Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-(3,4-dichlorobenzyl)-5-(morpholin-4-ylsulfonyl)-1H-indole-2,3-dione | slight inhibition | Homo sapiens | |
1-benzyl-5-(thiomorpholin-4-ylsulfonyl)-1H-indole-2,3-dione | - |
Homo sapiens | |
5-(azetidin-1-ylsulfonyl)-1-benzyl-1H-indole-2,3-dione | - |
Homo sapiens | |
5-(morpholin-4-ylsulfonyl)-1H-indole-2,3-dione | slight inhibition | Homo sapiens | |
Ac-Val-Glu-Ile-Asp-CHO | - |
Homo sapiens | |
additional information | development and synthesis of nonpeptidic caspase-6 inhibitors, overview. No inhibition of caspase-6 by Ac-IETD-CHO, Ac-YVAD-CHO, and Ac-DEVD-CHO | Homo sapiens | |
sulfonamide isatin Michael acceptors | small molecule inhibitors of caspase-6 | Homo sapiens | |
[1-(3,4-dichlorobenzyl)-2-oxo-5-(piperidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens | |
[1-(3,4-dichlorobenzyl)-2-oxo-5-(pyrrolidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens | |
[1-(3,4-dichlorobenzyl)-2-oxo-5-(thiomorpholin-4-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens | |
[1-(3,4-dichlorobenzyl)-5-(morpholin-4-ylsulfonyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens | |
[1-(4-methoxybenzyl)-2-oxo-5-(piperidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens | |
[1-(4-methoxybenzyl)-2-oxo-5-(pyrrolidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens | |
[1-(4-methoxybenzyl)-2-oxo-5-(thiomorpholin-4-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens | |
[1-(4-methoxybenzyl)-5-(morpholin-4-ylsulfonyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens | |
[1-benzyl-2-oxo-5-(piperidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens | |
[1-benzyl-2-oxo-5-(pyrrolidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens | |
[1-benzyl-2-oxo-5-(thiomorpholin-4-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens | |
[1-benzyl-5-(morpholin-4-ylsulfonyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens | |
[5-(azetidin-1-ylsulfonyl)-1-(3,4-dichlorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens | |
[5-(azetidin-1-ylsulfonyl)-1-(4-methoxybenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens | |
[5-(azetidin-1-ylsulfonyl)-1-benzyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
huntingtin + H2O | Homo sapiens | a key step in the onset of Huntingtons disease is the caspase-6 mediated cleavage of the protein huntingtin into toxic fragments | huntingtin peptide fragments | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
huntingtin + H2O | - |
Homo sapiens | huntingtin peptide fragments | - |
? | |
huntingtin + H2O | a key step in the onset of Huntingtons disease is the caspase-6 mediated cleavage of the protein huntingtin into toxic fragments | Homo sapiens | huntingtin peptide fragments | - |
? |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000151 | - |
- |
Homo sapiens | [1-benzyl-2-oxo-5-(thiomorpholin-4-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.000156 | - |
- |
Homo sapiens | [5-(azetidin-1-ylsulfonyl)-1-benzyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.000188 | - |
- |
Homo sapiens | [1-(4-methoxybenzyl)-2-oxo-5-(thiomorpholin-4-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.000197 | - |
- |
Homo sapiens | [5-(azetidin-1-ylsulfonyl)-1-(4-methoxybenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.00023 | - |
- |
Homo sapiens | [1-(3,4-dichlorobenzyl)-2-oxo-5-(thiomorpholin-4-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.000241 | - |
- |
Homo sapiens | [1-benzyl-2-oxo-5-(pyrrolidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.00028 | - |
- |
Homo sapiens | [5-(azetidin-1-ylsulfonyl)-1-(3,4-dichlorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.000325 | - |
- |
Homo sapiens | [1-benzyl-2-oxo-5-(piperidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.000358 | - |
- |
Homo sapiens | [1-(4-methoxybenzyl)-2-oxo-5-(pyrrolidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.000425 | - |
- |
Homo sapiens | [1-benzyl-5-(morpholin-4-ylsulfonyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.000453 | - |
- |
Homo sapiens | [1-(4-methoxybenzyl)-5-(morpholin-4-ylsulfonyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.000468 | - |
- |
Homo sapiens | [1-(3,4-dichlorobenzyl)-2-oxo-5-(pyrrolidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.000545 | - |
- |
Homo sapiens | [1-(4-methoxybenzyl)-2-oxo-5-(piperidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.000568 | - |
- |
Homo sapiens | [1-(3,4-dichlorobenzyl)-2-oxo-5-(piperidin-1-ylsulfonyl)-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.000592 | - |
- |
Homo sapiens | [1-(3,4-dichlorobenzyl)-5-(morpholin-4-ylsulfonyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]propanedinitrile | |
0.00128 | - |
- |
Homo sapiens | 1-benzyl-5-(thiomorpholin-4-ylsulfonyl)-1H-indole-2,3-dione | |
0.0015 | - |
above | Homo sapiens | 1-(3,4-dichlorobenzyl)-5-(morpholin-4-ylsulfonyl)-1H-indole-2,3-dione | |
0.002 | - |
above | Homo sapiens | 5-(morpholin-4-ylsulfonyl)-1H-indole-2,3-dione | |
0.00983 | - |
- |
Homo sapiens | 5-(azetidin-1-ylsulfonyl)-1-benzyl-1H-indole-2,3-dione |