Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(S)-1-(11,11-difluoroundecyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-(2-fluoroallyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-(2-fluoroethyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-(3-chloro-2-hydroxypropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-(3-chloropropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-(3-fluorobutyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-(3-fluoropropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-(3-hydroxypropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-(4-fluorobutyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-(4-hydroxybutyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-butyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-ethyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-methyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-propyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-isatin | - |
Homo sapiens | |
(S)-1-[3-(3-fluoropropoxy)propyl]-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-[3-(3-hydroxypropoxy)propyl]-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-1-[3-[3-(2-fluoroethoxy)propoxy]propyl]-5-[1-(2-methoxymethylpyrrolidinyl)-sulfonyl]isatin | - |
Homo sapiens | |
(S)-3,3-difluoro-1-(3-fluoropropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]indolin-2-one | - |
Homo sapiens | |
(S)-3,3-difluoro-1-propyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]indolin-2-one | - |
Homo sapiens | |
(S)-3,5-bis-trifluoromethylbenzyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-3-[3-[5-(1-(2-methoxymethylpyrrolidinyl)sulfonyl)-2,3-dioxoindolin-1-yl]propoxy]-propyl methanesulfonate | - |
Homo sapiens | |
(S)-3-[5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-2,3-dioxoindolin-1-yl]propanoic acid | - |
Homo sapiens | |
(S)-3-[5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-2,3-dioxoindolin-1-yl]propyl methanesulfonate | - |
Homo sapiens | |
(S)-4-fluorobenzyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-4-trifluoromethylbenzyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
(S)-4-[5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-2,3-dioxoindolin-1-yl]butyl 4-methyl-benzenesulfonate | - |
Homo sapiens | |
(S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-1-(3,3,3-trifluoropropyl)isatin | - |
Homo sapiens | |
(S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-1-(3,4,4-trifluorobut-3-enyl)isatin | - |
Homo sapiens | |
(S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-1-(4,4,4-trifluorobutyl)isatin | - |
Homo sapiens | |
6-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1H-indole-2,3-dione | - |
Homo sapiens | |
additional information | N-propyl- and N-butyl isatins, as well as the corresponding terminal alcohols and regioisomeric fluorobutyl derivatives are excellent inhibitors, fluorinated N-benzyl isatins as well as trifluoroalkyl and difluoroalkyl derivatives are moderate inhibitors, while isatins bearing different alkylether groups at N-1 are very weak or not active as inhibitors of caspases-3, inhibitory potencies and structure-activity relationships, overview | Homo sapiens | |
N-butyl-(S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens | |
N-propyl-(S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | - |
Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
DEVD-7-amido-4-fluoromethylcoumarin + H2O | - |
Homo sapiens | DEVD + 7-amino-4-fluoromethylcoumarin | - |
? |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000024 | - |
37°C | Homo sapiens | (S)-1-methyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.0000053 | - |
37°C | Homo sapiens | (S)-1-propyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-isatin | |
0.0000133 | - |
37°C | Homo sapiens | (S)-1-(3-chloro-2-hydroxypropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.000025 | - |
37°C | Homo sapiens | (S)-1-(3-fluorobutyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.000029 | - |
37°C | Homo sapiens | (S)-1-butyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.00003 | - |
37°C | Homo sapiens | (S)-1-(4-hydroxybutyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.000041 | - |
37°C | Homo sapiens | (S)-1-(4-fluorobutyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.000043 | - |
37°C | Homo sapiens | (S)-3,5-bis-trifluoromethylbenzyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.000056 | - |
37°C | Homo sapiens | (S)-4-[5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-2,3-dioxoindolin-1-yl]butyl 4-methyl-benzenesulfonate | |
0.000066 | - |
37°C | Homo sapiens | (S)-1-(11,11-difluoroundecyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.000078 | - |
37°C | Homo sapiens | (S)-1-(3-hydroxypropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.000082 | - |
37°C | Homo sapiens | (S)-4-trifluoromethylbenzyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.000083 | - |
37°C | Homo sapiens | (S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-1-(3,4,4-trifluorobut-3-enyl)isatin | |
0.00009 | - |
37°C | Homo sapiens | (S)-1-(3-chloropropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.00012 | - |
37°C | Homo sapiens | 6-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1H-indole-2,3-dione | |
0.000183 | - |
37°C | Homo sapiens | (S)-1-ethyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.000187 | - |
37°C | Homo sapiens | (S)-3-[5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-2,3-dioxoindolin-1-yl]propanoic acid | |
0.000191 | - |
37°C | Homo sapiens | (S)-4-fluorobenzyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.000213 | - |
37°C | Homo sapiens | (S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-1-(4,4,4-trifluorobutyl)isatin | |
0.00023 | - |
37°C | Homo sapiens | (S)-3-[5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-2,3-dioxoindolin-1-yl]propyl methanesulfonate | |
0.000359 | - |
37°C | Homo sapiens | (S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-1-(3,3,3-trifluoropropyl)isatin | |
0.0005 | - |
37°C | Homo sapiens | (S)-1-(2-fluoroallyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.00184 | - |
37°C | Homo sapiens | (S)-1-(2-fluoroethyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.00512 | - |
37°C | Homo sapiens | (S)-1-(3-fluoropropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.0068 | - |
37°C | Homo sapiens | (S)-3,3-difluoro-1-(3-fluoropropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]indolin-2-one | |
0.00943 | - |
37°C | Homo sapiens | (S)-1-[3-[3-(2-fluoroethoxy)propoxy]propyl]-5-[1-(2-methoxymethylpyrrolidinyl)-sulfonyl]isatin | |
0.0609 | - |
37°C | Homo sapiens | (S)-1-[3-(3-hydroxypropoxy)propyl]-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.1 | - |
above, 37°C | Homo sapiens | (S)-1-[3-(3-fluoropropoxy)propyl]-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin | |
0.1 | - |
above, 37°C | Homo sapiens | (S)-3,3-difluoro-1-propyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]indolin-2-one | |
0.1 | - |
above, 37°C | Homo sapiens | (S)-3-[3-[5-(1-(2-methoxymethylpyrrolidinyl)sulfonyl)-2,3-dioxoindolin-1-yl]propoxy]-propyl methanesulfonate |