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Literature summary extracted from

  • Ravez, S.; Corbet, C.; Spillier, Q.; Dutu, A.; Robin, A.D.; Mullarky, E.; Cantley, L.C.; Feron, O.; Frederick, R.
    alpha-Ketothioamide derivatives a promising tool to interrogate phosphoglycerate dehydrogenase (PHGDH) (2017), J. Med. Chem., 60, 1591-1597 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.95 (2,3-dihydro-1H-benzotriazol-1-yl)(4-phenylpiperazin-1-yl)methanone 0.1 mM, 37% inhibition Homo sapiens
1.1.1.95 (3,4-dichlorophenyl)(morpholin-4-yl)methanethione 0.1 mM, 96% inhibition Homo sapiens
1.1.1.95 1-(2-bromophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one
-
 Homo sapiens
1.1.1.95 1-(2-chlorophenyl)-1H-pyrrole-2,5-dione 0.1 mM, 78% inhibition Homo sapiens
1.1.1.95 1-(4-bromophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one
-
 Homo sapiens
1.1.1.95 1-(4-chlorophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one
-
 Homo sapiens
1.1.1.95 1-(4-fluorophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one
-
 Homo sapiens
1.1.1.95 1-(4-iodophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one
-
 Homo sapiens
1.1.1.95 1-(4-methoxybenzene-1-sulfonyl)piperazine 0.1 mM, 35% inhibition Homo sapiens
1.1.1.95 2-(morpholin-4-yl)-1-(3-nitrophenyl)-2-sulfanylideneethan-1-one
-
 Homo sapiens
1.1.1.95 2-(morpholin-4-yl)-1-(4-nitrophenyl)-2-sulfanylideneethan-1-one
-
 Homo sapiens
1.1.1.95 2-(morpholin-4-yl)-1-phenyl-2-sulfanylideneethan-1-one
-
 Homo sapiens
1.1.1.95 2-phenylmorpholine 0.1 mM, 61% inhibition Homo sapiens
1.1.1.95 3-pentyl-5,5-diphenylimidazolidine-2,4-dione 0.1 mM, 25% inhibition Homo sapiens
1.1.1.95 4,5,6,7-tetrahydro-1,3-benzothiazol-2-amine 0.1 mM, 46% inhibition Homo sapiens
1.1.1.95 4-benzyl-N-[3,5-bis(trifluoromethyl)phenyl]piperazine-1-carbothioamide 0.1 mM, 80% inhibition Homo sapiens
1.1.1.95 4-chloro-N-(2-nitrophenyl)benzamide 0.1 mM, 59% inhibition Homo sapiens
1.1.1.95 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 Homo sapiens
1.1.1.95 cyclohexa-2,5-diene-1,4-dione 0.1 mM, 100% inhibition Homo sapiens
1.1.1.95 ethyl 5-[(furan-2-carbonyl)amino]-3-methyl-4-(nitrilo-lambda4-sulfanyl)thiophene-2-carboxylate noncompetitive, i.e. CBR-5884 Homo sapiens
1.1.1.95 N-(4,6-dimethylpyridin-2-yl)-4-[[4-(trifluoromethyl)phenyl]methyl]piperazine-1-carbothioamide noncompetitive, i.e. NCT-503 Homo sapiens
1.1.1.95 N-(4,6-dimethylpyrimidin-2-yl)-4-nitrobenzamide 0.1 mM, 13% inhibition Homo sapiens
1.1.1.95 N-(diphenylmethyl)-4-nitrobenzamide 0.1 mM, 54% inhibition Homo sapiens
1.1.1.95 N-cyclohexyl-N'-phenylthiourea 0.1 mM, 28% inhibition Homo sapiens
1.1.1.95 naphthalene-1,4-dione 0.1 mM, 95% inhibition Homo sapiens
1.1.1.95 phenyl cyclohexylcarbamodithioate 0.1 mM, 51% inhibition Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.95 3-phospho-D-glycerate + NAD+ Homo sapiens
-
 3-phosphooxypyruvate + NADH + H+
-
 r

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.95 Homo sapiens O43175
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.95 3-phospho-D-glycerate + NAD+
-
 Homo sapiens 3-phosphooxypyruvate + NADH + H+
-
 r

Synonyms

EC Number Synonyms Comment Organism
1.1.1.95 Phgdh
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.95 NAD+
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.95 0.00987
-
 pH 8.8, 25°C Homo sapiens 1-(4-chlorophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one
1.1.1.95 0.016
-
 pH 8.8, 25°C Homo sapiens (3,4-dichlorophenyl)(morpholin-4-yl)methanethione
1.1.1.95 0.0309
-
 pH 8.8, 25°C Homo sapiens 2-(morpholin-4-yl)-1-phenyl-2-sulfanylideneethan-1-one
1.1.1.95 0.0351
-
 pH 8.8, 25°C Homo sapiens 2-(morpholin-4-yl)-1-(4-nitrophenyl)-2-sulfanylideneethan-1-one
1.1.1.95 0.0689
-
 pH 8.8, 25°C Homo sapiens 1-(4-fluorophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one
1.1.1.95 0.0752
-
 pH 8.8, 25°C Homo sapiens 4-chloro-N-(2-nitrophenyl)benzamide
1.1.1.95 0.0881
-
 pH 8.8, 25°C Homo sapiens 2-(morpholin-4-yl)-1-(3-nitrophenyl)-2-sulfanylideneethan-1-one
1.1.1.95 0.1307
-
 pH 8.8, 25°C Homo sapiens 1-(4-bromophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one
1.1.1.95 0.1607
-
 pH 8.8, 25°C Homo sapiens 1-(2-bromophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one
1.1.1.95 0.1777
-
 pH 8.8, 25°C Homo sapiens 1-(4-iodophenyl)-2-(morpholin-4-yl)-2-sulfanylideneethan-1-one

General Information

EC Number General Information Comment Organism
1.1.1.95 drug target the enzyme is an attractive drug target in tumors that overexpress PHGDH or amplify the PHGDH gene Homo sapiens