 8.0, 20°C, mutant R265A
0.2
5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00028
5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.00029
5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0014
5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH 8.0, 20°C, mutant F188A
0.0063
5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH 8.0, 20°C, mutant F227A
0.023
5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH 8.0, 20°C, mutant R265A
0.025
5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH 8.0, 20°C, mutant H185A
0.00043
atovaquone
Schistosoma mansoni
pH 8.2, 25°C
0.00043
atovaquone
Schistosoma mansoni
-
pH 8.2, 25°C
0.0026
atovaquone
Homo sapiens
pH 8.2, 25°C
0.0027
atovaquone
Homo sapiens
pH 8.2, 25°C
0.00001
brequinar
Homo sapiens
pH 8.0, 22°C
0.000037
brequinar
Homo sapiens
pH 8.2, 25°C
0.000037
brequinar
Homo sapiens
-
pH 8.2, 25°C
0.00073
brequinar
Homo sapiens
pH 8.0, 22°C
0.02
brequinar
Schistosoma mansoni
pH 8.2, 25°C
0.02
brequinar
Schistosoma mansoni
-
pH 8.2, 25°C
0.00016
diethyl [(dibenzo[b,d]thiophen-2-ylamino)methylidene]propanedioate
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.03
diethyl [(dibenzo[b,d]thiophen-2-ylamino)methylidene]propanedioate
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00004
ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
Plasmodium vivax
-
pH 8.0
0.00006
ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
Plasmodium berghei
-
pH 8.0
0.000083
ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
Plasmodium falciparum
pH 8.0
0.000083
ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.03
ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000014
Genz-667348
Plasmodium berghei
-
pH 8.0, temperature not specified in the publication
0.000022
Genz-667348
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
0.000042
Genz-667348
Plasmodium vivax
-
pH 8.0, temperature not specified in the publication
0.000012
Genz-668857
Plasmodium berghei
-
pH 8.0, temperature not specified in the publication
0.000015
Genz-668857
Plasmodium vivax
-
pH 8.0, temperature not specified in the publication
0.000044
Genz-668857
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
0.000015
Genz-669178
Plasmodium vivax
-
pH 8.0, temperature not specified in the publication
0.00004
Genz-669178
Plasmodium berghei
-
pH 8.0, temperature not specified in the publication
0.00005
Genz-669178
Plasmodium falciparum
pH 8.0, temperature not specified in the publication
0.0012
isolapachol
Schistosoma mansoni
pH 8.2, 25°C
-
0.01
isolapachol
Homo sapiens
pH 8.2, 25°C
-
0.000019
Lapachol
Schistosoma mansoni
pH 8.2, 25°C
0.0001
Lapachol
Homo sapiens
pH 8.2, 25°C
0.00005
N-(2,4-dichlorophenyl)naphthalene-2-carboxamide
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.05
N-(2,4-dichlorophenyl)naphthalene-2-carboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.049
N-(3,5-dichloro-phenyl)-2-methyl-3-nitro-benzamide
Plasmodium falciparum
wild-type, pH 8.0, 25°C
0.087
N-(3,5-dichloro-phenyl)-2-methyl-3-nitro-benzamide
Plasmodium falciparum
mutant L531A, pH 8.0, 25°C
0.1
N-(3,5-dichloro-phenyl)-2-methyl-3-nitro-benzamide
Plasmodium falciparum
mutant R265A, pH 8.0, 25°C
1.9
N-(3,5-dichloro-phenyl)-2-methyl-3-nitro-benzamide
Plasmodium falciparum
mutant F188A, pH 8.0, 25°C
2.9
N-(3,5-dichloro-phenyl)-2-methyl-3-nitro-benzamide
Plasmodium falciparum
mutant H185A, pH 8.0, 25°C
12
N-(3,5-dichloro-phenyl)-2-methyl-3-nitro-benzamide
Plasmodium falciparum
mutant F227A, pH 8.0, 25°C
0.000016
N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.2
N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00068
N-(3-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0014
N-(3-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.0005
N-(3-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0092
N-(3-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.000056
N-(anthracen-2-yl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.0007
N-(anthracen-2-yl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00021
N-anthracen-2-yl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH 8.0, 20°C, mutant F188A
0.0013
N-anthracen-2-yl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH 8.0, 20°C, mutant H185A
0.0024
N-anthracen-2-yl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH 8.0, 20°C, mutant R265A
0.0044
N-anthracen-2-yl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH 8.0, 20°C, mutant F227A
0.00025
N-cyclopropyl-5-(2,3-dihydro-4H-1,4-benzothiazin-4-yl)thiophene-2-carboxamide
Plasmodium falciparum
pH 8.0
0.00028
N-cyclopropyl-5-(2,3-dihydro-4H-1,4-benzothiazin-4-yl)thiophene-2-carboxamide
Plasmodium vivax
-
pH 8.0
0.00038
N-cyclopropyl-5-(2,3-dihydro-4H-1,4-benzothiazin-4-yl)thiophene-2-carboxamide
Plasmodium berghei
-
pH 8.0
0.01
N-propyl-5-(1H-pyrazol-1-yl)thiophene-2-carboxamide
Homo sapiens
-
above, pH not specified in the publication, temperature not specified in the publication
0.03
N-propyl-5-(1H-pyrazol-1-yl)thiophene-2-carboxamide
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.000077
N-[3-fluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.00021
N-[3-fluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000163
teriflunomide
Homo sapiens
Q02172
at pH 8.0 and 22°C
0.000312
teriflunomide
Homo sapiens
pH 8.2, 25°C
0.00032
teriflunomide
Homo sapiens
pH 8.2, 25°C
0.05
teriflunomide
Schistosoma mansoni
pH 8.2, 25°C
0.05
teriflunomide
Schistosoma mansoni
-
pH 8.2, 25°C
additional information
A77 1726
Mus musculus
-
IC50 value 150 ng per ml
additional information
A77 1726
Homo sapiens
-
IC50 value 440 ng per ml
additional information
[2-fluoro-2',5'-dimethyl-4'-[6-(3-methyl-2-butenyloxy)pyridin-3-yl]biphenyl-4-yl]-(3-methyl-2-butenyl)amine
Homo sapiens
-
IC50 value 23 ng per ml
additional information
[2-fluoro-2',5'-dimethyl-4'-[6-(3-methyl-2-butenyloxy)pyridin-3-yl]biphenyl-4-yl]-(3-methyl-2-butenyl)amine
Mus musculus
-
IC50 value 32 ng per ml
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Rowland, P.; Norager, S.; Jensen, K.F.; Larsen, S.
Crystallization and preliminary x-ray studies of membrane-associated Escherichia coli dihydroorotate dehydrogenase
Acta Crystallogr. Sect. D
56
659-661
2000
Escherichia coli
brenda
Bjoernberg, O.; Gruener, A.C.; Roepstorff, P.; Jensen, K.F.
The activity of Escherichia coli dihydroorotate dehydrogenase is dependent on a conserved loop identified by sequence homology, mutagenesis, and limited proteolysis
Biochemistry
38
2899-2908
1999
Escherichia coli, Lactococcus lactis
brenda
Palfey, B.A.; Bjoernberg, O.; Jensen, K.F.
Insight into the chemistry of flavin reduction and oxidation in Escherichia coli dihydroorotate dehydrogenase obtained by rapid reaction studies
Biochemistry
40
4381-4390
2001
Escherichia coli
brenda
Liu, S.; Neidhardt, E.A.; Grossman, T.H.; Ocain, T.; Clardy, J.
Structures of human dihydroorotate dehydrogenase in complex with antiproliferative agents
Structure
8
25-33
2000
Homo sapiens
brenda
Davis, J.P.; Copeland, R.A.
Histidine to alanine mutants of human dihydroorotate dehydrogenase. Identification of a brequinar-resistant mutant enzyme
Biochem. Pharmacol.
54
459-465
1997
Homo sapiens
brenda
Copeland, R.A.; Davis, J.P.; Dowling, R.L.; Lombardo, D.; Murphy, K.B.; Patterson, T.A.
Recombinant human dihydroorotate dehydrogenase: expression, purification, and characterization of a catalytically functional truncated enzyme
Arch. Biochem. Biophys.
323
79-86
1995
Homo sapiens
brenda
Bruneau, J.M.; Yea, C.M.; Spinella-Jaegle, S.; Fudali, C.; Woodward, K.; Robson, P.A.; Sautes, C.; Westwood, R.; Kuo, E.A.; Williamson, R.A.; Ruuth, E.
Purification of human dihydro-orotate dehydrogenase and its inhibition by A77 1726, the active metabolite of leflunomide
Biochem. J.
336
299-303
1998
Homo sapiens
-
brenda
Ullrich, A.; Knecht, W.; Fries, M.; Loffler, M.
Recombinant expression of N-terminal truncated mutants of the membrane bound mouse, rat and human flavoenzyme dihydroorotate dehydrogenase. A versatile tool to rate inhibitor effects?
Eur. J. Biochem.
268
1861-1868
2001
Homo sapiens, Mus musculus, Rattus norvegicus
brenda
Loeffler, M.; Becker, C.; Wegerle, E.; Schuster, G.
Catalytic enzyme histochemistry and biochemical analysis of dihydroorotate dehydrogenase/oxidase and succinate dehydrogenase in mammalian tissues, cells and mitochondria
Histochem. Cell Biol.
105
119-128
1996
Bos taurus, Cavia porcellus, Homo sapiens, Mus musculus, Sus scrofa, Rattus norvegicus (Q63707)
brenda
Bader, B.; Knecht, W.; Fries, M.; Loffler, M.
Expression, purification, and characterization of histidine-tagged rat and human flavoenzyme dihydroorotate dehydrogenase
Protein Expr. Purif.
13
414-422
1998
Homo sapiens, Rattus norvegicus
brenda
Krungkrai, J.
Purification, characterization and localization of mitochondrial dihydroorotate dehydrogenase in Plasmodium falciparum, human malaria parasite
Biochim. Biophys. Acta
1243
351-360
1995
Plasmodium falciparum
brenda
Marcinkeviciene, J.; Jiang, W.; Locke, G.; Kopcho, L.M.; Rogers, M.J.; Copeland, R.A.
A second dihydroorotate dehydrogenase (Type A) of the human pathogen Enterococcus faecalis: expression, purification, and steady-state kinetic mechanism
Arch. Biochem. Biophys.
377
178-186
2000
Enterococcus faecalis
brenda
Forman, H.J.; Kennedy, J.
Mammalian dihydroorotate dehydrogenase: physical and catalytic properties of the primary enzyme
Arch. Biochem. Biophys.
191
23-31
1978
Rattus norvegicus
brenda
Miller, R.W.
Dihydroorotate dehydrogenase (Neurospora)
Methods Enzymol.
51
63-69
1978
Neurospora crassa
brenda
Hines, V.; Keys, L.D.; Johnston, M.
Purification and properties of the bovine liver mitochondrial dihydroorotate dehydrogenase [published erratum appears in J Biol Chem 1987 Nov 5;262(31):15322]
J. Biol. Chem.
261
11386-11392
1986
Bos taurus
brenda
Hines, V.; Johnston, M.
Analysis of the kinetic mechanism of the bovine liver mitochondrial dihydroorotate dehydrogenase
Biochemistry
28
1222-1226
1989
Bos taurus
brenda
Karibian, D.
Dihydroorotate dehydrogenase (Escherichia coli)
Methods Enzymol.
51
58-63
1978
Escherichia coli
brenda
Miersch, J.; Krauss, G.J.; Metzger, U.
Properties and subcellular localization of dihydroorotate dehydrogenase in cells of tomato suspension culture
J. Plant Physiol.
122
55-66
1986
Solanum lycopersicum
-
brenda
Knecht, W.; Bergjohann, U.; Gonski, S.; Kirschbaum, B.; Loffler, M.
Functional expression of a fragment of human dihydroorotate dehydrogenase by means of the baculovirus expression vector system, and kinetic investigation of the purified recombinant enzyme
Eur. J. Biochem.
240
292-301
1996
Homo sapiens
brenda
Knecht, w.; Altekruse, D.; Rotgeri, A.; Gonski, S.; Loffler, M.
Rat dihydroorotate dehydrogenase: isolation of the recombinant enzyme from mitochondria of insect cells
Protein Expr. Purif.
10
89-99
1997
Rattus norvegicus (Q63707)
brenda
Davis, J.P.; Cain, G.A.; Pitts, W.J.; Magolda, R.L.; Copeland, R.A.
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase
Biochemistry
35
1270-1273
1996
Homo sapiens
brenda
Knecht, W.; Henseling, J.; Loffler, M.
Kinetics of inhibition of human and rat dihydroorotate dehydrogenase by atovaquone, lawsone derivatives, brequinar sodium and polyporic acid
Chem. Biol. Interact.
124
61-76
2000
Homo sapiens, Rattus norvegicus
brenda
McLean, J.E.; Neidhardt, E.A.; Grossman, T.H.; Hedstrom, L.
Multiple inhibitor analysis of the brequinar and leflunomide binding sites on human dihydroorotate dehydrogenase
Biochemistry
40
2194-2200
2001
Homo sapiens
brenda
Leban, J.; Saeb, W.; Garcia, G.; Baumgartner, R.; Kramer, B.
Discovery of a novel series of DHODH inhibitors by a docking procedure and QSAR refinement
Bioorg. Med. Chem. Lett.
14
55-58
2004
Homo sapiens
brenda
Ullrich, A.; Knecht, W.; Piskur, J.; Loffler, M.
Plant dihydroorotate dehydrogenase differs significantly in substrate specificity and inhibition from the animal enzymes
FEBS Lett.
529
346-350
2002
Arabidopsis thaliana (P32746), Arabidopsis thaliana
brenda
Loffler, M.; Knecht, W.; Rawls, J.; Ullrich, A.; Dietz, C.
Drosophila melanogaster dihydroorotate dehydrogenase: the N-terminus is important for biological function in vivo but not for catalytic properties in vitro
Insect Biochem. Mol. Biol.
32
1159-1169
2002
Drosophila melanogaster
brenda
Shi, J.; Palfey, B.A.; Dertouzos, J.; Jensen, K.F.; Gafni, A.; Steel, D.
Multiple states of the Tyr318Leu mutant of dihydroorotate dehydrogenase revealed by single-molecule kinetics
J. Am. Chem. Soc.
126
6914-6922
2004
Escherichia coli
brenda
Baldwin, J.; Farajallah, A.M.; Malmquist, N.A.; Rathod, P.K.; Phillips, M.A.
Malarial dihydroorotate dehydrogenase. Substrate and inhibitor specificity
J. Biol. Chem.
277
41827-41834
2002
Homo sapiens, Plasmodium falciparum (Q08210), Plasmodium falciparum
brenda
Baldwin, J.; Michnoff, C.H.; Malmquist, N.A.; White, J.; Roth, M.G.; Rathod, P.K.; Phillips, M.A.
High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase
J. Biol. Chem.
280
21847-21853
2005
Plasmodium falciparum
brenda
Takashima, E.; Inaoka, D.K.; Osanai, A.; Nara, T.; Odaka, M.; Aoki, T.; Inaka, K.; Harada, S.; Kita, K.
Characterization of the dihydroorotate dehydrogenase as a soluble fumarate reductase in Trypanosoma cruzi
Mol. Biochem. Parasitol.
122
189-200
2002
Trypanosoma cruzi
brenda
Hansen, M.; Le Nours, J.; Johansson, E.; Antal, T.; Ullrich, A.; Loffler, M.; Larsen, S.
Inhibitor binding in a class 2 dihydroorotate dehydrogenase causes variations in the membrane-associated N-terminal domain
Protein Sci.
13
1031-1042
2004
Rattus norvegicus
brenda
Fagan, R.L.; Nelson, M.N.; Pagano, P.M.; Palfey, B.A.
Mechanism of flavin reduction in class 2 dihydroorotate dehydrogenases
Biochemistry
45
14926-14932
2006
Escherichia coli, Homo sapiens
brenda
Zameitat, E.; Gojkovic, Z.; Knecht, W.; Piskur, J.; Loeffler, M.
Biochemical characterization of recombinant dihydroorotate dehydrogenase from the opportunistic pathogenic yeast Candida albicans
FEBS J.
273
3183-3191
2006
Candida albicans (Q874I4), Candida albicans
brenda
Baumgartner, R.; Walloschek, M.; Kralik, M.; Gotschlich, A.; Tasler, S.; Mies, J.; Leban, J.
Dual binding mode of a novel series of DHODH inhibitors
J. Med. Chem.
49
1239-1247
2006
Homo sapiens (Q02127), Homo sapiens
brenda
Heikkil, T.; Ramsey, C.; Davies, M.; Galtier, C.; Stead, A.M.W.; Johnson, A.P.; Fishwick, C.W.G.; Boa, A.N.; McConkey, G.A.
Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase
J. Med. Chem.
50
186-191
2007
Homo sapiens, Plasmodium falciparum (Q08210), Plasmodium falciparum
brenda
Small, Y.A.; Guallar, V.; Soudackov, A.V.; Hammes-Schiffer, S.
Hydrogen bonding pathways in human dihydroorotate dehydrogenase
J. Phys. Chem. B
110
19704-19710
2006
Homo sapiens (Q02127), Homo sapiens
brenda
Zameitat, E.; Freymark, G.; Dietz, C.D.; Loeffler, M.; Boelker, M.
Functional expression of human dihydroorotate dehydrogenase (DHODH) in pyr4 mutants of Ustilago maydis allows target validation of DHODH inhibitors in vivo
Appl. Environ. Microbiol.
73
3371-3379
2007
Homo sapiens (Q02127), Homo sapiens
brenda
Malmquist, N.A.; Gujjar, R.; Rathod, P.K.; Phillips, M.A.
Analysis of flavin oxidation and electron-transfer inhibition in Plasmodium falciparum dihydroorotate dehydrogenase
Biochemistry
47
2466-2475
2008
Plasmodium falciparum (Q08210), Plasmodium falciparum
brenda
Walse, B.; Dufe, V.; Svensson, B.; Fritzson, I.; Dahlberg, L.; Khairoullina, A.; Wellmar, U.; Al-Karadaghi, S.
The structures of human dihydroorotate dehydrogenase with and without inhibitor reveal conformational flexibility in the inhibitor and substrate binding sites
Biochemistry
47
8929-8936
2008
Homo sapiens (Q02127), Homo sapiens
brenda
Fagan, R.L.; Palfey, B.A.
Roles in binding and chemistry for conserved active site residues in the class 2 dihydroorotate dehydrogenase from Escherichia coli
Biochemistry
48
7169-7178
2009
Escherichia coli (P0A7E1), Escherichia coli
brenda
Kow, R.L.; Whicher, J.R.; McDonald, C.A.; Palfey, B.A.; Fagan, R.L.
Disruption of the proton relay network in the class 2 dihydroorotate dehydrogenase from Escherichia coli
Biochemistry
48
9801-9809
2009
Escherichia coli
brenda
Deguchi, M.; Kishino, J.; Hattori, M.; Furue, Y.; Yamamoto, M.; Mochizuki, I.; Iguchi, M.; Hirano, Y.; Hojou, K.; Nagira, M.; Nishitani, Y.; Okazaki, K.; Yasui, K.; Arimura, A.
Suppression of immunoglobulin production by a novel dihydroorotate dehydrogenase inhibitor, S-2678
Eur. J. Pharmacol.
601
163-170
2008
Homo sapiens, Mus musculus
brenda
Patel, V.; Booker, M.; Kramer, M.; Ross, L.; Celatka, C.; Kennedy, L.; Dvorin, J.; Duraisingh, M.; Sliz, P.; Wirth, D.; Clardy, J.
Identification and characterization of small molecule inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase
J. Biol. Chem.
283
35078-35085
2008
Plasmodium berghei, Plasmodium vivax, Plasmodium falciparum (Q08210), Plasmodium falciparum
brenda
Deng, X.; Gujjar, R.; El Mazouni, F.; Kaminsky, W.; Malmquist, N.A.; Goldsmith, E.J.; Rathod, P.K.; Phillips, M.A.
Structural plasticity of malaria dihydroorotate dehydrogenase allows selective binding of diverse chemical scaffolds
J. Biol. Chem.
284
26999-27009
2009
Plasmodium falciparum (Q08210), Plasmodium falciparum
brenda
Davies, M.; Heikkila, T.; McConkey, G.; Fishwick, C.; Parsons, M.; Johnson, A.
Structure-based design, synthesis, and characterization of inhibitors of human and Plasmodium falciparum dihydroorotate dehydrogenases
J. Med. Chem.
52
2683-2693
2009
Homo sapiens (Q02127), Homo sapiens, Plasmodium falciparum (Q08210), Plasmodium falciparum
brenda
Baumann, P.; Mandl-Weber, S.; Völkl, A.; Adam, C.; Bumeder, I.; Oduncu, F.; Schmidmaier, R.
Dihydroorotate dehydrogenase inhibitor A771726 (leflunomide) induces apoptosis and diminishes proliferation of multiple myeloma cells
Mol. Cancer Ther.
8
366-375
2009
Homo sapiens
brenda
Ojha, P.K.; Roy, K.
Chemometric modeling, docking and in silico design of triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors as antimalarials
Eur. J. Med. Chem.
45
4645-4656
2010
Plasmodium falciparum (Q08210)
brenda
Hail, N.; Chen, P.; Kepa, J.J.; Bushman, L.R.; Shearn, C.
Dihydroorotate dehydrogenase is required for N-(4-hydroxyphenyl)retinamide-induced reactive oxygen species production and apoptosis
Free Radic. Biol. Med.
49
109-116
2010
Homo sapiens
brenda
Phillips, M.A.; Rathod, P.K.
Plasmodium dihydroorotate dehydrogenase: a promising target for novel anti-malarial chemotherapy
Infect. Disord. Drug Targets
10
226-239
2010
Homo sapiens, Plasmodium falciparum (Q08210), Plasmodium falciparum
brenda
Booker, M.L.; Bastos, C.M.; Kramer, M.L.; Barker, R.H.; Skerlj, R.; Sidhu, A.B.; Deng, X.; Celatka, C.; Cortese, J.F.; Guerrero Bravo, J.E.; Crespo Llado, K.N.; Serrano, A.E.; Angulo-Barturen, I.; Jimenez-Diaz, M.B.; Viera, S.; Garuti, H.; Wittlin, S.; Papastogiannidis, P.; Lin, J.W.; Janse, C.J.; Khan, S.M.
Novel inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with anti-malarial activity in the mouse model
J. Biol. Chem.
285
33054-33064
2010
Plasmodium berghei, Plasmodium vivax, Plasmodium falciparum (Q08210), Plasmodium falciparum
brenda
Gujjar, R.; Marwaha, A.; El Mazouni, F.; White, J.; White, K.L.; Creason, S.; Shackleford, D.M.; Baldwin, J.; Charman, W.N.; Buckner, F.S.; Charman, S.; Rathod, P.K.; Phillips, M.A.
Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice
J. Med. Chem.
52
1864-1872
2009
Plasmodium falciparum
brenda
Schaefer, C.h.M.; Schaefer, M.K.; Loefflerr, M.
Region-specific distribution of dihydroorotate dehydrogenase in the rat central nervous system points to pyrimidine de novo synthesis in neurons
Nucleosides Nucleotides Nucleic Acids
29
476-481
2010
Rattus norvegicus
brenda
Couto, S.G.; Cristina Nonato, M.; Costa-Filho, A.J.
Site directed spin labeling studies of Escherichia coli dihydroorotate dehydrogenase N-terminal extension
Biochem. Biophys. Res. Commun.
414
487-492
2011
Escherichia coli (B1X8P9), Escherichia coli
brenda
Bedingfield, P.T.; Cowen, D.; Acklam, P.; Cunningham, F.; Parsons, M.R.; McConkey, G.A.; Fishwick, C.W.; Johnson, A.P.
Factors influencing the specificity of inhibitor binding to the human and malaria parasite dihydroorotate dehydrogenases
J. Med. Chem.
55
5841-5850
2012
Plasmodium falciparum, Homo sapiens (Q02127), Homo sapiens
brenda
Hortua Triana, M.A.; Huynh, M.H.; Garavito, M.F.; Fox, B.A.; Bzik, D.J.; Carruthers, V.B.; Loeffler, M.; Zimmermann, B.H.
Biochemical and molecular characterization of the pyrimidine biosynthetic enzyme dihydroorotate dehydrogenase from Toxoplasma gondii
Mol. Biochem. Parasitol.
184
71-81
2012
Toxoplasma gondii
brenda
Hegewald, J.; Gross, U.; Bohne, W.
Identification of dihydroorotate dehydrogenase as a relevant drug target for 1-hydroxyquinolones in Toxoplasma gondii
Mol. Biochem. Parasitol.
190
6-15
2013
Toxoplasma gondii
brenda
Hey-Mogensen, M.; Goncalves, R.L.; Orr, A.L.; Brand, M.D.
Production of superoxide/H2O2 by dihydroorotate dehydrogenase in rat skeletal muscle mitochondria
Free Radic. Biol. Med.
72
149-155
2014
Rattus norvegicus
brenda
Zhu, J.; Han, L.; Diao, Y.; Ren, X.; Xu, M.; Xu, L.; Li, S.; Li, Q.; Dong, D.; Huang, J.; Liu, X.; Zhao, Z.; Wang, R.; Zhu, L.; Xu, Y.; Qian, X.; Li, H.
Design, synthesis, X-ray crystallographic analysis, and biological evaluation of thiazole derivatives as potent and selective inhibitors of human dihydroorotate dehydrogenase
J. Med. Chem.
58
1123-1139
2015
Homo sapiens (Q02172), Homo sapiens
brenda
Munier-Lehmann, H.; Lucas-Hourani, M.; Guillou, S.; Helynck, O.; Zanghi, G.; Noel, A.; Tangy, F.; Vidalain, P.O.; Janin, Y.L.
Original 2-(3-alkoxy-1H-pyrazol-1-yl)pyrimidine derivatives as inhibitors of human dihydroorotate dehydrogenase (DHODH)
J. Med. Chem.
58
860-877
2015
Homo sapiens (Q02172), Homo sapiens
brenda
Stocks, P.A.; Barton, V.; Antoine, T.; Biagini, G.A.; Ward, S.A.; ONeill, P.M.
Novel inhibitors of the Plasmodium falciparum electron transport chain
Parasitology
141
50-65
2014
Plasmodium falciparum
brenda
Nonato, M.C.; de Padua, R.A.P.; David, J.S.; Reis, R.A.G.; Tomaleri, G.P.; DMuniz Pereira, H.; Calil, F.A.
Structural basis for the design of selective inhibitors for Schistosoma mansoni dihydroorotate dehydrogenase
Biochimie
158
180-190
2019
Schistosoma mansoni (G4VFD7), Schistosoma mansoni, Homo sapiens (Q02127), Homo sapiens
brenda
Petrovic, M.; Roschger, C.; Chaudary, S.; Zierer, A.; Mladenovic, M.; Jakovljevic, K.; Markovic, V.; Botta, B.; Joksovic, M.
Potent human dihydroorotate dehydrogenase inhibitory activity of new quinoline-4-carboxylic acids derived from phenolic aldehydes synthesis, cytotoxicity, lipophilicity and molecular docking studies
Bioorg. Chem.
105
104373
2020
Homo sapiens (Q02127), Homo sapiens
brenda
Calil, F.A.; David, J.S.; Chiappetta, E.R.C.; Fumagalli, F.; Mello, R.B.; Leite, F.H.A.; Castilho, M.S.; Emery, F.S.; Nonato, M.C.
Ligand-based design, synthesis and biochemical evaluation of potent and selective inhibitors of Schistosoma mansoni dihydroorotate dehydrogenase
Eur. J. Med. Chem.
167
357-366
2019
Schistosoma mansoni (G4VFD7), Schistosoma mansoni, Homo sapiens (Q02127), Homo sapiens
brenda
Garavito, M.F.; Narvaez-Ortiz, H.Y.; Pulido, D.C.; Loeffler, M.; Judelson, H.S.; Restrepo, S.; Zimmermann, B.H.
Phytophthora infestans dihydroorotate dehydrogenase is a potential target for chemical control - a comparison with the enzyme from Solanum tuberosum
Front. Microbiol.
10
1479
2019
Phytophthora infestans (I7EMP0), Phytophthora infestans, Solanum tuberosum (M1BCR0), Solanum tuberosum
brenda
Matsubayashi, M.; Inaoka, D.; Komatsuya, K.; Hatta, T.; Kawahara, F.; Sakamoto, K.; Hikosaka, K.; Yamagishi, J.; Sasai, K.; Shiba, T.; Harada, S.; Tsuji, N.; Kita, K.
Novel characteristics of mitochondrial electron transport chain from Eimeria tenella
Genes (Basel)
10
29
2019
Eimeria tenella (U6KL66), Eimeria tenella
brenda
Hartuti, E.D.; Sakura, T.; Tagod, M.S.O.; Yoshida, E.; Wang, X.; Mochizuki, K.; Acharjee, R.; Matsuo, Y.; Tokumasu, F.; Mori, M.; Waluyo, D.; Shiomi, K.; Nozaki, T.; Hamano, S.; Shiba, T.; Kita, K.; Inaoka, D.K.
Identification of 3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine derivatives as novel selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase
Int. J. Mol. Sci.
22
7236
2021
Plasmodium falciparum (Q08210), Plasmodium falciparum
brenda
Madak, J.; Cuthbertson, C.; Miyata, Y.; Tamura, S.; Petrunak, E.; Stuckey, J.; Han, Y.; He, M.; Sun, D.; Showalter, H.; Neamati, N.
Design, synthesis, and biological evaluation of 4-quinoline carboxylic acids as inhibitors of dihydroorotate dehydrogenase
J. Med. Chem.
61
5162-5186
2018
Homo sapiens (Q02127)
brenda
Rodriguez, J.M.O.; Krupinska, E.; Wacklin-Knecht, H.; Knecht, W.
Preparation of human dihydroorotate dehydrogenase for interaction studies with lipid bilayers
Nucleosides Nucleotides Nucleic Acids
39
1306-1319
2020
Homo sapiens (Q02127), Homo sapiens
brenda