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Literature summary for 2.3.1.48 extracted from

  • Gorsuch, S.; Bavetsias, V.; Rowlands, M.G.; Aherne, G.W.; Workman, P.; Jarman, M.; McDonald, E.
    Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs) (2009), Bioorg. Med. Chem., 17, 467-474.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2,5-diphenylisothiazol-3(2H)-one
-
Homo sapiens
2-(2-pyridyl)-isothiazol-3(2H)-one
-
Homo sapiens
2-(3-pyridyl)-isothiazol-3(2H)-one
-
Homo sapiens
2-(4-dimethylaminoaniline)-isothiazol-3(2H)-one
-
Homo sapiens
2-(4-morpholinoaniline)-isothiazol-3(2H)-one
-
Homo sapiens
2-(4-pyridyl)-isothiazol-3(2H)-one
-
Homo sapiens
2-(phenyl)-isothiazolo[5,4-b]pyridin-3(2H)-one
-
Homo sapiens
2-phenyl-5-(trityloxymethyl)isothiazol-3(2H)-one
-
Homo sapiens
2-phenylisothiazol-3(2H)-one
-
Homo sapiens
3-(Z)-(benzylsulfanyl)propenoic acid
-
Homo sapiens
3-(Z)-(benzylsulfinyl)-2-N-(4-dimethylaminoanilino)-propenamide
-
Homo sapiens
3-(Z)-(benzylsulfinyl)-2-N-(4-morpholinoanilino)-propenamide
-
Homo sapiens
3-(Z)-(benzylsulfinyl)-N-(2-pyridyl)propenamide
-
Homo sapiens
3-(Z)-(benzylsulfinyl)-N-(3-pyridyl)propenamide
-
Homo sapiens
3-(Z)-(benzylsulfinyl)-N-(4-pyridyl)propenamide
-
Homo sapiens
3-Z-benzylsulfanyl-4-trityloxy-but-2-enoic acid phenylamide
-
Homo sapiens
3-Z-benzylsulfinyl-4-trityloxy-but-2-enoic acid phenylamide
-
Homo sapiens
4-azidomethyl-2-phenyl-isothiazol-3(2H)-one
-
Homo sapiens
4-bromomethyl-2-phenylisothiazol-3(2H)-one
-
Homo sapiens
4-methoxymethyl-2-phenyl-isothiazol-3(2H)-one
-
Homo sapiens
4-methyl-2-phenylisothiazol-3(2H)-one
-
Homo sapiens
4-methyl-5-methoxy-2-phenyl-isothiazol-3(2H)-one
-
Homo sapiens
4-trityloxy-but-2-ynoic acid phenylamide
-
Homo sapiens
5-acetoxymethyl-2-phenylisothiazol-3(2H)-one
-
Homo sapiens
5-azidomethyl-2-phenylisothiazol-3(2H)-one
-
Homo sapiens
5-chloro-4-methyl-2-phenylisothiazol-3(2H)-one
-
Homo sapiens
5-hydroxymethyl-2-phenylisothiazol-3(2H)-one
-
Homo sapiens
5-methyl-2-phenylisothiazol-3(2H)-one
-
Homo sapiens
5-phenylureidomethyl-2-phenylisothiazol-3(2H)-one
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
HAT
-
Homo sapiens
p300
-
Homo sapiens
PCAF
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0015
-
2-(4-pyridyl)-isothiazol-3(2H)-one PCAF Homo sapiens
0.003
-
2-(4-pyridyl)-isothiazol-3(2H)-one p300 Homo sapiens
0.0054
-
2-(4-dimethylaminoaniline)-isothiazol-3(2H)-one PCAF Homo sapiens
0.0065
-
2-(3-pyridyl)-isothiazol-3(2H)-one PCAF Homo sapiens
0.0075
-
2-(4-morpholinoaniline)-isothiazol-3(2H)-one PCAF Homo sapiens
0.0099
-
2-(4-morpholinoaniline)-isothiazol-3(2H)-one p300 Homo sapiens
0.0144
-
2-(3-pyridyl)-isothiazol-3(2H)-one p300 Homo sapiens
0.019
-
2-(2-pyridyl)-isothiazol-3(2H)-one PCAF Homo sapiens
0.0198
-
2,5-diphenylisothiazol-3(2H)-one PCAF Homo sapiens
0.023
-
2-phenylisothiazol-3(2H)-one p300 Homo sapiens
0.028
-
2-(2-pyridyl)-isothiazol-3(2H)-one p300 Homo sapiens
0.028
-
2-phenylisothiazol-3(2H)-one PCAF Homo sapiens
0.032
-
4-methyl-2-phenylisothiazol-3(2H)-one PCAF Homo sapiens
0.0427
-
4-azidomethyl-2-phenyl-isothiazol-3(2H)-one PCAF Homo sapiens
0.058
-
5-azidomethyl-2-phenylisothiazol-3(2H)-one PCAF Homo sapiens
0.102
-
4-methoxymethyl-2-phenyl-isothiazol-3(2H)-one PCAF Homo sapiens
0.109
-
5-hydroxymethyl-2-phenylisothiazol-3(2H)-one PCAF Homo sapiens
0.162
-
5-acetoxymethyl-2-phenylisothiazol-3(2H)-one PCAF Homo sapiens
0.2
-
5-chloro-4-methyl-2-phenylisothiazol-3(2H)-one above, PCAF Homo sapiens
0.2
-
4-methyl-5-methoxy-2-phenyl-isothiazol-3(2H)-one above, PCAF Homo sapiens
0.2
-
5-methyl-2-phenylisothiazol-3(2H)-one above, PCAF Homo sapiens
0.2
-
5-phenylureidomethyl-2-phenylisothiazol-3(2H)-one above, PCAF Homo sapiens