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Literature summary extracted from

  • Liu, R.; Zhang, Z.; Yang, H.; Zhou, K.; Geng, M.; Zhou, W.; Zhang, M.; Huang, X.; Li, Y.
    Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors (2019), Eur. J. Med. Chem., 180, 171-190 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.48 (4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl) phenyl)phosphonic acid
-
 Homo sapiens
2.3.1.48 (4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)phenyl)phosphonic acid
-
 Homo sapiens
2.3.1.48 (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-sulfanylidenedihydropyrimidine-4,6(1H,5H)-dione
-
 Homo sapiens
2.3.1.48 2-(3,5-difluoro-4-hydroxyphenyl)-4-((5-(4,5-dimethyl-2-(trifluoromethyl)phenyl)furan-2-yl)methylene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one
-
 Homo sapiens
2.3.1.48 2-(3,5-difluoro-4-hydroxyphenyl)-4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one
-
 Homo sapiens
2.3.1.48 2-(3,5-difluoro-4-hydroxyphenyl)-5-methyl-4-((5-(2-(trifluoromethoxy)phenyl)furan-2-yl)methylene)-2,4-dihydro-3H-pyrazol-3-one
-
 Homo sapiens
2.3.1.48 2-(3,5-difluoro-4-hydroxyphenyl)-5-methyl-4-((5-(3-oxo-2,3-dihydro-1H-inden-4-yl)furan-2-yl)methylene)-2,4-dihydro-3H-pyrazol-3-one
-
 Homo sapiens
2.3.1.48 2-(4-(2H-tetrazol-5-yl) phenyl)-4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one
-
 Homo sapiens
2.3.1.48 2-(4-(2H-tetrazol-5-yl)phenyl)-4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one
-
 Homo sapiens
2.3.1.48 2-(4-bromophenyl)-5-nitro[1,2]thiazolo[5,4-b]pyridin-3(2H)-one
-
 Homo sapiens
2.3.1.48 4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2-(4- (methylsulfonyl) phenyl)-2,4-dihydro-3H-pyrazol-3-one
-
 Homo sapiens
2.3.1.48 4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2-(4-(methylsulfonyl)phenyl)-2,4-dihydro-3H-pyrazol-3-one
-
 Homo sapiens
2.3.1.48 4-(3-cyclopropyl-4-((5-(4,5-dimethyl-2-(trifluoromethyl)phenyl)thiophen- 2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(3-cyclopropyl-4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(3-methyl-4-((5-(2-nitrophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(3-methyl-5-oxo-4-((5-(2-(trifluoromethoxy)phenyl)furan-2-yl)methylene)-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(3-methyl-5-oxo-4-((5-(3-oxo-2,3-dihydro-1H-inden-4-yl)furan-2-yl)methylene)-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(4-((2-(4,5-dimethyl-2-nitrophenyl)thiazol-5-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(4-((5-(2-(difluoromethyl)phenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(4-((5-(2-(dimethylphosphoryl)phenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(4-((5-(4,5-dimethyl-2-(trifluoromethyl)phenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-1H-pyrrol-2-yl)methylene)-3-methyl-5-oxo-4, 5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-2,5-dioxoimidazolidin-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-ethyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid C646, selective inhibitor Homo sapiens
2.3.1.48 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzonitrile
-
 Homo sapiens
2.3.1.48 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)thiophen-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(4-(1-(5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)ethylidene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(4-(2-((4,5-dimethyl-2-nitrophenyl)amino)-2-oxoethyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(4-(3-((4,5-dimethyl-2-nitrophenyl)amino)-3-oxopropyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(4-chlorophenyl)-2-(2-cyclopentylidenehydrazinyl)-1,3-thiazole
-
 Homo sapiens
2.3.1.48 4-(5-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-2,4- dioxothiazolidin-3-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(5-(4,5-dimethyl-2-nitrobenzoyl)-1H-indazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(5-(4,5-dimethyl-2-nitrobenzoyl)-1H-indol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-(5-(4,5-dimethyl-2-nitrobenzyl)-1H-indazol-1-yl)benzoic acid
-
 Homo sapiens
2.3.1.48 4-([(2E)-2-cyano-3-[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]prop-2-enoyl]amino)benzoic acid
-
 Homo sapiens
2.3.1.48 4-acetyl-2-methyl-N-(morpholin-4-yl)-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
 Homo sapiens
2.3.1.48 4-hydroxy-2-pentylquinoline-3-carboxylic acid
-
 Homo sapiens
2.3.1.48 A-485
-
 Homo sapiens
2.3.1.48 CPTH2
-
 Homo sapiens
2.3.1.48 DCH36-06
-
 Homo sapiens
2.3.1.48 MC 1823
-
 Homo sapiens
2.3.1.48 N-[(4-fluorophenyl)methyl]-2-[(1R)-5-[(methylcarbamoyl)amino]-2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-[1,3]oxazolidin]-3'-yl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]acetamide
-
 Homo sapiens
2.3.1.48 NSC694616
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.48 Homo sapiens Q09472
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.1.48 breast cancer cell
-
 Homo sapiens
-
2.3.1.48 mammary ductal carcinoma cell
-
 Homo sapiens
-
2.3.1.48 MCF-7 cell
-
 Homo sapiens
-
2.3.1.48 T-47D cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.48 acetyl-CoA + biotinylated histone H3 (1-21) peptide
-
 Homo sapiens CoA + acetylated biotinylated histone H3 (1-21) peptide
-
 ?
2.3.1.48 acetyl-CoA + [histone H3]-L-lysine27
-
 Homo sapiens CoA + [histone H3]-N6-acetyl-L-lysine27
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.48 p300
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.48 0.00016
-
 at pH 8.0 and 25°C Homo sapiens 4-(3-cyclopropyl-4-((5-(4,5-dimethyl-2-(trifluoromethyl)phenyl)thiophen- 2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.00019
-
 at pH 8.0 and 25°C Homo sapiens 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-ethyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.0002
-
 at pH 8.0 and 25°C Homo sapiens 4-(3-cyclopropyl-4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.00023
-
 at pH 8.0 and 25°C Homo sapiens 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)thiophen-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.00023
-
 at pH 8.0 and 37°C Homo sapiens 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.00029
-
 at pH 8.0 and 25°C Homo sapiens 4-(4-((5-(4,5-dimethyl-2-(trifluoromethyl)phenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.00047
-
 at pH 8.0 and 25°C Homo sapiens (4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)phenyl)phosphonic acid
2.3.1.48 0.00056
-
 at pH 8.0 and 25°C Homo sapiens 4-(3-methyl-4-((5-(2-nitrophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.00058
-
 at pH 8.0 and 25°C Homo sapiens 4-(3-methyl-5-oxo-4-((5-(3-oxo-2,3-dihydro-1H-inden-4-yl)furan-2-yl)methylene)-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.00067
-
 at pH 8.0 and 25°C Homo sapiens 2-(4-(2H-tetrazol-5-yl)phenyl)-4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one
2.3.1.48 0.00086
-
 at pH 8.0 and 25°C Homo sapiens 4-(4-((2-(4,5-dimethyl-2-nitrophenyl)thiazol-5-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.00113
-
 at pH 8.0 and 25°C Homo sapiens 4-(3-methyl-5-oxo-4-((5-(2-(trifluoromethoxy)phenyl)furan-2-yl)methylene)-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.00117
-
 at pH 8.0 and 25°C Homo sapiens 4-(4-((5-(2-(difluoromethyl)phenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.00153
-
 at pH 8.0 and 25°C Homo sapiens 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzonitrile
2.3.1.48 0.00195
-
 at pH 8.0 and 25°C Homo sapiens 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-1H-pyrrol-2-yl)methylene)-3-methyl-5-oxo-4, 5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.00207
-
 at pH 8.0 and 25°C Homo sapiens 4-(4-(1-(5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)ethylidene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.00373
-
 at pH 8.0 and 25°C Homo sapiens 2-(3,5-difluoro-4-hydroxyphenyl)-5-methyl-4-((5-(3-oxo-2,3-dihydro-1H-inden-4-yl)furan-2-yl)methylene)-2,4-dihydro-3H-pyrazol-3-one
2.3.1.48 0.00406
-
 at pH 8.0 and 25°C Homo sapiens 4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2-(4-(methylsulfonyl)phenyl)-2,4-dihydro-3H-pyrazol-3-one
2.3.1.48 0.0048
-
 at pH 8.0 and 25°C Homo sapiens 2-(3,5-difluoro-4-hydroxyphenyl)-4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one
2.3.1.48 0.00605
-
 at pH 8.0 and 25°C Homo sapiens 2-(3,5-difluoro-4-hydroxyphenyl)-5-methyl-4-((5-(3-oxo-2,3-dihydro-1H-inden-4-yl)furan-2-yl)methylene)-2,4-dihydro-3H-pyrazol-3-one
2.3.1.48 0.00713
-
 at pH 8.0 and 25°C Homo sapiens 4-([(2E)-2-cyano-3-[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]prop-2-enoyl]amino)benzoic acid
2.3.1.48 0.00731
-
 at pH 8.0 and 25°C Homo sapiens 2-(3,5-difluoro-4-hydroxyphenyl)-4-((5-(4,5-dimethyl-2-(trifluoromethyl)phenyl)furan-2-yl)methylene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one
2.3.1.48 0.00961
-
 at pH 8.0 and 25°C Homo sapiens 4-(4-(2-((4,5-dimethyl-2-nitrophenyl)amino)-2-oxoethyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.01
-
 IC50 above 0.01 mM, at pH 8.0 and 25°C Homo sapiens 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-2,5-dioxoimidazolidin-1-yl)benzoic acid
2.3.1.48 0.01
-
 IC50 above 0.01 mM, at pH 8.0 and 25°C Homo sapiens 4-(4-(3-((4,5-dimethyl-2-nitrophenyl)amino)-3-oxopropyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.01
-
 IC50 above 0.01 mM, at pH 8.0 and 25°C Homo sapiens 4-(5-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-2,4- dioxothiazolidin-3-yl)benzoic acid
2.3.1.48 0.01
-
 IC50 above 0.01 mM, at pH 8.0 and 25°C Homo sapiens 4-(5-(4,5-dimethyl-2-nitrobenzoyl)-1H-indazol-1-yl)benzoic acid
2.3.1.48 0.01
-
 IC50 above 0.01 mM, at pH 8.0 and 25°C Homo sapiens 4-(5-(4,5-dimethyl-2-nitrobenzyl)-1H-indazol-1-yl)benzoic acid
2.3.1.48 0.01
-
 IC50 above 0.01 mM, at pH 8.0 and 25°C Homo sapiens 4-(4-((5-(2-(dimethylphosphoryl)phenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
2.3.1.48 0.01
-
 IC50 above 0.01 mM, at pH 8.0 and 25°C Homo sapiens 2-(3,5-difluoro-4-hydroxyphenyl)-5-methyl-4-((5-(2-(trifluoromethoxy)phenyl)furan-2-yl)methylene)-2,4-dihydro-3H-pyrazol-3-one
2.3.1.48 0.01
-
 IC50 above 0.01 mM, at pH 8.0 and 25°C Homo sapiens 4-(5-(4,5-dimethyl-2-nitrobenzoyl)-1H-indol-1-yl)benzoic acid