Inhibitors | Comment | Organism | Structure |
---|---|---|---|
additional information | design, synthesis, and structure-activity relationship of a series of activated protein C inhibitors with selectivity against thrombin by a basic and/or aromatic functionality for binding to the S2 pocket, for the treatment of haemophilia | Homo sapiens | |
N-(2-carboxyethyl)-3-cyclohexyl-L-alanyl-N-(4-carbamimidoylbenzyl)argininamide | - |
Homo sapiens | |
N-(4-carbamimidoylbenzyl)-2-[(3-cyclohexyl-L-alanyl)amino]-4-(piperidin-4-yl)butanamide | - |
Homo sapiens | |
N-(carboxymethyl)-3-cyclohexyl-D-alanyl-4-(aminomethyl)-N-(4-carbamimidoylbenzyl)phenylalaninamide | - |
Homo sapiens | |
N-(carboxymethyl)-3-cyclohexyl-D-alanyl-4-amino-N-(4-carbamimidoylbenzyl)-D-phenylalaninamide | - |
Homo sapiens | |
N-(carboxymethyl)-3-cyclohexyl-D-alanyl-N-(4-carbamimidoylbenzyl)-4-cyanophenylalaninamide | - |
Homo sapiens | |
N-(carboxymethyl)-3-cyclohexyl-D-alanyl-N-(4-carbamimidoylbenzyl)-D-phenylalaninamide | - |
Homo sapiens | |
N-(carboxymethyl)-3-cyclohexyl-D-alanyl-N-(4-carbamimidoylbenzyl)-D-tyrosinamide | - |
Homo sapiens | |
N-(carboxymethyl)-3-cyclohexyl-L-alanyl-N-(4-carbamimidoylbenzyl)-3-piperidin-4-ylalaninamide | - |
Homo sapiens | |
N-(carboxymethyl)-3-cyclohexyl-L-alanyl-N-(4-carbamimidoylbenzyl)-3-pyrrolidin-2-yl-D-alaninamide | - |
Homo sapiens | |
N-(carboxymethyl)-3-cyclohexyl-L-alanyl-N-(4-carbamimidoylbenzyl)-3-pyrrolidin-2-yl-L-alaninamide | - |
Homo sapiens | |
N-(carboxymethyl)-3-cyclohexyl-L-alanyl-N-(4-carbamimidoylbenzyl)argininamide | - |
Homo sapiens | |
N-[(1S)-2-([1-[(4-carbamimidoylbenzyl)amino]-1-oxo-4-(piperidin-4-yl)butan-2-yl]amino)-1-cyclohexyl-2-oxoethyl]glycine | - |
Homo sapiens | |
N-[(1S)-2-([2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]amino)-1-cyclohexyl-2-oxoethyl]glycine | the compound shows a 21fold selectivity for activated protein C over thrombin | Homo sapiens | |
N-[(2S)-1-([1-[(4-carbamimidoylbenzyl)amino]-1-oxo-4-(piperidin-4-yl)butan-2-yl]amino)-3-cyclohexyl-1-oxopropan-2-yl]glycine | the compound shows a 23fold selectivity for activated protein C over thrombin | Homo sapiens | |
N-[(2S)-1-[[(1S)-2-[(4-carbamimidoylbenzyl)amino]-2-oxo-1-(piperidin-4-yl)ethyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]glycine | - |
Homo sapiens | |
N2-[(2S)-2-amino-2-cyclohexylacetyl]-N-(4-carbamimidoylbenzyl)argininamide | - |
Homo sapiens | |
[[(2R)-1-[[(2R)-1-[(4-carbamimidoylbenzyl)amino]-3-(naphthalen-1-yl)-1-oxopropan-2-yl]amino]-3-cyclohexyl-1-oxopropan-2-yl]amino]acetic acid | non-preferred name | Homo sapiens | |
[[(2R)-1-[[(2R)-1-[(4-carbamimidoylbenzyl)amino]-3-(naphthalen-2-yl)-1-oxopropan-2-yl]amino]-3-cyclohexyl-1-oxopropan-2-yl]amino]acetic acid | non-preferred name | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Synonyms | Comment | Organism |
---|---|---|
Activated protein C | - |
Homo sapiens |
APC | - |
Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00013 | - |
pH 7.4, 37°C | Homo sapiens | N-(carboxymethyl)-3-cyclohexyl-D-alanyl-4-amino-N-(4-carbamimidoylbenzyl)-D-phenylalaninamide | |
0.00026 | - |
pH 7.4, 37°C | Homo sapiens | N-(carboxymethyl)-3-cyclohexyl-D-alanyl-N-(4-carbamimidoylbenzyl)-D-tyrosinamide | |
0.00047 | - |
pH 7.4, 37°C | Homo sapiens | N-(carboxymethyl)-3-cyclohexyl-L-alanyl-N-(4-carbamimidoylbenzyl)argininamide | |
0.00067 | - |
pH 7.4, 37°C | Homo sapiens | N-(carboxymethyl)-3-cyclohexyl-D-alanyl-N-(4-carbamimidoylbenzyl)-D-phenylalaninamide | |
0.00098 | - |
pH 7.4, 37°C | Homo sapiens | [[(2R)-1-[[(2R)-1-[(4-carbamimidoylbenzyl)amino]-3-(naphthalen-2-yl)-1-oxopropan-2-yl]amino]-3-cyclohexyl-1-oxopropan-2-yl]amino]acetic acid | |
0.0011 | - |
pH 7.4, 37°C | Homo sapiens | [[(2R)-1-[[(2R)-1-[(4-carbamimidoylbenzyl)amino]-3-(naphthalen-1-yl)-1-oxopropan-2-yl]amino]-3-cyclohexyl-1-oxopropan-2-yl]amino]acetic acid | |
0.0011 | - |
pH 7.4, 37°C | Homo sapiens | N-(carboxymethyl)-3-cyclohexyl-D-alanyl-4-(aminomethyl)-N-(4-carbamimidoylbenzyl)phenylalaninamide | |
0.0013 | - |
pH 7.4, 37°C | Homo sapiens | N-(carboxymethyl)-3-cyclohexyl-L-alanyl-N-(4-carbamimidoylbenzyl)-3-piperidin-4-ylalaninamide | |
0.0016 | - |
pH 7.4, 37°C | Homo sapiens | N2-[(2S)-2-amino-2-cyclohexylacetyl]-N-(4-carbamimidoylbenzyl)argininamide | |
0.0017 | - |
pH 7.4, 37°C | Homo sapiens | N-[(1S)-2-([2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]amino)-1-cyclohexyl-2-oxoethyl]glycine | |
0.0028 | - |
pH 7.4, 37°C | Homo sapiens | N-(2-carboxyethyl)-3-cyclohexyl-L-alanyl-N-(4-carbamimidoylbenzyl)argininamide | |
0.0031 | - |
pH 7.4, 37°C | Homo sapiens | N-[(2S)-1-[[(1S)-2-[(4-carbamimidoylbenzyl)amino]-2-oxo-1-(piperidin-4-yl)ethyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]glycine | |
0.0031 | - |
pH 7.4, 37°C | Homo sapiens | N-(4-carbamimidoylbenzyl)-2-[(3-cyclohexyl-L-alanyl)amino]-4-(piperidin-4-yl)butanamide | |
0.0038 | - |
pH 7.4, 37°C | Homo sapiens | N-(carboxymethyl)-3-cyclohexyl-D-alanyl-N-(4-carbamimidoylbenzyl)-4-cyanophenylalaninamide | |
0.0056 | - |
pH 7.4, 37°C | Homo sapiens | N-(carboxymethyl)-3-cyclohexyl-L-alanyl-N-(4-carbamimidoylbenzyl)-3-pyrrolidin-2-yl-L-alaninamide | |
0.0092 | - |
pH 7.4, 37°C | Homo sapiens | N-[(2S)-1-([1-[(4-carbamimidoylbenzyl)amino]-1-oxo-4-(piperidin-4-yl)butan-2-yl]amino)-3-cyclohexyl-1-oxopropan-2-yl]glycine | |
0.044 | - |
above, pH 7.4, 37°C | Homo sapiens | N-(carboxymethyl)-3-cyclohexyl-L-alanyl-N-(4-carbamimidoylbenzyl)-3-pyrrolidin-2-yl-D-alaninamide | |
0.044 | - |
above, pH 7.4, 37°C | Homo sapiens | N-[(1S)-2-([1-[(4-carbamimidoylbenzyl)amino]-1-oxo-4-(piperidin-4-yl)butan-2-yl]amino)-1-cyclohexyl-2-oxoethyl]glycine |