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1.1.1.95: phosphoglycerate dehydrogenase

This is an abbreviated version!
For detailed information about phosphoglycerate dehydrogenase, go to the full flat file.

Word Map on EC 1.1.1.95

Reaction

3-phospho-D-glycerate
+
NAD+
=
3-phosphooxypyruvate
+
NADH
+
H+

Synonyms

3-PGDH, 3-phosphoglycerate dehydrogenase, 3-phosphoglyceric acid dehydrogenase, 3PGDH, A10, alpha-phosphoglycerate dehydrogenase, ApPGDH, At1g17745, At3g19480, At4g34200, BvSHMTa, BvSHMTb, D-3-PG dehydrogenase, D-3-phosphoglycerate dehydrogenase, D-3-phosphoglycerate:NAD oxidoreductase, D-phosphoglycerate dehydrogenase, dehydrogenase, phosphoglycerate, EDA9, EhPGDH, glycerate 3-phosphate dehydrogenase, glycerate-1,3-phosphate dehydrogenase, MARPO_0030s0029, More, NAD-dependent D-3-phosphoglycerate dehydrogenase, PGDH, PGDH1, PGDH2, PGDH3, PGK, Phgdh, phosphoglycerate dehydrogenase, phosphoglycerate kinase, phosphoglycerate oxidoreductase, phosphoglyceric acid dehydrogenase, Rv2996c, serA, serA1, type 1 D-3-phosphoglycerate dehydrogenase, type III 3-phosphoglycerate dehydrogenase, type IIIK PGDH

ECTree

     1 Oxidoreductases
         1.1 Acting on the CH-OH group of donors
             1.1.1 With NAD+ or NADP+ as acceptor
                1.1.1.95 phosphoglycerate dehydrogenase

Inhibitors

Inhibitors on EC 1.1.1.95 - phosphoglycerate dehydrogenase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(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-phosphoglycerate
3-phosphohydroxypyruvate
3-phosphooxypyruvate
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
amino acids
-
-
AMP
-
weak inhibitory effect on 3-phospho-D-glycerate oxidation, remaining activity: 75%
azacoccone E
non-competitive inhibitor in a time-dependent manner
-
beta-Alanine
-
slightly
BI-4916
-
-
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
-
glycine
hydroxyglutarate
-
product inhibition of the alpha-ketoglutarate reduction
iodoacetate
-
-
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
L-alanine
L-allothreonine
-
-
L-homoserine
-
-
L-Ser
L-serine
L-threonine
-
-
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-Butylmaleimide
-
-
N-cyclohexyl-N'-phenylthiourea
0.1 mM, 28% inhibition
-
N-ethylmaleimide
N-Heptylmaleimide
-
-
N-methyl-N-(4-methylpyridin-2-yl)-4-[3-(trifluoromethyl)phenyl]piperazine-1-carbothioamide
-
-
N-morpholinobenzenesulfonamide
-
-
N-Pentylmaleimide
-
-
N-Phenylmaleimide
-
-
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
-
-
sulfhydryl reagents
-
-
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
-
-
additional information
-