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Literature summary for 3.4.22.56 extracted from

  • Lee, D.; Long, S.A.; Adams, J.L.; Chan, G.; et al.
    Potent and selective nonpeptide inhibitors of caspases 3 and 7 inhibit apoptosis and maintain cell functionality (2000), J. Biol. Chem., 275, 16007-16014.
    View publication on PubMed
Search for more literature for 3.4.22.56

Inhibitors

Inhibitors Comment Organism Structure
(R)-5-[1-(2-methoxymethyl)pyrrolidinylsulfonyl]isatin IC50: 0.018 mM Homo sapiens
(R)-5-[1-[2-(anilinomethyl)pyrrolidinyl]sulfonyl]isatin IC50: 0.0055 mM Homo sapiens
(S)-(+)-5-[1-[2-(thiophenoxymethyl)pyrrolidinyl]sulfonyl]isatin IC50: 44 nM Homo sapiens
(S)-1-(4-pyridinylmethyl)-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonal]isatin IC50: 4.2 nM Homo sapiens
(S)-1-(carboxymethyl)-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin IC50: 170 nM Homo sapiens
(S)-1-(cyclohexylmethyl)-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonal]isatin IC50: 5.2 nM Homo sapiens
(S)-1-allyl-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin IC50: 4.6 nM Homo sapiens
(S)-1-benzyl-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin IC50: 2.5 nM Homo sapiens
(S)-1-methyl-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin IC50: 30 nM Homo sapiens
(S)-1-[(tert-butyloxycarbonyl)methyl]-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin IC50: 3.1 nM Homo sapiens
(S)-5-[1-(2-methoxymethyl)pyrrolidinylsulfonyl]isatin IC50: 120 nM Homo sapiens
(S)-5-[1-[(2-methoxycarbonyl)pyrrolidinyl]sulfonyl]isatin IC50: 170 nM Homo sapiens
(S)-5-[1-[(2-tert-butoxycarbonyl)pyrrolidinyl]sulfonyl]isatin IC50: 70 nM Homo sapiens
(S)-5-[1-[2-(anilinomethyl)pyrrolidinyl]sulfonyl]isatin IC50: 31 nM Homo sapiens
(S)-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin IC50: 44 nM Homo sapiens
(S)-5-[1-[2-(phenylaminocarbonyl)pyrrolidinyl]sulfonyl]isatin IC50: 140 nM Homo sapiens
(S)-5-[1-[[2-(dimethylamino)carbonyl]pyrrolidinyl]sulfonyl]isatin IC50: 410 nM Homo sapiens
5-[1-(azetidinyl)sulfonyl]isatin IC50: 170 nM Homo sapiens
5-[1-(hexamethyleneimino)sulfonyl]isatin IC50: 0.0019 mM Homo sapiens
5-[1-(piperidinyl)sulfonyl]isatin IC50: 0.0022 mM Homo sapiens
5-[1-(pyrrolidinyl)sulfonyl]isatin IC50: 0.0028 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P42574
-
-

Source Tissue

Source Tissue Comment Organism Textmining
chondrocyte
-
 Homo sapiens
-
JURKAT cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-DEVD-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens acetyl-DEVD + 7-amino-4-methylcoumarin
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000012
-
 (S)-1-benzyl-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin pH 7.5, 30°C Homo sapiens
0.000015
-
 (S)-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin pH 7.5, 30°C Homo sapiens
0.000019
-
 (S)-1-[(tert-butyloxycarbonyl)methyl]-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin pH 7.5, 30°C Homo sapiens
0.00006
-
 (S)-5-[1-(2-methoxymethyl)pyrrolidinylsulfonyl]isatin pH 7.5, 30°C Homo sapiens
0.0014
-
 5-[1-(pyrrolidinyl)sulfonyl]isatin pH 7.5, 30°C Homo sapiens
0.012
-
 (R)-5-[1-[2-(anilinomethyl)pyrrolidinyl]sulfonyl]isatin pH 7.5, 30°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000025
-
 IC50: 2.5 nM Homo sapiens (S)-1-benzyl-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin
0.0000031
-
 IC50: 3.1 nM Homo sapiens (S)-1-[(tert-butyloxycarbonyl)methyl]-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin
0.0000042
-
 IC50: 4.2 nM Homo sapiens (S)-1-(4-pyridinylmethyl)-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonal]isatin
0.0000046
-
 IC50: 4.6 nM Homo sapiens (S)-1-allyl-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin
0.0000052
-
 IC50: 5.2 nM Homo sapiens (S)-1-(cyclohexylmethyl)-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonal]isatin
0.00003
-
 IC50: 30 nM Homo sapiens (S)-1-methyl-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin
0.000031
-
 IC50: 31 nM Homo sapiens (S)-5-[1-[2-(anilinomethyl)pyrrolidinyl]sulfonyl]isatin
0.000044
-
 IC50: 44 nM Homo sapiens (S)-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin
0.000044
-
 IC50: 44 nM Homo sapiens (S)-(+)-5-[1-[2-(thiophenoxymethyl)pyrrolidinyl]sulfonyl]isatin
0.00007
-
 IC50: 70 nM Homo sapiens (S)-5-[1-[(2-tert-butoxycarbonyl)pyrrolidinyl]sulfonyl]isatin
0.00012
-
 IC50: 120 nM Homo sapiens (S)-5-[1-(2-methoxymethyl)pyrrolidinylsulfonyl]isatin
0.00014
-
 IC50: 140 nM Homo sapiens (S)-5-[1-[2-(phenylaminocarbonyl)pyrrolidinyl]sulfonyl]isatin
0.00017
-
 IC50: 170 nM Homo sapiens (S)-1-(carboxymethyl)-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin
0.00017
-
 IC50: 170 nM Homo sapiens (S)-5-[1-[(2-methoxycarbonyl)pyrrolidinyl]sulfonyl]isatin
0.00017
-
 IC50: 170 nM Homo sapiens 5-[1-(azetidinyl)sulfonyl]isatin
0.00041
-
 IC50: 410 nM Homo sapiens (S)-5-[1-[[2-(dimethylamino)carbonyl]pyrrolidinyl]sulfonyl]isatin
0.0019
-
 IC50: 0.0019 mM Homo sapiens 5-[1-(hexamethyleneimino)sulfonyl]isatin
0.0022
-
 IC50: 0.0022 mM Homo sapiens 5-[1-(piperidinyl)sulfonyl]isatin
0.0028
-
 IC50: 0.0028 mM Homo sapiens 5-[1-(pyrrolidinyl)sulfonyl]isatin
0.0055
-
 IC50: 0.0055 mM Homo sapiens (R)-5-[1-[2-(anilinomethyl)pyrrolidinyl]sulfonyl]isatin
0.018
-
 IC50: 0.018 mM Homo sapiens (R)-5-[1-(2-methoxymethyl)pyrrolidinylsulfonyl]isatin