Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Maurer, B.; Rumpf, T.; Scharfe, M.; Stolfa, D.A.; Schmitt, M.L.; He, W.; Verdin, E.; Sippl, W.; Jung, M.
    Inhibitors of the NAD(+)-dependent protein desuccinylase and demalonylase Sirt5 (2012), ACS Med. Chem. Lett., 3, 1050-1053.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.B43 (5E)-1-ethyl-5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 (5E)-5-(1H-indol-3-ylmethylidene)-1-methyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 (5E)-5-[4-(benzyloxy)benzylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 (5E)-5-[4-(benzyloxy)benzylidene]-1-ethyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 (5E)-5-[4-(benzyloxy)benzylidene]-1-methyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 (5E)-5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 5-(biphenyl-4-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 5-[(1-benzyl-1H-indol-3-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 5-[(6-methoxynaphthalen-1-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 5-[4-(benzyloxy)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 5-[4-(propan-2-yl)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 5-[4-[(2-chlorobenzyl)oxy]-3-methoxybenzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 5-[4-[(4-bromobenzyl)oxy]benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.B43 cambinol
-
 Homo sapiens
2.3.1.B43 additional information no inhibition by EX-527, HR 103 or Ro 31-8220 Homo sapiens
2.3.1.B43 nicotinamide
-
 Homo sapiens
2.3.1.B43 sirtinol
-
 Homo sapiens
2.3.1.B43 suramin
-
 Homo sapiens
2.3.1.286 (5E)-1-ethyl-5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 10% inhibition at 0.05 mM Homo sapiens
2.3.1.286 (5E)-5-(1H-indol-3-ylmethylidene)-1-methyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 17% inhibition at 0.05 mM; 20% inhibition at 0.05 mM Homo sapiens
2.3.1.286 (5E)-5-[4-(benzyloxy)benzylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 13% inhibition at 0.05 mM Homo sapiens
2.3.1.286 (5E)-5-[4-(benzyloxy)benzylidene]-1-ethyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 25% inhibition at 0.05 mM Homo sapiens
2.3.1.286 (5E)-5-[4-(benzyloxy)benzylidene]-1-methyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 22% inhibition at 0.05 mM Homo sapiens
2.3.1.286 (5E)-5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 41% inhibition at 0.05 mM Homo sapiens
2.3.1.286 2-[1-[3-(amidinothio)propyl]-1H-indol-3-yl]-3-(1-methylindol-3-yl)maleimide methanesulfonate i.e. Ro 31-8220; i.e. Ro 31-8220; i.e. Ro 31-8220 Homo sapiens
2.3.1.286 5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 14% inhibition at 0.05 mM Homo sapiens
2.3.1.286 5-(biphenyl-4-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.286 5-[(1-benzyl-1H-indol-3-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 20% inhibition at 0.05 mM Homo sapiens
2.3.1.286 5-[(6-methoxynaphthalen-1-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.286 5-[4-(benzyloxy)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.286 5-[4-(propan-2-yl)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 13% inhibition at 0.05 mM Homo sapiens
2.3.1.286 5-[4-[(2-chlorobenzyl)oxy]-3-methoxybenzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.286 5-[4-[(4-bromobenzyl)oxy]benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.286 5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 30% inhibition at 0.05 mM Homo sapiens
2.3.1.286 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide i.e. EX-527; i.e. EX-527; i.e. EX-527 Homo sapiens
2.3.1.286 cambinol
-
 Homo sapiens
2.3.1.286 additional information no inhibition at 0.05 mM: (5E)-1-ethyl-5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione; no inhibition at 0.05 mM: (5E)-5-[4-(benzyloxy)benzylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione; no inhibition by EX-527, HR 103 or Ro 31-8220; no inhibition by EX-527, HR 103 or Ro 31-8220; no inhibition by EX-527, HR 103 or Ro 31-8220 Homo sapiens
2.3.1.286 nicotinamide
-
 Homo sapiens
2.3.1.286 sirtinol 24% inhibition at 0.05 mM Homo sapiens
2.3.1.286 suramin
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.B43 Homo sapiens Q9NXA8
-
-
2.3.1.286 Homo sapiens Q8IXJ6
-
-
2.3.1.286 Homo sapiens Q96EB6
-
-
2.3.1.286 Homo sapiens Q9NTG7
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.B43 NAD+ + N2-benzyloxycarbonyl-N6-succinyl-L-lysine-7-amido-4-methylcoumarin i.e. 3-[(5-[[(benzyloxy)carbonyl]amino]-5-[(4-methyl-2-oxo-2H-chromen-7-yl)carbamoyl]pentyl)carbamoyl]-propanoic acid Homo sapiens nicotinamide + N2-benzyloxycarbonyl-L-lysine-7-amido-4-methylcoumarin + 2'-O-succinyl-ADP-ribose
-
 ?
2.3.1.286 NAD+ + N2-benzyloxycarbonyl-N6-succinyl-L-lysine-7-amido-4-methylcoumarin i.e. 3-[(5-[[(benzyloxy)carbonyl]amino]-5-[(4-methyl-2-oxo-2H-chromen-7-yl)carbamoyl]pentyl)carbamoyl]-propanoic acid Homo sapiens nicotinamide + N2-benzyloxycarbonyl-L-lysine-7-amido-4-methylcoumarin + 2'-O-succinyl-ADP-ribose
-
 ?
2.3.1.286 NAD+ + N2-benzyloxycarbonyl-N6-succinyl-L-lysine-7-amido-4-methylcoumarin i.e. 3-[(5-[[(benzyloxy)carbonyl]amino]-5-[(4-methyl-2-oxo-2H-chromen-7-yl)carbamoyl]pentyl)carbamoyl]-propanoic acid Homo sapiens nicotinamide + N2-benzyloxycarbonyl-L-lysine-7-amido-4-methylcoumarin + 2'-O-succinyl-ADP ribose
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.B43 SIRT5
-
 Homo sapiens
2.3.1.286 SIRT1
-
 Homo sapiens
2.3.1.286 SIRT2
-
 Homo sapiens
2.3.1.286 SIRT3
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.B43 0.0023
-
 pH 8.0, 37°C Homo sapiens (5E)-5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.B43 0.0036
-
 pH 8.0, 37°C Homo sapiens 5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.B43 0.0062
-
 pH 8.0, 37°C Homo sapiens 5-[4-[(4-bromobenzyl)oxy]benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.B43 0.0124
-
 pH 8.0, 37°C Homo sapiens 5-[4-[(2-chlorobenzyl)oxy]-3-methoxybenzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.B43 0.0126
-
 pH 8.0, 37°C Homo sapiens 5-[4-(benzyloxy)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.B43 0.0129
-
 pH 8.0, 37°C Homo sapiens (5E)-5-[4-(benzyloxy)benzylidene]-1-ethyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.B43 0.0166
-
 pH 8.0, 37°C Homo sapiens 5-[(1-benzyl-1H-indol-3-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.B43 0.0178
-
 pH 8.0, 37°C Homo sapiens (5E)-5-[4-(benzyloxy)benzylidene]-1-methyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.B43 0.0224
-
 pH 8.0, 37°C Homo sapiens 5-[(6-methoxynaphthalen-1-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.B43 0.027
-
 pH 8.0, 37°C Homo sapiens (5E)-5-(1H-indol-3-ylmethylidene)-1-methyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.B43 0.03
-
 pH 8.0, 37°C Homo sapiens 5-(biphenyl-4-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.B43 0.0394
-
 pH 8.0, 37°C Homo sapiens 5-[4-(propan-2-yl)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.B43 0.043
-
 pH 8.0, 37°C Homo sapiens cambinol
2.3.1.B43 0.0465
-
 pH 8.0, 37°C Homo sapiens 5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.B43 0.047
-
 pH 8.0, 37°C Homo sapiens nicotinamide
2.3.1.B43 0.047
-
 pH 8.0, 37°C Homo sapiens suramin
2.3.1.B43 0.049
-
 pH 8.0, 37°C Homo sapiens sirtinol
2.3.1.B43 0.0559
-
 pH 8.0, 37°C Homo sapiens (5E)-1-ethyl-5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.B43 0.0673
-
 pH 8.0, 37°C Homo sapiens (5E)-5-[4-(benzyloxy)benzylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.0001 0.001 pH 8.0, 37°C Homo sapiens 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
2.3.1.286 0.0003 0.0026 pH 8.0, 37°C Homo sapiens suramin
2.3.1.286 0.0008
-
 pH 8.0, 37°C Homo sapiens 2-[1-[3-(amidinothio)propyl]-1H-indol-3-yl]-3-(1-methylindol-3-yl)maleimide methanesulfonate
2.3.1.286 0.0011 0.02 pH 8.0, 37°C Homo sapiens suramin
2.3.1.286 0.0012 0.1 pH 8.0, 37°C Homo sapiens nicotinamide
2.3.1.286 0.0034
-
 pH 8.0, 37°C Homo sapiens 5-[4-[(4-bromobenzyl)oxy]benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.0035
-
 pH 8.0, 37°C Homo sapiens 2-[1-[3-(amidinothio)propyl]-1H-indol-3-yl]-3-(1-methylindol-3-yl)maleimide methanesulfonate
2.3.1.286 0.0037
-
 pH 8.0, 37°C Homo sapiens 2-[1-[3-(amidinothio)propyl]-1H-indol-3-yl]-3-(1-methylindol-3-yl)maleimide methanesulfonate
2.3.1.286 0.0075
-
 pH 8.0, 37°C Homo sapiens 5-[4-[(2-chlorobenzyl)oxy]-3-methoxybenzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.0087
-
 pH 8.0, 37°C Homo sapiens 5-(biphenyl-4-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.0097
-
 pH 8.0, 37°C Homo sapiens (5E)-5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.0098
-
 pH 8.0, 37°C Homo sapiens 5-[4-(benzyloxy)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.01
-
 pH 8.0, 37°C Homo sapiens (5E)-5-[4-(benzyloxy)benzylidene]-1-methyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.0104
-
 pH 8.0, 37°C Homo sapiens 5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.0117
-
 pH 8.0, 37°C Homo sapiens 5-[(6-methoxynaphthalen-1-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.0144
-
 pH 8.0, 37°C Homo sapiens (5E)-5-[4-(benzyloxy)benzylidene]-1-ethyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.0147
-
 pH 8.0, 37°C Homo sapiens 5-[4-(propan-2-yl)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.02 0.033 pH 8.0, 37°C Homo sapiens 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
2.3.1.286 0.0203
-
 pH 8.0, 37°C Homo sapiens 5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.0293
-
 pH 8.0, 37°C Homo sapiens 5-[4-(benzyloxy)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.03
-
 pH 8.0, 37°C Homo sapiens nicotinamide
2.3.1.286 0.0303
-
 pH 8.0, 37°C Homo sapiens 5-[4-[(4-bromobenzyl)oxy]benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.037 0.131 pH 8.0, 37°C Homo sapiens sirtinol
2.3.1.286 0.038 0.058 pH 8.0, 37°C Homo sapiens sirtinol
2.3.1.286 0.0403
-
 pH 8.0, 37°C Homo sapiens 5-(biphenyl-4-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.0433
-
 pH 8.0, 37°C Homo sapiens 5-[(6-methoxynaphthalen-1-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.0464
-
 pH 8.0, 37°C Homo sapiens 5-[4-[(2-chlorobenzyl)oxy]-3-methoxybenzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
2.3.1.286 0.049
-
 pH 8.0, 37°C Homo sapiens 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
2.3.1.286 0.05 0.1 pH 8.0, 37°C Homo sapiens nicotinamide
2.3.1.286 0.056
-
 pH 8.0, 37°C Homo sapiens cambinol
2.3.1.286 0.059
-
 pH 8.0, 37°C Homo sapiens cambinol
2.3.1.286 0.116
-
 pH 8.0, 37°C Homo sapiens 5-[(1-benzyl-1H-indol-3-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione