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Literature summary for 2.3.1.48 extracted from

  • Madia, V.; Benedetti, R.; Barreca, M.; Ngo, L.; Pescatori, L.; Messore, A.; Pupo, G.; Saccoliti, F.; Valente, S.; Mai, A.; Scipione, L.; Zheng, Y.; Tintori, C.; Botta, M.; Cecchetti, V.; Altucci, L.; Di Santo, R.; Costi, R.
    Structure-activity relationships on cinnamoyl derivatives as inhibitors of p300 histone acetyltransferase (2017), ChemMedChem, 12, 1359-1368 .
    View publication on PubMed
Search for more literature for 2.3.1.48

Activating Compound

Activating Compound Comment Organism Structure
(3E,5E)-1-ethyl-3,5-bis[(4-hydroxy-3-nitrophenyl)methylidene]piperidin-4-one 128% activity at 0.1 mM Homo sapiens
(3E,5E)-3,5-bis[(3,4-dihydroxyphenyl)methylidene]piperidin-4-one 114% activity at 0.1 mM Homo sapiens
[(3E,5E)-3,5-bis[(3,4-dihydroxyphenyl)methylidene]-4-oxocyclohexyl]acetic acid 128% activity at 0.1 mM Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2E,6E)-2,6-bis[(3,4-dihydroxyphenyl)methylidene]cyclohexan-1-one 89% residual activity at 0.1 mM Homo sapiens
(2E,6E)-2,6-bis[(3,5-dibromo-4-hydroxyphenyl)methylidene]cyclohexan-1-one complete inhibition at 0.1 mM Homo sapiens
(2E,6E)-2,6-bis[(3-fluoro-4-hydroxyphenyl)methylidene]cyclohexan-1-one 6.3% residual activity at 0.1 mM Homo sapiens
(2E,6E)-2,6-bis[(4-hydroxy-3-methylphenyl)methylidene]cyclohexan-1-one 3.0% residual activity at 0.1 mM Homo sapiens
(2E,6E)-2,6-bis[(4-hydroxyphenyl)methylidene]cyclohexan-1-one 28.6% residual activity at 0.1 mM Homo sapiens
(3E,5E)-1-benzyl-3,5-bis[(3,4-dihydroxyphenyl)methylidene]piperidin-4-one 19.4% residual activity at 0.1 mM Homo sapiens
(3E,5E)-3,5-bis[(3,4-dihydroxyphenyl)methylidene]-1-methylpiperidin-4-one 82.4% residual activity at 0.1 mM Homo sapiens
(3Z,5Z)-3,5-bis[(3-bromo-4-hydroxyphenyl)methylidene]thian-4-one 7.13% residual activity at 0.1 mM Homo sapiens
1-benzyl-3,5-bis[(E)-3-bromo-4-hydroxybenzylidene]piperidin-4-one 81.6% residual activity at 0.1 mM Homo sapiens
2,5-bis[(E)-3-bromo-4-hydroxybenzylidene]cyclopentan-1-one 41.2% residual activity at 0.1 mM Homo sapiens
2,6-bis(3,4-dibromobenzylidene)cyclohexan-1-one 85.1% residual activity at 0.1 mM Homo sapiens
2,6-bis(3-bromo-4-hydroxybenzylidene)cyclohexanone RC56, specific inhibitor, complete inhibition at 0.1 mM Homo sapiens
2,6-bis(3-chloro-4-hydroxybenzylidene)cyclohexan-1-one 7.7% residual activity at 0.1 mM Homo sapiens
2,6-bis(3-chloro-5-fluoro-4-hydroxybenzylidene)cyclohexan-1-one 41.1% residual activity at 0.1 mM Homo sapiens
2,6-bis(4-hydroxy-3-iodobenzylidene)cyclohexan-1-one 5.8% residual activity at 0.1 mM Homo sapiens
2,6-bis[(6-hydroxy-1,1'-biphenyl-3-yl)methylene]cyclohexan-1-one 92.2% residual activity at 0.1 mM Homo sapiens
4,4'-(2-hydroxycyclohexane-1,3-diylidene)bis(methanylylidene)-bis(2-bromophenol) 12.5% residual activity at 0.1 mM Homo sapiens
5,5'-[(5-carboxy-2-oxocyclohexane-1,3-diylidene)bis(methanylylidene)]bis(2-hydroxybenzoic acid) 70.1% residual activity at 0.1 mM Homo sapiens
anacardic acid
-
 Homo sapiens
curcumin
-
 Homo sapiens
epigallocatechin-3-gallate
-
 Homo sapiens
garcinol
-
 Homo sapiens
Lys-CoA
-
 Homo sapiens
Plumbagin
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
acetyl-CoA + [histone H3]-L-lysine20 Homo sapiens
-
 CoA + [histone H3]-N6-acetyl-L-lysine20
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q09472
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-CoA + [histone H3]-L-lysine20
-
 Homo sapiens CoA + [histone H3]-N6-acetyl-L-lysine20
-
 ?

Synonyms

Synonyms Comment Organism
HAT
-
 Homo sapiens
p300
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0023
-
 at pH 8.0 and 30°C Homo sapiens (2E,6E)-2,6-bis[(3,5-dibromo-4-hydroxyphenyl)methylidene]cyclohexan-1-one
0.0081
-
 at pH 8.0 and 30°C Homo sapiens 2,6-bis(4-hydroxy-3-iodobenzylidene)cyclohexan-1-one
0.0268
-
 at pH 8.0 and 30°C Homo sapiens (2E,6E)-2,6-bis[(4-hydroxy-3-methylphenyl)methylidene]cyclohexan-1-one
0.0309
-
 at pH 8.0 and 30°C Homo sapiens 2,6-bis(3-bromo-4-hydroxybenzylidene)cyclohexanone
0.035
-
 at pH 8.0 and 30°C Homo sapiens (3Z,5Z)-3,5-bis[(3-bromo-4-hydroxyphenyl)methylidene]thian-4-one
0.0389
-
 at pH 8.0 and 30°C Homo sapiens (2E,6E)-2,6-bis[(3-fluoro-4-hydroxyphenyl)methylidene]cyclohexan-1-one
0.0455
-
 at pH 8.0 and 30°C Homo sapiens 2,6-bis(3-chloro-4-hydroxybenzylidene)cyclohexan-1-one