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Literature summary extracted from

  • Wu, L.; Lu, M.; Yan, Z.; Tang, X.; Sun, B.; Liu, W.; Zhou, H.; Yang, C.
    1,2-benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors (2014), Bioorg. Med. Chem., 22, 2416-2426.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.56 2-(3-oxo-1,2-benzothiazol-2(3H)-yl)-N-[4-(1H-pyrrol-1-yl)phenyl]acetamide
-
 Homo sapiens
3.4.22.56 2-(3-oxo-1,2-benzothiazol-2(3H)-yl)-N-[4-(piperidin-1-yl)phenyl]acetamide
-
 Homo sapiens
3.4.22.56 2-(3-oxo-1,2-benzothiazol-2(3H)-yl)-N-[4-(pyridin-2-yl)phenyl]acetamide
-
 Homo sapiens
3.4.22.56 3-oxo-N-(2-phenylethyl)-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 3-oxo-N-(3-phenylpropyl)-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 3-oxo-N-[2-(pyridin-2-yl)ethyl]-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 3-oxo-N-[2-(thiophen-2-yl)ethyl]-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 3-oxo-N-[4-(1H-pyrrol-1-yl)phenyl]-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 3-oxo-N-[4-(piperidin-1-yl)phenyl]-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 3-oxo-N-[4-(piperidin-1-ylsulfonyl)phenyl]-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 3-oxo-N-[4-(pyridin-2-yl)phenyl]-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 3-oxo-N-[4-(pyrrolidin-1-yl)phenyl]-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 3-oxo-N-[4-(pyrrolidin-1-ylsulfonyl)phenyl]-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 additional information 1,2-benzisothiazol-3(2H)-one, lacks caspase-3 inhibitory activity Homo sapiens
3.4.22.56 N-(4-benzoylphenyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 N-(5-methylpyridin-2-yl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 N-(furan-2-ylmethyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 N-benzyl-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 N-[2-(4-methylpiperazin-1-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 N-[2-(morpholin-4-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 N-[3-(4-methylpiperazin-1-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 N-[3-(morpholin-4-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 N-[4-(1,3-dioxolan-2-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 N-[4-(4-methylpiperazin-1-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 N-[4-(morpholin-4-yl)benzyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 N-[4-(morpholin-4-yl)phenyl]-2-(3-oxo-1,2-benzothiazol-2(3H)-yl)acetamide
-
 Homo sapiens
3.4.22.56 N-[4-(morpholin-4-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 N-[4-(morpholin-4-ylsulfonyl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens
3.4.22.56 N-[4-[(4-methylpiperazin-1-yl)sulfonyl]phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.56 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.22.56 N-acetyl-LDEVD-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens N-acetyl-LDEVD + 7-amino-4-methylcoumarin
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.22.56 CASP-3
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.22.56 0.00000115
-
 at pH 7.5, temperature not specified in the publication Homo sapiens N-[4-(morpholin-4-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.0000221
-
 at pH 7.5, temperature not specified in the publication Homo sapiens 3-oxo-N-[4-(pyridin-2-yl)phenyl]-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.000031
-
 at pH 7.5, temperature not specified in the publication Homo sapiens 3-oxo-N-(2-phenylethyl)-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.00003105
-
 at pH 7.5, temperature not specified in the publication Homo sapiens 3-oxo-N-[2-(thiophen-2-yl)ethyl]-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.00004153
-
 at pH 7.5, temperature not specified in the publication Homo sapiens N-benzyl-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.00004904
-
 at pH 7.5, temperature not specified in the publication Homo sapiens 3-oxo-N-(3-phenylpropyl)-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.00004939
-
 at pH 7.5, temperature not specified in the publication Homo sapiens 3-oxo-N-[2-(pyridin-2-yl)ethyl]-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.0000555
-
 at pH 7.5, temperature not specified in the publication Homo sapiens N-[3-(morpholin-4-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.00005685
-
 at pH 7.5, temperature not specified in the publication Homo sapiens N-[4-(morpholin-4-yl)benzyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.0000606
-
 at pH 7.5, temperature not specified in the publication Homo sapiens N-[4-[(4-methylpiperazin-1-yl)sulfonyl]phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.00006201
-
 at pH 7.5, temperature not specified in the publication Homo sapiens N-[4-(4-methylpiperazin-1-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.00008055
-
 at pH 7.5, temperature not specified in the publication Homo sapiens N-(furan-2-ylmethyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.00009792
-
 at pH 7.5, temperature not specified in the publication Homo sapiens 3-oxo-N-[4-(piperidin-1-yl)phenyl]-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.0001808
-
 at pH 7.5, temperature not specified in the publication Homo sapiens N-[3-(4-methylpiperazin-1-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.0002697
-
 at pH 7.5, temperature not specified in the publication Homo sapiens N-[2-(morpholin-4-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.0004307
-
 at pH 7.5, temperature not specified in the publication Homo sapiens N-(4-benzoylphenyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.000501
-
 at pH 7.5, temperature not specified in the publication Homo sapiens 2-(3-oxo-1,2-benzothiazol-2(3H)-yl)-N-[4-(pyridin-2-yl)phenyl]acetamide
3.4.22.56 0.000729
-
 at pH 7.5, temperature not specified in the publication Homo sapiens 2-(3-oxo-1,2-benzothiazol-2(3H)-yl)-N-[4-(1H-pyrrol-1-yl)phenyl]acetamide
3.4.22.56 0.0007834
-
 at pH 7.5, temperature not specified in the publication Homo sapiens N-[4-(morpholin-4-ylsulfonyl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.01356
-
 at pH 7.5, temperature not specified in the publication Homo sapiens N-[2-(4-methylpiperazin-1-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
3.4.22.56 0.04674
-
 at pH 7.5, temperature not specified in the publication Homo sapiens N-(5-methylpyridin-2-yl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide