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0.000082
(-)-epicatechin gallate
-
25°C, pH 7.6
0.00012
(-)-epigallocatechin gallate
-
25°C, pH 7.6
0.0000027
(2E)-1-(1-cyclohexylphthalazin-2(1H)-yl)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]prop-2-en-1-one
pH and temperature not specified in the publication
0.000005
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-(1-phenoxyphthalazin-2(1H)-yl)prop-2-en-1-one
pH and temperature not specified in the publication
0.0000026
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-(1-phenylphthalazin-2(1H)-yl)prop-2-en-1-one
pH and temperature not specified in the publication
0.0000045
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-(1-propylphthalazin-2(1H)-yl)prop-2-en-1-one
pH and temperature not specified in the publication
0.0000072
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-[1-(2-methylphenyl)phthalazin-2(1H)-yl]prop-2-en-1-one
pH and temperature not specified in the publication
0.0000038
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-[1-(3,3,3-trifluoropropyl)phthalazin-2(1H)-yl]prop-2-en-1-one
pH and temperature not specified in the publication
0.0000071
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-[1-(3,5-dimethylphenyl)phthalazin-2(1H)-yl]prop-2-en-1-one
pH and temperature not specified in the publication
0.0000048
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-[1-(3-fluorophenyl)phthalazin-2(1H)-yl]prop-2-en-1-one
pH and temperature not specified in the publication
0.0000038
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-[1-(3-methylbut-2-en-1-yl)phthalazin-2(1H)-yl]prop-2-en-1-one
pH and temperature not specified in the publication
0.0000035
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-[1-(3-methylbutyl)phthalazin-2(1H)-yl]prop-2-en-1-one
pH and temperature not specified in the publication
0.0000056
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-[1-(4-fluorophenyl)phthalazin-2(1H)-yl]prop-2-en-1-one
pH and temperature not specified in the publication
0.0000067
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-[1-(4-methoxyphenoxy)phthalazin-2(1H)-yl]prop-2-en-1-one
pH and temperature not specified in the publication
0.0000062
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-[1-(4-methylphenoxy)phthalazin-2(1H)-yl]prop-2-en-1-one
pH and temperature not specified in the publication
0.0000051
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-[1-(4-methylphenyl)phthalazin-2(1H)-yl]prop-2-en-1-one
pH and temperature not specified in the publication
0.0000074
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-[1-(hexan-3-yl)phthalazin-2(1H)-yl]prop-2-en-1-one
pH and temperature not specified in the publication
0.0000038
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-[1-(propan-2-yl)phthalazin-2(1H)-yl]prop-2-en-1-one
pH and temperature not specified in the publication
0.0000188
(2E)-3-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]-1-[1-[4-(trifluoromethoxy)phenoxy]phthalazin-2(1H)-yl]prop-2-en-1-one
pH and temperature not specified in the publication
0.0000007
(E)-1-(1-cyclopropyl-6,7-dimethoxyphthalazin-2(1H)-yl)-3-(5-((2,4-diaminopyrimidin-5-yl)methyl)-2,3-dimethoxyphenyl)prop-2-en-1-one
30°C, pH not specified in the publication
-
0.0000012
(E)-3-(5-((2,4-diaminopyrimidin-5-yl)methyl)-2,3-dimethoxyphenyl)-1-(1-(4-methoxyphenyl)phthalazin-2(1H)-yl)prop-2-en-1-one, (E)-3-(5-((2,4-diaminopyrimidin-5-yl)methyl)-2,3-dimethoxyphenyl)-1-(1-phenylphthalazin-2(1H)-yl)prop-2-en-1-one
30°C, pH not specified in the publication
-
0.0000012
(E)-3-(5-((2,4-diaminopyrimidin-5-yl)methyl)-2,3-dimethoxyphenyl)-1-(1-phenylphthalazin-2(1H)-yl)prop-2-en-1-one
-
30°C, pH not specified in the publication
-
0.0000012
(E)-3-(5-((2,4-diaminopyrimidin-5-yl)methyl)-2,3-dimethoxyphenyl)-1-(1-propylphthalazin-2(1H)-yl)prop-2-en-1-one
30°C, pH not specified in the publication
-
0.0000011
(E)-3-(5-((2,4-diaminopyrimidin-5-yl)methyl)-2,3-dimethoxyphenyl)-1-(6,7-dimethoxy-1-propylphthalazin-2(1H)-yl)prop-2-en-1-one
30°C, pH not specified in the publication
-
0.0000012
(E)-3-(5-((2,4-diaminopyrimidin-5-yl)methyl)-2,3-dimethoxyphenyl)-1-(6,7-dimethyl-1-propylphthalazin-2(1H)-yl)prop-2-en-1-one
30°C, pH not specified in the publication
-
0.000062 - 0.0005
(E)-5-[2-(2-methoxyphenyl)prop-1-en-1-yl]furo[2,3-d]pyrimidine-2,4-diamine
0.00016 - 0.0016
(Z)-5-[2-(2-methoxyphenyl)prop-1-en-1-yl]furo[2,3-d]pyrimidine-2,4-diamine
0.0000115
1,4-phenylenebis(methylene) bis(N-[amino(imino)methyl](imidothiocarbamate))
25°C, pH 7.5
0.01116
1-(3-ethoxyphenyl)-6,6-dimethyl-1,6-dihydro-1,3,5-triazine-2,4-diamine
pH 7.3, 22°C
0.00102
1-(4-chlorophenyl)-6,6-dimethyl-1,6-dihydro-1,3,5-triazine-2,4-diamine
pH 7.3, 22°C
0.00402
1-(4-ethoxyphenyl)-6,6-dimethyl-1,6-dihydro-1,3,5-triazine-2,4-diamine
pH 7.3, 22°C
0.02022
1-[3-(aminomethyl)phenyl]-6,6-dimethyl-1,6-dihydro-1,3,5-triazine-2,4-diamine
pH 7.3, 22°C
0.0008802
1-[3-chloro-4-(5-phenylpentyl)phenyl]-6,6-dimethyl-1,6-dihydro-1,3,5-triazine-2,4-diamine
pH 7.3, 22°C
0.0393
1-[4-(aminomethyl)phenyl]-6,6-dimethyl-1,6-dihydro-1,3,5-triazine-2,4-diamine
pH 7.3, 22°C
0.0000037
2,4-diamino-5,6-dihydro-6,6-dimethyl-5-(4'-methoxyphenyl)-s-triazine
-
-
0.000097 - 0.00049
2,4-diamino-5-[3-(2-methoxy-5-phenylphenyl)prop-1-ynyl]-6-ethylpyrimidine
0.00043 - 0.00259
2,4-diamino-5-[3-(2-phenyl-5-methoxyphenyl)prop-1-ynyl]-6-ethylpyrimidine
0.00000026 - 0.0000244
2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine
0.065
2,4-diaminopyrimidine
-
pH 6.0, 25°C recombinant His-tagged enzyme
0.459
2,4-diaminoquinazoline
-
pH 6.0, 25°C recombinant His-tagged enzyme
0.00039 - 0.00489
3-(2,4-diamino-6-methylpyrimidin-5-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-yn-1-ol
0.00000003
3-(2-(3-[(2,4-diamino-6-ethylpyrimidin-5-yl)oxy]propoxy)phenyl)propanoic acid
pH 6, temperature not specified in the publication, isolate PKNY146CSP
-
0.000958
3-(4,6-diamino-2,2-dimethyl-1,3,5-triazin-1(2H)-yl)benzonitrile
pH 7.3, 22°C
0.0021
3-O-(3,4,5-trimethoxybenzoyl)-(-)-epicatechin
-
pH 7.4, 25°C
0.0000094
4-((5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl)ethynyl)benzoic acid
pH 7.0
0.0000036 - 0.000049
4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoic acid
0.00000078
4-(N-[(2,4-Diamino-6-pteridyl)methyl]-N-methylamino)benzoate
-
-
0.0000014 - 0.000034
4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]phenol
0.00289
4-[3-(4,6-diamino-2,2-dimethyl-1,3,5-triazin-1(2H)-yl)benzamido]benzene-1-sulfonyl fluoride
pH 7.3, 22°C
0.105
4-[4,6-diamino-2-(4-chlorophenyl)-1,3,5-triazin-1(2H)-yl]benzene-1-sulfonamide
pH 7.3, 22°C
0.0000497
4-[4-[3-(4,6-diamino-2,2-dimethyl-1,3,5-triazin-1-yl)phenyl]butyl]benzenesulfonyl fluoride
pH 7.3, 22°C
0.0000926
4-[6-[4-(4,6-diamino-2,2-dimethyl-1,3,5-triazin-1-yl)phenyl]hexyl]benzenesulfonyl fluoride
pH 7.3, 22°C
0.0000003 - 0.0000534
5-(3,4-dichlorophenyl)-6-ethylpyrimidine-2,4-diamine
0.0000008 - 0.0000033
5-(3-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
0.0000003 - 0.000303
5-(4-bromophenyl)-6-ethylpyrimidine-2,4-diamine
0.0000043 - 0.001576
5-(4-chlorophenyl)-6-(4-methoxyphenyl)pyrimidine-2,4-diamine
0.0000003 - 0.000385
5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
0.0000003 - 0.000798
5-(4-chlorophenyl)-6-isobutylpyrimidine-2,4-diamine
0.0000003 - 0.000541
5-(4-chlorophenyl)-6-isopropylpyrimidine-2,4-diamine
0.0000029 - 0.003461
5-(4-chlorophenyl)-6-phenylpyrimidine-2,4-diamine
0.0000005 - 0.000359
5-(4-chlorophenyl)-6-propylpyrimidine-2,4-diamine
0.000024 - 0.000188
5-(5-[[(2,4-diamino-6-quinazolinyl)methyl](propyl)amino]-2-methoxyphenoxy) pentanoate
0.15
5-methyltetrahydrofolate
-
-
0.00006 - 0.00077
5-[(R/S)-2-(2'-methoxyphenyl)-3-methylbutyl]furo[2,3-d]-pyrimidine-2,4-diamine
0.00078 - 0.0046
5-[(R/S)-2-(2'-methoxyphenyl)-3-methylpentyl]furo[2,3-d]pyrimidine-2,4-diamine
0.00062 - 0.0053
5-[(R/S)-2-(2'-methoxyphenyl)-4-methylpentyl]furo[2,3-d]pyrimidine-2,4-diamine
0.0033 - 0.012
5-[(R/S)-2-(2'-methoxyphenyl)hexyl]furo[2,3-d]pyrimidine-2,4-diamine
0.0025 - 0.0028
5-[(R/S)-2-(2'-methoxyphenyl)pentyl]furo[2,3-d]pyrimidine-2,4-diamine
0.00006 - 0.00065
5-[(R/S)-2-cyclopropyl-2-(2'-methoxyphenyl)ethyl]furo-[2,3-d]pyrimidine-2,4-diamine
0.00007 - 0.00083
5-[(Z/E)-2-(2'-methoxyphenyl)-3-methylbut-1-en-1-yl]-furo[2,3-d]pyrimidine-2,4-diamine
0.00007 - 0.0011
5-[(Z/E)-2-(2'-methoxyphenyl)-3-methylpent-1-en-1-yl]-furo[2,3-d]pyrimidine-2,4-diamine
0.00091 - 0.011
5-[(Z/E)-2-(2'-methoxyphenyl)-4-methylpent-1-en-1-yl]-furo[2,3-d]pyrimidine-2,4-diamine
0.00055 - 0.0043
5-[(Z/E)-2-(2'-methoxyphenyl)hex-1-en-1-yl]furo[2,3-d]-pyrimidine-2,4-diamine
0.00014 - 0.0016
5-[(Z/E)-2-(2'-methoxyphenyl)pent-1-en-1-yl]furo[2,3-d]-pyrimidine-2,4-diamine
0.00008 - 0.0013
5-[(Z/E)-2-cyclopropyl-2-(2'-methoxyphenyl)vinyl]furo-[2,3-d]pyrimidine-2,4-diamine
0.00183 - 0.00752
5-[3-(2,5-dimethoxybiphenyl-4-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
0.0003 - 0.0205
5-[3-(2,5-dimethoxyphenyl)prop-1-yn-1-yl]-6-ethylpyrimidine-2,4-diamine
0.0002 - 0.00451
5-[3-(2,5-dimethoxyphenyl)prop-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
0.0016 - 0.0092
5-[3-(2-methoxybiphenyl-4-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
0.00164 - 0.0117
5-[3-(3-methoxybiphenyl-4-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
0.00103 - 0.00266
5-[3-(5-methoxybiphenyl-3-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
0.000083 - 0.00131
5-[3-(biphenyl-3-yl)prop-1-yn-1-yl]-6-ethylpyrimidine-2,4-diamine
0.002 - 0.00981
5-[3-methoxy-3-(3,4,5-trimethoxyphenyl)prop-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
0.00155
6,6-dimethyl-1-(4-methylphenyl)-1,6-dihydro-1,3,5-triazine-2,4-diamine
pH 7.3, 22°C
0.0003591
6,6-dimethyl-1-[3-(4-phenylbutyl)phenyl]-1,6-dihydro-1,3,5-triazine-2,4-diamine
pH 7.3, 22°C
0.0000052 - 0.000038
6-(2-[4-(benzyloxy)phenyl]ethyl)quinazoline-2,4-diamine
0.0000009 - 0.000617
6-ethyl-5-(4-methoxyphenyl)pyrimidine-2,4-diamine
0.00000155 - 0.00000733
6-ethyl-5-phenylpyrimidine-2,4-diamine
0.000064 - 0.00119
6-ethyl-5-[3-(3,4,5-trimethoxyphenyl)prop-1-yn-1-yl]pyrimidine-2,4-diamine
0.00023 - 0.0017
6-ethyl-5-[3-(4-methoxybiphenyl-3-yl)prop-1-yn-1-yl]pyrimidine-2,4-diamine
0.00017 - 0.0341
6-methyl-5-[3-(3,4,5-trimethoxyphenyl)but-1-yn-1-yl]pyrimidine-2,4-diamine
0.00119 - 0.00391
6-methyl-5-[3-(3,4,5-trimethoxyphenyl)pent-1-yn-1-yl]pyrimidine-2,4-diamine
0.000049 - 0.00125
6-methyl-5-[3-(3,4,5-trimethoxyphenyl)prop-1-yn-1-yl]pyrimidine-2,4-diamine
0.00294 - 0.00481
6-methyl-5-[3-methyl-3-(3,4,5-trimethoxyphenyl)but-1-yn-1-yl]pyrimidine-2,4-diamine
0.0000016 - 0.0000118
6-[(3,4-dimethoxyanilino)methyl]-2,4-quinazolinediamine
0.0000019 - 0.000042
6-[2-(4-butoxyphenyl)ethyl]quinazoline-2,4-diamine
0.0000078 - 0.000048
6-[2-(4-ethoxyphenyl)ethyl]quinazoline-2,4-diamine
0.0000076 - 0.000072
6-[2-(4-hexoxyphenyl)ethyl]quinazoline-2,4-diamine
0.0000053 - 0.000269
6-[2-(4-octyloxyphenyl)ethyl]quinazoline-2,4-diamine
0.00000742
7-[(4-aminophenyl)methyl]-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine
pH 7.3, 22°C
0.0000122
7-[5-[(2,4-diaminopyrimidin-5-yl)methyl]-2,3-dimethoxyphenyl]hept-6-ynoic acid
pH 7.0
0.0000000078 - 0.0000021
aminopterin
0.00000023 - 0.0000009
AR-101
0.00000022 - 0.0000035
Ar-102
0.748
atherospermidine
pH 6.0, 28°C, recombinant enzyme
0.00000011 - 8
cycloguanil
0.005
deoxytubulosine
-
-
0.00178
epicatechin-3-O-gallate
-
pH 7.4, 25°C
0.00092
epigallocatechin-3-O-gallate
-
pH 7.4, 25°C
0.0000013 - 0.0000096
ethyl 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoate
0.0000002 - 0.0000026
iclaprim
0.717
isomoschatoline
pH 6.0, 28°C, recombinant enzyme
0.00034
L-erythro-biopterin
-
with 7,8-dihydrofolate
2.615
liriodenine
pH 6.0, 28°C, recombinant enzyme
1.26
melosmine
pH 6.0, 28°C, recombinant enzyme
0.00000000002 - 0.022
methotrexate
0.0000006 - 0.0000241
methyl 4-(2,6-diamino-5-phenylpyrimidin-4-yl)butanoate
0.0000033 - 0.000024
methyl 4-[(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) methyl]benzene carboxylate
0.0000005 - 0.0000028
methyl 4-[2,6-diamino-5-(3-chlorophenyl)pyrimidin-4-yl]butanoate
0.0000016 - 0.000013
methyl 5-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) pentanoate
0.00018
N10-formylaminopterin
Tequatrovirus T4
-
-
0.0016
N10-formyldihydrofolate
-
-
0.000348
nolatrexed
pH 7.4, 25°C, recombinant enzyme
0.0000005 - 0.00029
pemetrexed
0.0000039 - 0.000008
piritrexim
0.000045
pralatrexate
-
-
0.0000052 - 0.00035
PY957
0.00000005 - 0.068
pyrimethamine
0.0000082
quinone methide
-
pH 7.4, 25°C
0.0000931 - 0.002
raltitrexed
0.0000021
TMP
pH and temperature not specified in the publication
0.000001 - 0.046
trimethoprim
0.00000023 - 0.000000597
trimetrexate
0.007
tylophorinidine
-
-
-
0.00000044 - 0.0000155
WR99210
additional information
additional information
-
0.000062
(E)-5-[2-(2-methoxyphenyl)prop-1-en-1-yl]furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.0005
(E)-5-[2-(2-methoxyphenyl)prop-1-en-1-yl]furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.00016
(Z)-5-[2-(2-methoxyphenyl)prop-1-en-1-yl]furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.0016
(Z)-5-[2-(2-methoxyphenyl)prop-1-en-1-yl]furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.000097
2,4-diamino-5-[3-(2-methoxy-5-phenylphenyl)prop-1-ynyl]-6-ethylpyrimidine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.00033
2,4-diamino-5-[3-(2-methoxy-5-phenylphenyl)prop-1-ynyl]-6-ethylpyrimidine
wild type enzyme, at pH 7.0 and 25°C
0.00049
2,4-diamino-5-[3-(2-methoxy-5-phenylphenyl)prop-1-ynyl]-6-ethylpyrimidine
mutant enzyme F96I, at pH 7.0 and 25°C
0.00043
2,4-diamino-5-[3-(2-phenyl-5-methoxyphenyl)prop-1-ynyl]-6-ethylpyrimidine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.00104
2,4-diamino-5-[3-(2-phenyl-5-methoxyphenyl)prop-1-ynyl]-6-ethylpyrimidine
mutant enzyme F96I, at pH 7.0 and 25°C
0.00259
2,4-diamino-5-[3-(2-phenyl-5-methoxyphenyl)prop-1-ynyl]-6-ethylpyrimidine
wild type enzyme, at pH 7.0 and 25°C
0.00000026
2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine
mutant K37Q enzyme, pH 7.4, 37°C
0.00000058
2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine
recombinant mutant N64F enzyme, pH 7.4, 37°C
0.00000071
2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine
mutant K37Q/F69N enzyme, pH 7.4, 37°C
0.0000008
2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine
mutant K37S enzyme, pH 7.4, 37°C
0.00000142
2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine
mutant K37S/F69S enzyme, pH 7.4, 37°C
0.0000027
2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine
wild-type enzyme, pH 7.4, 37°C
0.0000063
2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine
wild-type enzyme, pH 7.4, 37°C
0.0000244
2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine
recombinant wild-type enzyme, pH 7.4, 37°C
0.00039
3-(2,4-diamino-6-methylpyrimidin-5-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-yn-1-ol
mutant enzyme Y102F, at pH 7.0 and 25°C
0.00439
3-(2,4-diamino-6-methylpyrimidin-5-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-yn-1-ol
mutant enzyme F96I, at pH 7.0 and 25°C
0.00489
3-(2,4-diamino-6-methylpyrimidin-5-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-yn-1-ol
wild type enzyme, at pH 7.0 and 25°C
0.0000036
4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoic acid
pH 7, 22.6°C
0.000049
4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoic acid
pH 7.3, 22.6°C
0.0000014
4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]phenol
-
pH 7.0, 25°C
0.000034
4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]phenol
-
pH 7.0, 25°C
0.0000003
5-(3,4-dichlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.000001
5-(3,4-dichlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.0000126
5-(3,4-dichlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
mutant C59R/S108N, pH 7.0, 25°C
0.0000534
5-(3,4-dichlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C
0.0000008
5-(3-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.0000014
5-(3-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
mutant C59R/S108N, pH 7.0, 25°C
0.0000016
5-(3-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.0000033
5-(3-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C
0.0000003
5-(4-bromophenyl)-6-ethylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.0000153
5-(4-bromophenyl)-6-ethylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.0000443
5-(4-bromophenyl)-6-ethylpyrimidine-2,4-diamine
-
mutant C59R/S108N, pH 7.0, 25°C
0.000303
5-(4-bromophenyl)-6-ethylpyrimidine-2,4-diamine
-
mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C
0.0000043
5-(4-chlorophenyl)-6-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.0002473
5-(4-chlorophenyl)-6-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.000742
5-(4-chlorophenyl)-6-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
mutant C59R/S108N, pH 7.0, 25°C
0.001576
5-(4-chlorophenyl)-6-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C
0.0000003
5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.0000282
5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.0000539
5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
mutant C59R/S108N, pH 7.0, 25°C
0.000385
5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C
0.0000003
5-(4-chlorophenyl)-6-isobutylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.000099
5-(4-chlorophenyl)-6-isobutylpyrimidine-2,4-diamine
-
mutant C59R/S108N, pH 7.0, 25°C
0.0001291
5-(4-chlorophenyl)-6-isobutylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.000798
5-(4-chlorophenyl)-6-isobutylpyrimidine-2,4-diamine
-
mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C
0.0000003
5-(4-chlorophenyl)-6-isopropylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.0000362
5-(4-chlorophenyl)-6-isopropylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.000113
5-(4-chlorophenyl)-6-isopropylpyrimidine-2,4-diamine
-
mutant C59R/S108N, pH 7.0, 25°C
0.000541
5-(4-chlorophenyl)-6-isopropylpyrimidine-2,4-diamine
-
mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C
0.0000029
5-(4-chlorophenyl)-6-phenylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.0006
5-(4-chlorophenyl)-6-phenylpyrimidine-2,4-diamine
-
mutant C59R/S108N, pH 7.0, 25°C
0.003461
5-(4-chlorophenyl)-6-phenylpyrimidine-2,4-diamine
-
mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C
0.0000005
5-(4-chlorophenyl)-6-propylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.0000494
5-(4-chlorophenyl)-6-propylpyrimidine-2,4-diamine
-
mutant C59R/S108N, pH 7.0, 25°C
0.0000519
5-(4-chlorophenyl)-6-propylpyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.000359
5-(4-chlorophenyl)-6-propylpyrimidine-2,4-diamine
-
mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C
0.000024
5-(5-[[(2,4-diamino-6-quinazolinyl)methyl](propyl)amino]-2-methoxyphenoxy) pentanoate
pH 7, 22.6°C
0.000188
5-(5-[[(2,4-diamino-6-quinazolinyl)methyl](propyl)amino]-2-methoxyphenoxy) pentanoate
pH 7.3, 22.6°C
0.00006
5-[(R/S)-2-(2'-methoxyphenyl)-3-methylbutyl]furo[2,3-d]-pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.00077
5-[(R/S)-2-(2'-methoxyphenyl)-3-methylbutyl]furo[2,3-d]-pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.00078
5-[(R/S)-2-(2'-methoxyphenyl)-3-methylpentyl]furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.0046
5-[(R/S)-2-(2'-methoxyphenyl)-3-methylpentyl]furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.00062
5-[(R/S)-2-(2'-methoxyphenyl)-4-methylpentyl]furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.0053
5-[(R/S)-2-(2'-methoxyphenyl)-4-methylpentyl]furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.0033
5-[(R/S)-2-(2'-methoxyphenyl)hexyl]furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.012
5-[(R/S)-2-(2'-methoxyphenyl)hexyl]furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.0025
5-[(R/S)-2-(2'-methoxyphenyl)pentyl]furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.0028
5-[(R/S)-2-(2'-methoxyphenyl)pentyl]furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.00006
5-[(R/S)-2-cyclopropyl-2-(2'-methoxyphenyl)ethyl]furo-[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.00065
5-[(R/S)-2-cyclopropyl-2-(2'-methoxyphenyl)ethyl]furo-[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.00007
5-[(Z/E)-2-(2'-methoxyphenyl)-3-methylbut-1-en-1-yl]-furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.00083
5-[(Z/E)-2-(2'-methoxyphenyl)-3-methylbut-1-en-1-yl]-furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.00007
5-[(Z/E)-2-(2'-methoxyphenyl)-3-methylpent-1-en-1-yl]-furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.0011
5-[(Z/E)-2-(2'-methoxyphenyl)-3-methylpent-1-en-1-yl]-furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.00091
5-[(Z/E)-2-(2'-methoxyphenyl)-4-methylpent-1-en-1-yl]-furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.011
5-[(Z/E)-2-(2'-methoxyphenyl)-4-methylpent-1-en-1-yl]-furo[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.00055
5-[(Z/E)-2-(2'-methoxyphenyl)hex-1-en-1-yl]furo[2,3-d]-pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.0043
5-[(Z/E)-2-(2'-methoxyphenyl)hex-1-en-1-yl]furo[2,3-d]-pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.00014
5-[(Z/E)-2-(2'-methoxyphenyl)pent-1-en-1-yl]furo[2,3-d]-pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.0016
5-[(Z/E)-2-(2'-methoxyphenyl)pent-1-en-1-yl]furo[2,3-d]-pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.00008
5-[(Z/E)-2-cyclopropyl-2-(2'-methoxyphenyl)vinyl]furo-[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.0013
5-[(Z/E)-2-cyclopropyl-2-(2'-methoxyphenyl)vinyl]furo-[2,3-d]pyrimidine-2,4-diamine
-
pH 7.4, 37°C
0.00183
5-[3-(2,5-dimethoxybiphenyl-4-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.00516
5-[3-(2,5-dimethoxybiphenyl-4-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
wild type enzyme, at pH 7.0 and 25°C
0.00752
5-[3-(2,5-dimethoxybiphenyl-4-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
mutant enzyme F96I, at pH 7.0 and 25°C
0.0003
5-[3-(2,5-dimethoxyphenyl)prop-1-yn-1-yl]-6-ethylpyrimidine-2,4-diamine
wild type enzyme, at pH 7.0 and 25°C
0.00069
5-[3-(2,5-dimethoxyphenyl)prop-1-yn-1-yl]-6-ethylpyrimidine-2,4-diamine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.0205
5-[3-(2,5-dimethoxyphenyl)prop-1-yn-1-yl]-6-ethylpyrimidine-2,4-diamine
mutant enzyme F96I, at pH 7.0 and 25°C
0.0002
5-[3-(2,5-dimethoxyphenyl)prop-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.00036
5-[3-(2,5-dimethoxyphenyl)prop-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
wild type enzyme, at pH 7.0 and 25°C
0.00451
5-[3-(2,5-dimethoxyphenyl)prop-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
mutant enzyme F96I, at pH 7.0 and 25°C
0.0016
5-[3-(2-methoxybiphenyl-4-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.00583
5-[3-(2-methoxybiphenyl-4-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
wild type enzyme, at pH 7.0 and 25°C
0.0092
5-[3-(2-methoxybiphenyl-4-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
mutant enzyme F96I, at pH 7.0 and 25°C
0.00164
5-[3-(3-methoxybiphenyl-4-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.0104
5-[3-(3-methoxybiphenyl-4-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
mutant enzyme F96I, at pH 7.0 and 25°C
0.0117
5-[3-(3-methoxybiphenyl-4-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
wild type enzyme, at pH 7.0 and 25°C
0.00103
5-[3-(5-methoxybiphenyl-3-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.0011
5-[3-(5-methoxybiphenyl-3-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
mutant enzyme F96I, at pH 7.0 and 25°C
0.00266
5-[3-(5-methoxybiphenyl-3-yl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
wild type enzyme, at pH 7.0 and 25°C
0.000083
5-[3-(biphenyl-3-yl)prop-1-yn-1-yl]-6-ethylpyrimidine-2,4-diamine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.00037
5-[3-(biphenyl-3-yl)prop-1-yn-1-yl]-6-ethylpyrimidine-2,4-diamine
wild type enzyme, at pH 7.0 and 25°C
0.00131
5-[3-(biphenyl-3-yl)prop-1-yn-1-yl]-6-ethylpyrimidine-2,4-diamine
mutant enzyme F96I, at pH 7.0 and 25°C
0.002
5-[3-methoxy-3-(3,4,5-trimethoxyphenyl)prop-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.00635
5-[3-methoxy-3-(3,4,5-trimethoxyphenyl)prop-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
mutant enzyme F96I, at pH 7.0 and 25°C
0.00981
5-[3-methoxy-3-(3,4,5-trimethoxyphenyl)prop-1-yn-1-yl]-6-methylpyrimidine-2,4-diamine
wild type enzyme, at pH 7.0 and 25°C
0.0000052
6-(2-[4-(benzyloxy)phenyl]ethyl)quinazoline-2,4-diamine
-
pH 7.0, 25°C
0.000038
6-(2-[4-(benzyloxy)phenyl]ethyl)quinazoline-2,4-diamine
-
pH 7.0, 25°C
0.0000009
6-ethyl-5-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.0000031
6-ethyl-5-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
wild-type, pH 7.0, 25°C
0.000086
6-ethyl-5-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
mutant C59R/S108N, pH 7.0, 25°C
0.000617
6-ethyl-5-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C
0.00000155
6-ethyl-5-phenylpyrimidine-2,4-diamine
wild-type
0.00000733
6-ethyl-5-phenylpyrimidine-2,4-diamine
mutant S58R/S117N
0.000064
6-ethyl-5-[3-(3,4,5-trimethoxyphenyl)prop-1-yn-1-yl]pyrimidine-2,4-diamine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.00032
6-ethyl-5-[3-(3,4,5-trimethoxyphenyl)prop-1-yn-1-yl]pyrimidine-2,4-diamine
wild type enzyme, at pH 7.0 and 25°C
0.00119
6-ethyl-5-[3-(3,4,5-trimethoxyphenyl)prop-1-yn-1-yl]pyrimidine-2,4-diamine
mutant enzyme F96I, at pH 7.0 and 25°C
0.00023
6-ethyl-5-[3-(4-methoxybiphenyl-3-yl)prop-1-yn-1-yl]pyrimidine-2,4-diamine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.00121
6-ethyl-5-[3-(4-methoxybiphenyl-3-yl)prop-1-yn-1-yl]pyrimidine-2,4-diamine
wild type enzyme, at pH 7.0 and 25°C
0.0017
6-ethyl-5-[3-(4-methoxybiphenyl-3-yl)prop-1-yn-1-yl]pyrimidine-2,4-diamine
mutant enzyme F96I, at pH 7.0 and 25°C
0.00017
6-methyl-5-[3-(3,4,5-trimethoxyphenyl)but-1-yn-1-yl]pyrimidine-2,4-diamine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.0102
6-methyl-5-[3-(3,4,5-trimethoxyphenyl)but-1-yn-1-yl]pyrimidine-2,4-diamine
wild type enzyme, at pH 7.0 and 25°C
0.0341
6-methyl-5-[3-(3,4,5-trimethoxyphenyl)but-1-yn-1-yl]pyrimidine-2,4-diamine
mutant enzyme F96I, at pH 7.0 and 25°C
0.00119
6-methyl-5-[3-(3,4,5-trimethoxyphenyl)pent-1-yn-1-yl]pyrimidine-2,4-diamine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.00337
6-methyl-5-[3-(3,4,5-trimethoxyphenyl)pent-1-yn-1-yl]pyrimidine-2,4-diamine
wild type enzyme, at pH 7.0 and 25°C
0.00391
6-methyl-5-[3-(3,4,5-trimethoxyphenyl)pent-1-yn-1-yl]pyrimidine-2,4-diamine
mutant enzyme F96I, at pH 7.0 and 25°C
0.000049
6-methyl-5-[3-(3,4,5-trimethoxyphenyl)prop-1-yn-1-yl]pyrimidine-2,4-diamine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.00115
6-methyl-5-[3-(3,4,5-trimethoxyphenyl)prop-1-yn-1-yl]pyrimidine-2,4-diamine
mutant enzyme F96I, at pH 7.0 and 25°C
0.00125
6-methyl-5-[3-(3,4,5-trimethoxyphenyl)prop-1-yn-1-yl]pyrimidine-2,4-diamine
wild type enzyme, at pH 7.0 and 25°C
0.00294
6-methyl-5-[3-methyl-3-(3,4,5-trimethoxyphenyl)but-1-yn-1-yl]pyrimidine-2,4-diamine
mutant enzyme Y102F, at pH 7.0 and 25°C
0.00428
6-methyl-5-[3-methyl-3-(3,4,5-trimethoxyphenyl)but-1-yn-1-yl]pyrimidine-2,4-diamine
wild type enzyme, at pH 7.0 and 25°C
0.00481
6-methyl-5-[3-methyl-3-(3,4,5-trimethoxyphenyl)but-1-yn-1-yl]pyrimidine-2,4-diamine
mutant enzyme F96I, at pH 7.0 and 25°C
0.0000016
6-[(3,4-dimethoxyanilino)methyl]-2,4-quinazolinediamine
pH 7, 22.6°C
0.0000118
6-[(3,4-dimethoxyanilino)methyl]-2,4-quinazolinediamine
pH 7.3, 22.6°C
0.0000019
6-[2-(4-butoxyphenyl)ethyl]quinazoline-2,4-diamine
-
pH 7.0, 25°C
0.000042
6-[2-(4-butoxyphenyl)ethyl]quinazoline-2,4-diamine
-
pH 7.0, 25°C
0.0000078
6-[2-(4-ethoxyphenyl)ethyl]quinazoline-2,4-diamine
-
pH 7.0, 25°C
0.000048
6-[2-(4-ethoxyphenyl)ethyl]quinazoline-2,4-diamine
-
pH 7.0, 25°C
0.0000076
6-[2-(4-hexoxyphenyl)ethyl]quinazoline-2,4-diamine
-
pH 7.0, 25°C
0.000072
6-[2-(4-hexoxyphenyl)ethyl]quinazoline-2,4-diamine
-
pH 7.0, 25°C
0.0000053
6-[2-(4-octyloxyphenyl)ethyl]quinazoline-2,4-diamine
-
pH 7.0, 25°C
0.000269
6-[2-(4-octyloxyphenyl)ethyl]quinazoline-2,4-diamine
-
pH 7.0, 25°C
0.0000000078
aminopterin
-
-
0.00000061
aminopterin
-
-
0.0000017
aminopterin
-
pH 6, 25°C
0.0000021
aminopterin
pH 6, 25°C
0.00000023
AR-101
wild-type enzyme
0.0000009
AR-101
mutant F98Y
0.00000022
Ar-102
wild-type enzyme
0.0000035
Ar-102
mutant F98Y
0.00000011
cycloguanil
pH 6, temperature not specified in the publication, isolate PKNY146CSP
0.00000024
cycloguanil
mutant K27E, pH 5.0, 25°C
0.00000028
cycloguanil
mutant Y35G/F37L, pH 5.0, 25°C
0.0000006
cycloguanil
mutant Y35Q/F37R, pH 5.0, 25°C
0.000001
cycloguanil
-
wild-type, 25°C, pH 7.0
0.0000012
cycloguanil
mutant Y35L/F37R, pH 5.0, 25°C
0.0000015
cycloguanil
wild-type, pH 5.0, 25°C
0.0000016
cycloguanil
-
recombinant mutant S108T
0.0000018
cycloguanil
mutant Y35L/F37T, pH 5.0, 25°C
0.00000199
cycloguanil
-
mutant W48Y/N188Y, 25°C, pH 7.0
0.000002
cycloguanil
-
recombinant mutant S108A
0.0000026
cycloguanil
-
recombinant wild-type enzyme
0.000003
cycloguanil
-
recombinant mutant S108C
0.00000548
cycloguanil
-
mutant W48Y, 25°C, pH 7.0
0.000015
cycloguanil
-
recombinant mutant S108N
0.000017
cycloguanil
-
recombinant mutant S108G
0.0000205
cycloguanil
-
mutant enzyme T86S, in 50 mM TES, pH 7.0, at 37°C
0.000067
cycloguanil
-
wild-type enzyme
0.000158
cycloguanil
-
recombinant mutant S108Q
0.000256
cycloguanil
-
wild type enzyme, in 50 mM TES, pH 7.0, at 37°C
0.000743
cycloguanil
-
mutant enzyme
0.001915
cycloguanil
-
mutant enzyme T86N, in 50 mM TES, pH 7.0, at 37°C
8
cycloguanil
-
above, pH 6.0, 25°C recombinant His-tagged enzyme
0.0000013
ethyl 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoate
pH 7, 22.6°C
0.0000096
ethyl 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoate
pH 7.3, 22.6°C
0.000026
folate
-
-
0.025
folate
-
with 7,8-dihydrofolate
0.036
folate
-
with 7,8-dihydrofolate
0.0000002
iclaprim
wild-type enzyme
0.0000026
iclaprim
mutant F98Y
0.00000000002
methotrexate
-
recombinant enzyme
0.000000002
methotrexate
pH 7.4, 37°C, mutant Q35K
0.000000003
methotrexate
pH 7.4, 37°C, mutant N64S
0.0000000061
methotrexate
-
-
0.000000007
methotrexate
-
-
0.000000009
methotrexate
-
recombinant enzyme
0.000000009
methotrexate
-
isozyme type III, R-plasmid encoded
0.000000014
methotrexate
-
pH 7.4, 37°C, wild-type enzyme
0.000000016
methotrexate
-
recombinant enzyme derived from E. coli
0.000000019
methotrexate
pH 7.4, 37°C, mutant Q35K/N64F
0.0000000289
methotrexate
-
25°C
0.000000029
methotrexate
pH 7.4, 37°C, mutant N64F
0.000000031
methotrexate
-
wild-type, pH 7.6, 23°C
0.000000031
methotrexate
wild-type, pH 7.6, 23°C
0.000000042
methotrexate
-
pH 7.4, 37°C, wild-type enzyme
0.000000047
methotrexate
pH 7.4, 37°C, mutant Q35S
0.000000047
methotrexate
pH 7.4, 37°C, mutant Q35S/N64S
0.000000063
methotrexate
-
pH 7.4, 37°C, mutant K37Q
0.000000093
methotrexate
pH 7.4, 37°C, wild-type enzyme
0.000000095
methotrexate
pH 7.4, 25°C, recombinant enzyme
0.0000001
methotrexate
-
recombinant enzyme
0.00000015
methotrexate
-
recombinant from E. coli
0.0000002
methotrexate
-
-
0.00000023
methotrexate
-
recombinant bifunctional enzyme
0.0000003
methotrexate
-
-
0.0000005
methotrexate
-
pH 6, 25°C
0.0000007
methotrexate
pH 6, 25°C
0.0000013
methotrexate
-
pH 6.0, 25°C recombinant His-tagged enzyme
0.0000014
methotrexate
-
recombinant enzyme
0.0000017
methotrexate
mutant F31P, pH 7.6, 23°C
0.0000052
methotrexate
-
wild-type enzyme
0.0000069
methotrexate
-
mutant enzyme
0.000009
methotrexate
mutant F31G/Q35N, pH 7.6, 23°C
0.00001
methotrexate
mutant F31P/Q35H, pH 7.6, 23°C
0.000012
methotrexate
mutant F31P/Q35E, pH 7.6, 23°C
0.000012
methotrexate
mutant F31R/F34A/Q35N, pH 7.6, 23°C
0.000018
methotrexate
-
wild-type enzyme
0.00002
methotrexate
-
mutant V115A, pH 7.6, 23°C
0.00002
methotrexate
-
mutant V115C, pH 7.6, 23°C
0.000021
methotrexate
mutant F31R/Q35E, pH 7.6, 23°C
0.000026
methotrexate
-
-
0.00003
methotrexate
mutant F31S/Q35E, pH 7.6, 23°C
0.000059
methotrexate
mutant F31R/F34T/Q35S, pH 7.6, 23°C
0.000086
methotrexate
mutant F31R/F34T/Q35R, pH 7.6, 23°C
0.00009
methotrexate
-
bacterial, R factor encoded isozyme type II
0.00018
methotrexate
mutant F31A/F34V/Q35H, pH 7.6, 23°C
0.0011
methotrexate
-
with 7,8-dihydrofolate
0.0059
methotrexate
-
competitive
0.022
methotrexate
pH 6.0, 28°C, recombinant enzyme
0.0000006
methyl 4-(2,6-diamino-5-phenylpyrimidin-4-yl)butanoate
-
wild-type, pH 7.0, 25°C
0.0000055
methyl 4-(2,6-diamino-5-phenylpyrimidin-4-yl)butanoate
-
mutant C59R/S108N, pH 7.0, 25°C
0.0000087
methyl 4-(2,6-diamino-5-phenylpyrimidin-4-yl)butanoate
-
wild-type, pH 7.0, 25°C
0.0000241
methyl 4-(2,6-diamino-5-phenylpyrimidin-4-yl)butanoate
-
mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C
0.0000033
methyl 4-[(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) methyl]benzene carboxylate
pH 7, 22.6°C
0.000024
methyl 4-[(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) methyl]benzene carboxylate
pH 7.3, 22.6°C
0.0000005
methyl 4-[2,6-diamino-5-(3-chlorophenyl)pyrimidin-4-yl]butanoate
-
wild-type, pH 7.0, 25°C
0.0000025
methyl 4-[2,6-diamino-5-(3-chlorophenyl)pyrimidin-4-yl]butanoate
-
wild-type, pH 7.0, 25°C
0.0000027
methyl 4-[2,6-diamino-5-(3-chlorophenyl)pyrimidin-4-yl]butanoate
-
mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C
0.0000028
methyl 4-[2,6-diamino-5-(3-chlorophenyl)pyrimidin-4-yl]butanoate
-
mutant C59R/S108N, pH 7.0, 25°C
0.0000016
methyl 5-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) pentanoate
pH 7, 22.6°C
0.000013
methyl 5-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) pentanoate
pH 7.3, 22.6°C
0.0018
NADP+
-
-
0.0023
NADP+
-
with 7,8-dihydrofolate
0.021
NADP+
-
with 7,8-dihydrofolate
0.0000005
pemetrexed
-
wild-type, pH 7.6, 23°C
0.000131
pemetrexed
-
mutant V115A, pH 7.6, 23°C
0.000283
pemetrexed
-
mutant V115C, pH 7.6, 23°C
0.00029
pemetrexed
pH 7.4, 25°C, recombinant enzyme
0.0000039
piritrexim
-
-
0.000008
piritrexim
-
recombinant enzyme
0.0000052
PY957
pH 7.4, 37°C, mutant N64F
0.0000076
PY957
-
pH 7.4, 37°C, mutant K37Q
0.0000083
PY957
pH 7.4, 37°C, mutant Q35K
0.000013
PY957
pH 7.4, 37°C, mutant Q35K/N64F
0.0000219
PY957
-
pH 7.4, 37°C, wild-type enzyme
0.000023
PY957
pH 7.4, 37°C, mutant N64S
0.0000263
PY957
-
pH 7.4, 37°C, wild-type enzyme
0.000066
PY957
pH 7.4, 37°C, mutant Q35S/N64S
0.00023
PY957
pH 7.4, 37°C, wild-type enzyme
0.00035
PY957
pH 7.4, 37°C, mutant Q35S
0.00000005
pyrimethamine
pH 6, temperature not specified in the publication, isolate PKNY146CSP
0.00000012
pyrimethamine
mutant K27E, pH 5.0, 25°C
0.00000016
pyrimethamine
wild-type
0.0000002
pyrimethamine
mutant Y35G/F37L, pH 5.0, 25°C
0.00000028
pyrimethamine
-
recombinant bifunctional enzyme
0.00000037
pyrimethamine
-
trimethoprim-sensitive strain
0.00000057
pyrimethamine
mutant Y35L/F37T, pH 5.0, 25°C
0.0000006
pyrimethamine
wild-type, pH 5.0, 25°C
0.00000061
pyrimethamine
mutant Y35Q/F37R, pH 5.0, 25°C
0.00000072
pyrimethamine
-
wild-type, 25°C, pH 7.0
0.000001
pyrimethamine
-
recombinant enzyme
0.000001
pyrimethamine
-
mutant W48Y/N188Y, 25°C, pH 7.0
0.0000012
pyrimethamine
mutant Y35L/F37R, pH 5.0, 25°C
0.0000014
pyrimethamine
-
recombinant mutant S108T
0.0000015
pyrimethamine
-
recombinant wild-type enzyme
0.00000174
pyrimethamine
-
mutant W48Y, 25°C, pH 7.0
0.0000021
pyrimethamine
-
mutant enzyme T86S, in 50 mM TES, pH 7.0, at 37°C
0.0000022
pyrimethamine
-
-
0.000004
pyrimethamine
-
recombinant mutant S108A
0.000006
pyrimethamine
-
recombinant mutant S108C
0.00000635
pyrimethamine
pH 7.4, 25°C, recombinant enzyme
0.000007
pyrimethamine
-
recombinant mutant S108G
0.0000081
pyrimethamine
-
mutant I51N/C59R/N108S/I164L, pH 7.0
0.000013
pyrimethamine
-
recombinant mutant S108N
0.000014
pyrimethamine
-
trimethoprim-resistant sdtrain
0.0000176
pyrimethamine
-
mutant N51I/C59R/N108S/I164L, pH 7.0
0.000021
pyrimethamine
-
-
0.000024
pyrimethamine
-
wild type enzyme, in 50 mM TES, pH 7.0, at 37°C
0.000029
pyrimethamine
-
-
0.00005
pyrimethamine
mutant S58R/S117N
0.000064
pyrimethamine
-
wild-type enzyme
0.000065
pyrimethamine
-
recombinant enzyme derived from E. coli
0.0000724
pyrimethamine
-
mutant N51I/C59R/N108T/I164L, pH 7.0
0.000095
pyrimethamine
-
recombinant mutant S108Q
0.000147
pyrimethamine
-
mutant N51I/C59R/S108N/I164L/I150V/N182I/N201D, pH 7.0
0.000179
pyrimethamine
-
mutant enzyme T86N, in 50 mM TES, pH 7.0, at 37°C
0.000209
pyrimethamine
-
mutant N51I/C59R/S108N/I164L, pH 7.0
0.000292
pyrimethamine
-
mutant N51I/C59R/S108N/I164L/K96N, pH 7.0
0.000514
pyrimethamine
-
mutant N51I/C59R/S108N/I164L/D187A, pH 7.0
0.0007
pyrimethamine
-
recombinant enzyme
0.00072
pyrimethamine
-
with 7,8-dihydrofolate
0.00093
pyrimethamine
-
mutant enzyme
0.0036
pyrimethamine
-
pH 6, 25°C
0.013
pyrimethamine
-
pH 6.0, 25°C recombinant His-tagged enzyme
0.015
pyrimethamine
pH 6, 25°C
0.068
pyrimethamine
pH 6.0, 28°C, recombinant enzyme
0.0000931
raltitrexed
pH 7.4, 25°C, recombinant enzyme
0.0016
raltitrexed
-
pH 6, 25°C
0.002
raltitrexed
pH 6, 25°C
0.000001
trimethoprim
-
strains MB 1428 and MB 3746
0.000003
trimethoprim
mutant H26Y/Q60K/A77V/V78A/Q81H/Q91S/L100V/E133A/A149T, pH 7.0, 25°C
0.000004
trimethoprim
-
bacterial chromosomal encoded isozyme type I
0.000006
trimethoprim
wild-type enzyme
0.0000071
trimethoprim
-
trimethoprim-sensitive strain
0.000011
trimethoprim
-
strain MB 3747
0.0000176
trimethoprim
pH 7.4, 25°C, recombinant enzyme
0.000019
trimethoprim
-
isozyme type III, R-plasmid encoded
0.000019
trimethoprim
-
bacterial chromosomal encoded isozyme type III
0.000043
trimethoprim
-
pH 7.4, 37°C, wild-type enzyme
0.000068
trimethoprim
-
trimethoprim-resistant strain
0.000075
trimethoprim
-
pH 7.4, 37°C, mutant K37Q
0.000098
trimethoprim
-
wild-type enzyme
0.0001
trimethoprim
mutant F98Y
0.000143
trimethoprim
-
mutant enzyme
0.000147
trimethoprim
wild-type, pH 7.0, 25°C
0.00027
trimethoprim
pH 7.4, 37°C, mutant N64S
0.00028
trimethoprim
-
recombinant enzyme derived from E. coli
0.00039
trimethoprim
pH 7.4, 37°C, mutant Q35K
0.00048
trimethoprim
mutant enzyme Y102F, at pH 7.0 and 25°C
0.00049
trimethoprim
pH 7.4, 37°C, mutant N64F
0.00065
trimethoprim
pH 7.4, 37°C, mutant Q35K/N64F
0.0008
trimethoprim
-
pH 7.4, 37°C, wild-type enzyme
0.00081
trimethoprim
-
recombinant enzyme
0.0012
trimethoprim
pH 7.4, 37°C, mutant Q35S/N64S
0.0018
trimethoprim
pH 7.4, 37°C, mutant Q35S
0.0027
trimethoprim
-
with N10-formyldihydrofolate
0.0043
trimethoprim
-
recombinant from E. coli
0.0052
trimethoprim
pH 7.4, 37°C, wild-type enzyme
0.00598
trimethoprim
pH 6, 25°C
0.0064
trimethoprim
-
with 7,8-dihydrofolate
0.01
trimethoprim
-
bacterial, R factor encoded isozymes type I
0.0137
trimethoprim
mutant enzyme F96I, at pH 7.0 and 25°C
0.015
trimethoprim
-
pH 6, 25°C
0.0241
trimethoprim
wild type enzyme, at pH 7.0 and 25°C
0.033
trimethoprim
pH 6.0, 28°C, recombinant enzyme
0.046
trimethoprim
-
pH 6.0, 25°C recombinant His-tagged enzyme
0.00000023
trimetrexate
-
recombinant enzyme derived from E. coli
0.000000597
trimetrexate
pH 7.4, 25°C, recombinant enzyme
0.00000044
WR99210
-
wild-type, 25°C, pH 7.0
0.00000085
WR99210
-
mutant N51I/C59R/S108N/I164L/K96N, pH 7.0
0.0000009
WR99210
-
mutant enzyme T86S, in 50 mM TES, pH 7.0, at 37°C
0.0000011
WR99210
-
mutant N51I/C59R/S108N/I164L/I150V/N182I/N201D, pH 7.0
0.0000011
WR99210
-
wild type enzyme, in 50 mM TES, pH 7.0, at 37°C
0.0000012
WR99210
-
mutant N51I/C59R/S108N/I164L/D187A, pH 7.0
0.00000121
WR99210
-
mutant W48Y/N188Y, 25°C, pH 7.0
0.00000154
WR99210
-
mutant W48Y, 25°C, pH 7.0
0.0000021
WR99210
-
mutant N51I/C59R/S108N/I164L, pH 7.0
0.0000036
WR99210
-
mutant I51N/C59R/N108S/I164L, pH 7.0
0.0000039
WR99210
-
mutant enzyme T86N, in 50 mM TES, pH 7.0, at 37°C
0.0000073
WR99210
-
mutant N51I/C59R/N108S/I164L, pH 7.0
0.0000155
WR99210
-
mutant N51I/C59R/N108T/I164L, pH 7.0
additional information
additional information
-
-
-
additional information
additional information
-
-
-
additional information
additional information
-
-
-
additional information
additional information
-
-
-
additional information
additional information
-
-
-
additional information
additional information
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-
-
additional information
additional information
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-
-
additional information
additional information
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-
-
additional information
additional information
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-
-
additional information
additional information
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-
-
additional information
additional information
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-
-
additional information
additional information
-
-
-
additional information
additional information
-
-
-
additional information
additional information
-
overview
-
additional information
additional information
-
overview
-
additional information
additional information
-
overview
-
additional information
additional information
-
Ki of substrates 7,8-dihydrofolate and NADPH for the 2 isozymes
-
additional information
additional information
-
Ki-values for the native enzyme are higher than for the recombinant enzyme
-
additional information
additional information
-
overview, effect of methotrexate and trimethoprim
-
additional information
additional information
-
overview, effect of methotrexate and trimethoprim
-
additional information
additional information
-
overview, effect of methotrexate and trimethoprim
-
additional information
additional information
-
overview, effect of methotrexate and trimethoprim
-
additional information
additional information
protozoa
-
overview, effect of methotrexate and trimethoprim
-
additional information
additional information
protozoa
-
overview, effect of methotrexate and trimethoprim
-
additional information
additional information
-
folate antagonists
-
additional information
additional information
-
Ki of substrates dihydrofolate, NADPH and acetylpyridine adenine nucleotide
-
additional information
additional information
-
inhibition kinetics
-
additional information
additional information
inhibition kinetics
-
additional information
additional information
-
inhibition kinetics
-
additional information
additional information
inhibition kinetics, overview
-
additional information
additional information
-
inhibition kinetics, overview
-
additional information
additional information
inhibition kinetics, overview
-
additional information
additional information
antifolate inhibition kinetics, overview
-
additional information
additional information
-
antifolate inhibition kinetics, overview
-
additional information
additional information
-
comparison of inhibition kinetics of wild-type and mutant enzymes with those of the enzyme from Homo sapiens
-
additional information
additional information
comparison of inhibition kinetics of wild-type and mutant enzymes with those of the enzymes Pneumocystis carinii and Pneumocystis jirovecii
-
additional information
additional information
-
comparison of inhibition kinetics of wild-type and mutant enzymes with those of the enzymes Pneumocystis carinii and Pneumocystis jirovecii
-
additional information
additional information
-
comparison of inhibition kinetics of wild-type enzyme with those of wild-type and mutant enzyme from Homo sapiens
-
additional information
additional information
-
stopped-flow inhibition kinetics, molecular modeling, overview
-
additional information
additional information
inhibition kinetics of wild-type and mutant enzymes, comparison with the inhibition kinetics of enzymes and enzyme mutants from Homo sapiens and Pneumocystis carinii, overview
-
additional information
additional information
-
inhibition kinetics of wild-type and mutant enzymes, comparison with the inhibition kinetics of enzymes and enzyme mutants from Homo sapiens and Pneumocystis carinii, overview
-
additional information
additional information
inhibition kinetics of wild-type and mutant enzymes, comparison with the inhibition kinetics of enzymes and enzyme mutants from Homo sapiens and Pneumocystis jirovecii, overview
-
additional information
additional information
-
inhibition kinetics of wild-type and mutant enzymes, comparison with the inhibition kinetics of enzymes and enzyme mutants from Homo sapiens and Pneumocystis jirovecii, overview
-
additional information
additional information
inhibition kinetics of wild-type and mutant enzymes, comparison with the inhibition kinetics of enzymes and enzyme mutants from Pneumocystis carinii and Pneumocystis jirovecii, overview
-
additional information
additional information
-
inhibition kinetics of wild-type and mutant enzymes, comparison with the inhibition kinetics of enzymes and enzyme mutants from Pneumocystis carinii and Pneumocystis jirovecii, overview
-
additional information
additional information
all the investigated molecules are assumed to act as full competitive inhibitor and analysed according to the non-tight binding Michaelis-Menten model
-
additional information
pemetrexed
-
value above 0.0002 mM