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(2,3-dihydro-1H-benzotriazol-1-yl)(4-phenylpiperazin-1-yl)methanone
0.1 mM, 37% inhibition
-
(3,4-dichlorophenyl)(morpholin-4-yl)methanethione
0.1 mM, 96% inhibition
-
(3R)-N-(4,6-dimethylpyridin-2-yl)-3-methyl-4-[[4-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide
-
-
(3R,5S)-N-(4,6-dimethylpyridin-2-yl)-3,5-dimethyl-4-[[4-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide
-
-
(3S)-N-(4,6-dimethylpyridin-2-yl)-3-methyl-4-[[4-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide
-
-
(4-methylpyridin-2-yl)[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]methanethione
-
-
(NH4)2SO4
-
inhibitory effect on NADPH-dependent 3-phosphohydroxypyruvate reduction
(R)-2-amino-1-propanol
-
slightly
1-(2,4-dichlorophenyl)-2-morpholino-2-thioxoethan-1-one
-
-
1-(2-bromophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one
-
-
1-(2-chlorophenyl)-1H-pyrrole-2,5-dione
0.1 mM, 78% inhibition
-
1-(4-bromophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one
-
-
1-(4-chlorophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one
-
-
1-(4-chlorophenyl)-2-morpholino-2-thioxoethan-1-one
-
-
1-(4-fluorophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one
-
-
1-(4-iodophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one
-
-
1-(4-methoxybenzene-1-sulfonyl)piperazine
0.1 mM, 35% inhibition
-
2-(4-methylpiperidin-1-yl)-1-phenyl-2-thioxoethan-1-one
-
-
2-(4-methylpyridin-2-yl)-1-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]ethane-1-thione
-
-
2-(morpholin-4-yl)-1-(3-nitrophenyl)-2-sulfanylideneethan-1-one
-
-
2-(morpholin-4-yl)-1-(4-nitrophenyl)-2-sulfanylideneethan-1-one
-
-
2-(morpholin-4-yl)-1-phenyl-2-sulfanylideneethan-1-one
-
-
2-chloro-4-(5-[(Z)-[2-(ethylcarbamothioyl)hydrazinylidene]methyl]furan-3-yl)benzoic acid
i.e. PKUMDL-WQ-2101, specifically binds to the enzyme (PHGDH) in PHGDH-amplified breast cancer cells with EC50 values less than 0.010 mM in serine-replete media. Mainly inhibits PHGDH activity by forming hydrogen-bond networks with R134, K57, and T59 of site I and T59, T56, and K57 of site II, respectively
-
2-methyl-N-(2-[[(2E)-2-[2-[(2-nitrobenzyl)oxy]benzylidene]hydrazinyl]carbonyl]phenyl)benzamide
-
2-morpholino-1-phenyl-2-thioxoethan-1-one
-
-
2-phenylmorpholine
0.1 mM, 61% inhibition
-
3-pentyl-5,5-diphenylimidazolidine-2,4-dione
0.1 mM, 25% inhibition
-
3-[(E)-(5-cyano-2-hydroxy-4-methyl-6-oxo-1,6-dihydropyridin-3-yl)diazenyl]benzoic acid
i.e. PKUMDL-WQ-2201, specifically binds to the enzyme (PHGDH) in PHGDH-amplified breast cancer cells with EC50 values less than 0.010 mM in serine-replete media. Mainly inhibits PHGDH activity by forming hydrogen-bond networks with R134, K57, and T59 of site I and T59, T56, and K57 of site II, respectively
-
4,5,6,7-tetrahydro-1,3-benzothiazol-2-amine
0.1 mM, 46% inhibition
-
4-(5-[(Z)-[1-(3,4-dimethylphenyl)-3,5-dioxopyrazolidin-4-ylidene]methyl]furan-2-yl)-N-(1,3-thiazol-2-yl)benzenesulfonamide
-
4-benzyl-N-(4,6-dimethylpyridin-2-yl)piperazine-1-carbothioamide
-
-
4-benzyl-N-[3,5-bis(trifluoromethyl)phenyl]piperazine-1-carbothioamide
0.1 mM, 80% inhibition
-
4-chloro-N-(2-nitrophenyl)benzamide
0.1 mM, 59% inhibition
-
4-[(1S)-1-[(5-chloro-6-[2-[(2-hydroxyethyl)amino]-2-oxoethoxy]-1H-indole-2-carbonyl)amino]-2-hydroxyethyl]benzoic acid
competitive, i.e. SPR Kd
-
4-[(2-chlorophenyl)methyl]-N-(4,6-dimethylpyridin-2-yl)piperazine-1-carbothioamide
-
-
4-[(3,5-dioxo-1,2,6-thiadiazinan-4-ylidene)methyl]phenyl 2,3-diphenylquinoxaline-6-carboxylate
-
4-[(3-chlorophenyl)methyl]-N-(4,6-dimethylpyridin-2-yl)piperazine-1-carbothioamide
-
-
4-[(4,6-dimethylpyridin-2-yl)carbamothioyl]-1-[[4-(trifluoromethyl)phenyl]methyl]piperazine-2-carboxylic acid
-
-
4-[(4-bromophenyl)methyl]-N-(4,6-dimethylpyridin-2-yl)piperazine-1-carbothioamide
-
-
4-[3-(trifluoromethyl)phenyl]-N-[4-(trifluoromethyl)pyridin-2-yl]piperazine-1-carbothioamide
-
-
5-[(2-furanylcarbonyl)amino]-3-methyl-4-thiocyanato-2-thiophenecarboxylic acid ethyl ester
i.e. CBR-5884, covalent inhibitor that binds to a Cys in the non-active site and disrupts its oligomeric state. CBR-5884 inhibits the growth of cells by 35% to 60% in serine-abundant media, and by 80% to 90% in serine-depleted media at 0.030 mM
-
adenosine 5'-diphosphoribose
0.12 mM, 50% inhibition. NAD+ competitive inhibitor
Ag+
-
inhibition can be overcome by addition of dithiothreitol
AMP
-
weak inhibitory effect on 3-phospho-D-glycerate oxidation, remaining activity: 75%
azacoccone E
non-competitive inhibitor in a time-dependent manner
-
cyclohexa-2,5-diene-1,4-dione
0.1 mM, 100% inhibition
ethyl 5-[(furan-2-carbonyl)amino]-3-methyl-4-(nitrilo-lambda4-sulfanyl)thiophene-2-carboxylate
noncompetitive, i.e. CBR-5884
-
hydroxyglutarate
-
product inhibition of the alpha-ketoglutarate reduction
ixocarpalactone A
non-competitive inhibitor relative to the substrate of NAD coenzyme
-
K2HPO4
-
inhibitory effect on NADPH-dependent 3-phosphohydroxypyruvate reduction. It appears that the phosphate ion PO43- exerts its inhibitory effect by binding to the free enzyme and NADPH-enzyme complex
Mercurials
-
inhibition can be overcome by addition of dithiothreitol
-
methyl 2-([4-[3-(trifluoromethyl)phenyl]piperazine-1-carbothioyl]amino)pyridine-4-carboxylate
-
-
morpholino(phenyl)methanethione
-
-
N'-(4,6-dimethylpyridin-2-yl)-N-methyl-N-[2-(methyl[[4-(trifluoromethyl)phenyl]methyl]amino)ethyl]thiourea
-
-
N-(3-methylphenyl)-4-[3-(trifluoromethyl)phenyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)(oxo)[4-(trifluoromethyl)phenyl]ethanethioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-3-(hydroxymethyl)-4-[[4-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-3-([[4-(trifluoromethyl)phenyl]methyl]amino)piperidine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-3-methyl-4-[[4-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-3-phenyl-4-[[4-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-3-[3-(trifluoromethyl)anilino]piperidine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-3-[4-(trifluoromethyl)anilino]piperidine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-(2-methoxyphenyl)piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-(3-methoxyphenyl)piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-(4-(trifluoromethyl)benzyl)piperazine-1-carbothioamide
i.e. NCT-503, non-competitive inhibitor in regards to substrates and cofactors, closely binds to the active site
-
N-(4,6-dimethylpyridin-2-yl)-4-(4-methoxyphenyl)piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-(pyridin-2-yl)piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-(pyridin-3-yl)piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-(pyridin-4-yl)piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[(2-fluorophenyl)methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[(2-methylphenyl)methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[(3-fluorophenyl)methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[(3-methylphenyl)methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[(4-fluorophenyl)methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[(4-methylphenyl)methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[(pyridin-2-yl)methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[(pyridin-3-yl)methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[(pyridin-4-yl)methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[2-(trifluoromethyl)phenyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[2-[4-(trifluoromethyl)phenyl]ethyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[3-(trifluoromethyl)anilino][1,4'-bipiperidine]-1'-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[3-(trifluoromethyl)benzoyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[3-(trifluoromethyl)phenyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[4-(trifluoromethyl)anilino][1,4'-bipiperidine]-1'-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[4-(trifluoromethyl)benzoyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[4-(trifluoromethyl)phenyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[6-(trifluoromethyl)pyridin-2-yl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[[2-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[[3-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[[4-(trifluoromethoxy)phenyl]methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[[4-(trifluoromethyl)phenyl]methyl]-1,4-diazepane-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[[4-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide
-
N-(4,6-dimethylpyridin-2-yl)-5-[[4-(trifluoromethyl)phenyl]methyl]hexahydropyrrolo[3,4-c]pyrrole-2(1H)-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-N'-[2-(methyl[[4-(trifluoromethyl)phenyl]methyl]amino)ethyl]thiourea
-
-
N-(4,6-dimethylpyridin-2-yl)-N'-[2-([[4-(trifluoromethyl)phenyl]methyl]amino)ethyl]thiourea
-
-
N-(4,6-dimethylpyridin-2-yl)[4-(trifluoromethyl)phenyl]ethanethioamide
-
-
N-(4,6-dimethylpyrimidin-2-yl)-4-nitrobenzamide
0.1 mM, 13% inhibition
-
N-(4-methylpyridin-2-yl)-4-[3-(trifluoromethyl)phenyl]piperazine-1-carbothioamide
-
-
N-(4-methylpyridin-2-yl)-4-[3-(trifluoromethyl)phenyl]piperazine-1-carboxamide
-
-
N-(4-methylpyridin-2-yl)-4-[3-(trifluoromethyl)phenyl]piperazine-1-carboximidamide
-
-
N-(4-methylquinolin-2-yl)-4-[3-(trifluoromethyl)phenyl]piperazine-1-carbothioamide
-
-
N-(diphenylmethyl)-4-nitrobenzamide
0.1 mM, 54% inhibition
-
N-(pyridin-2-yl)-4-[3-(trifluoromethyl)phenyl]piperazine-1-carbothioamide
-
-
N-(pyridin-3-yl)-4-[3-(trifluoromethyl)phenyl]piperazine-1-carbothioamide
-
-
N-(pyridin-4-yl)-4-[3-(trifluoromethyl)phenyl]piperazine-1-carbothioamide
-
-
N-(quinolin-2-yl)-4-[3-(trifluoromethyl)phenyl]piperazine-1-carbothioamide
-
-
N-cyclohexyl-N'-phenylthiourea
0.1 mM, 28% inhibition
-
N-methyl-N-(4-methylpyridin-2-yl)-4-[3-(trifluoromethyl)phenyl]piperazine-1-carbothioamide
-
-
N-morpholinobenzenesulfonamide
-
-
N-[(pyridin-2-yl)methyl]-4-[3-(trifluoromethyl)phenyl]piperazine-1-carbothioamide
-
-
N-[1'-[(4,6-dimethylpyridin-2-yl)carbamothioyl][1,4'-bipiperidin]-4-yl]-3-(trifluoromethyl)benzamide
-
-
N-[1-[(4,6-dimethylpyridin-2-yl)carbamothioyl]piperidin-3-yl]-4-(trifluoromethyl)benzamide
-
-
NAD+
-
product inhibition, competitive to NADH
naphthalene-1,4-dione
0.1 mM, 95% inhibition
p-chloromercuribenzoate
-
-
p-hydroxymercuribenzoate
-
-
phenyl cyclohexylcarbamodithioate
0.1 mM, 51% inhibition
-
pyridoxal 5'-phosphate
-
-
pyridoxamine 5'-phosphate
-
-
ZnCl2
-
inhibitory effect on 3-phosphohydroxypyruvate reduction, remaining activity: 29%
[4-[(4,6-dimethylpyridin-2-yl)carbamothioyl]piperazin-1-yl]methyl 2-methoxybenzoate
-
-
[4-[(4,6-dimethylpyridin-2-yl)carbamothioyl]piperazin-1-yl]methyl 3-methoxybenzoate
-
-
[4-[(4,6-dimethylpyridin-2-yl)carbamothioyl]piperazin-1-yl]methyl 4-methoxybenzoate
-
-
3-phosphoglycerate
-
-
3-phosphoglycerate
-
noncompetitive to phosphohydroxypyruvate
3-phosphohydroxypyruvate
substrate inhibition
3-phosphohydroxypyruvate
uncompetitive substrate inhibition at high substrate concentration
3-phosphohydroxypyruvate
-
product inhibition of 3-phospho-D-glycerate oxidation, variable substrate: 3-phospho-D-glycerate, inhibition pattern: competitive; product inhibition of 3-phospho-D-glycerate oxidation, variable substrate: NAD, inhibition pattern: non-competitive
3-phosphooxypyruvate
product inhibition
3-phosphooxypyruvate
significant substrate inhibition
3-phosphooxypyruvate
significant substrate inhibition. NADH bound at or near the ASB site and reduces the amount of substrate inhibition due to substrate interaction at the ASB site
ADP
-
free ADP is more effective than the magnesium complex
ADP
-
weak inhibitory effect on 3-phospho-D-glycerate oxidation, remaining activity: 86%
ATP
-
free ATP is more effective than the magnesium complex
ATP
-
weak inhibitory effect on 3-phospho-D-glycerate oxidation, remaining activity: 85%
glycine
-
-
glycine
-
mutants show less to no inhibition
L-alanine
-
-
L-alanine
-
native enzyme and mutant H344A
L-Ser
-
mutant enzyme SerADELTA197, a C-terminally truncated mutant enzyme, shows inhibition
L-Ser
-
binding of the inhibitor to the apoenzyme displays positive cooperativity in the binding of the first two serine molecules and negative cooperativity in the binding of the last two serine molecules. At least two NADH-induced conformational forms of the enzyme bind the inhibitor in the physiological range. Successive binding of NADH to the enzyme results in an increase in the affinity for the first inhibitor ligand bound and a lessening of both the positive and negative cooperativity of inhibitor binding
L-serine
-
L-serine
10 mM, inhibits AtPGDH3 at 55%; 10 mM, inhibits AtPGDH3 at 55%
L-serine
-
dithiothreitol inhibits enzyme inhibition by serine
L-serine
-
feedback regulation of the wild-type enzyme
L-serine
-
50% inhibition at 0.005 mM and pH 7.5
L-serine
-
inhibition of enzyme from E. coli, Salmonella typhimurium and Haemophilus influenzae, not of mammalian enzyme, inhibition in both reaction directions
L-serine
-
allosteric inhibition, regulates the pathway of serine biosynthesis by end product inhibition interacting with His344, Asn346 and Asn364
L-serine
-
50% inhibition at 0.008 mM L-serine; allosteric inhibition, regulates the pathway of serine biosynthesis by end product inhibition interacting with His344, Asn346 and Asn364
L-serine
-
sigmoidal binding curve with mutant G294V/G336V, mutants with decreased sensitivity to serine
L-serine
feedback regulation, positive and negative cooperativity in absence of NADH, positive in presence of NADH, overview
L-serine
the enzyme contains an ACT regulatory domain which binds L-serine for feedback regulation, binding site lies around residues H344-N364
L-serine
physiological inhibitor, exerts its effect on at least two steps in the kinetic mechanism. There is a small but significant effect on the dissociation constant of NADH, increasing the Kd to 5 and 23 microM from 0.6 and 9 microM, respectively, for the two sets of sites in the enzyme. After the second substrate is added, serine reduces the amplitude of the signal without a significant effect on the observed rate constants for binding. The serine concentration that reduces the amplitude by 50% is equal to the K0.5 for serine inhibition. Serine binding eliminates a conformational change subsequent to substrate binding by formation of a dead-end quaternary complex consisting of enzyme, coenzyme, substrate, and effector. The rate data conform to a model in which serine can bind to two forms of the enzyme with different affinities
L-serine
potent inhibitor
L-serine
40% inhibition in a cooperative manner
L-serine
-
I0.5: 0.03 mM. In presence of KCl, the binding and the inhibition of L-serine, are cooperative and in the absence of KCl they are not
L-serine
two serine molecules bound to the regulatory domain, anion- and serine-binding sites between two adjacent subunits
L-serine
-
non-linear and competitive
N-(4,6-dimethylpyridin-2-yl)-4-[[4-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide
-
-
N-(4,6-dimethylpyridin-2-yl)-4-[[4-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide
noncompetitive, i.e. NCT-503
-
N-ethylmaleimide
-
-
N-ethylmaleimide
-
D-3-phosphoglycerate and AMP protect against inhibition
NADH
-
inhibition of phosphoglycerate oxidation
NADH
-
product inhibition of 3-phospho-D-glycerate oxidation, variable substrate: 3-phospho-D-glycerate, inhibition pattern: non-competitive; product inhibition of 3-phospho-D-glycerate oxidation, variable substrate: NAD, inhibition pattern: competitive
additional information
-
Ser, Tyr, Val, Gly, Trp, O-acetyl-L-Ser, and Cys have no effect on enzyme activity in both directions
-
additional information
L-serine (10 mM) does not inhibit AtPGDH2
-
additional information
L-serine (10 mM) does not inhibit AtPGDH2
-
additional information
L-serine (10 mM) does not inhibit AtPGDH2
-
additional information
-
L-serine (10 mM) does not inhibit AtPGDH2
-
additional information
the enzyme contains an ACT domain, which is involved in the allosteric regulation mechanism
-
additional information
-
the enzyme contains an ACT domain, which is involved in the allosteric regulation mechanism
-
additional information
substrate inhibition at concentrations above 0.1 mM
-
additional information
-
substrate inhibition at concentrations above 0.1 mM
-
additional information
HOAX expression downregulates the enzyme by 40%
-
additional information
-
HOAX expression downregulates the enzyme by 40%
-
additional information
mechanism of substrate inhibition, linked to this pH-dependent depression in activity, overview
-
additional information
-
mechanism of substrate inhibition, linked to this pH-dependent depression in activity, overview
-
additional information
CBR5884, a potent inhibitor of the human enzyme (PGDH), does not inhibit the enzyme from Mycobacterium tuberculosis
-
additional information
-
CBR5884, a potent inhibitor of the human enzyme (PGDH), does not inhibit the enzyme from Mycobacterium tuberculosis
-
additional information
-
unlike the Escherichia coli PGDH no inhibition by L-serine
-