Application | Comment | Organism |
---|---|---|
drug development | Cat S is an attractive therapeutic target and selective Cat S inhibitors may also modulate a number of other diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, asthma, atherosclerosis and neuropathic pain | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide | - |
Homo sapiens | |
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide | - |
Homo sapiens | |
2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide | - |
Homo sapiens | |
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide | - |
Homo sapiens | |
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens | |
2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide | - |
Homo sapiens | |
2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide | - |
Homo sapiens | |
2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens | |
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens | |
2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens | |
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens | |
2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens | |
2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens | |
2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens | |
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile | - |
Homo sapiens | |
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile | - |
Homo sapiens | |
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens | |
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens | |
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens | |
N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens | |
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens | |
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens | |
N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | - |
Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
lysosome | - |
Homo sapiens | 5764 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | major role of Cat S in these cells is the processing of the major histocompatibility complex class II associated invariant chain, which is essential for the normal functioning of the immune system, Cat S is largely responsible for the last proteolytic cleavage step of the invariant chain that produces class II-associated leupeptin induced peptide | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P25774 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
B-lymphocyte | - |
Homo sapiens | - |
culture condition:antigen-presenting cell | - |
Homo sapiens | - |
dendritic cell | - |
Homo sapiens | - |
macrophage | - |
Homo sapiens | - |
spleen | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
L-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O | - |
Homo sapiens | L-Leu-Leu-Arg + 7-amino-4-methylcoumarin | - |
? | |
additional information | major role of Cat S in these cells is the processing of the major histocompatibility complex class II associated invariant chain, which is essential for the normal functioning of the immune system, Cat S is largely responsible for the last proteolytic cleavage step of the invariant chain that produces class II-associated leupeptin induced peptide | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
Cat S | - |
Homo sapiens |
cathepsin S | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
additional information | - |
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
additional information | - |
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
additional information | - |
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
additional information | - |
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
0.000001 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
0.000002 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
0.000002 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile | |
0.000002 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
0.000003 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
0.000004 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
0.000006 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
0.000007 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
0.000014 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide | |
0.000015 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
0.000021 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
0.000022 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide | |
0.000022 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile | |
0.000022 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide | |
0.000023 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
0.000024 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide | |
0.000032 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide | |
0.000093 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide | |
0.00013 | - |
inhibition is determined by a fluorometric assay with recombinant Cat S | Homo sapiens | 2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide |