Any feedback?
Literature summary for 3.4.21.B61 extracted from
- Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT (2011), Bioorg. Med. Chem. Lett., 21, 4860-4864 .
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 5-oxo-N-(phenylmethanesulfonyl)-5-(piperazin-1-yl)-D-norvalyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens |  |
| 5-oxo-N-(phenylmethanesulfonyl)-5-[4-(pyrimidin-2-yl)piperazin-1-yl]-D-norvalyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| 5-[4-[(benzyloxy)carbonyl]piperazin-1-yl]-5-oxo-N-(phenylmethanesulfonyl)-D-norvalyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| benzyl 4-[(3R)-4-[(2S)-2-[[(4-carbamimidoylphenyl)methyl]carbamoyl]pyrrolidin-1-yl]-4-oxo-3-[(phenylmethanesulfonyl)amino]butanoyl]piperazine-1-carboxylate | - |
Homo sapiens | |
| N-(phenylmethanesulfonyl)-4-carbamimidoyl-D-phenylalanyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| N-(phenylmethanesulfonyl)-4-cyano-D-phenylalanyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| N-(phenylmethanesulfonyl)-D-alpha-aspartyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| N-(phenylmethanesulfonyl)-D-cyclohexylalanyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| N-(phenylmethanesulfonyl)-D-leucyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| N-(phenylmethanesulfonyl)-D-phenylalanyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| N-(phenylmethanesulfonyl)-D-valyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| N-[(4-carbamimidoylphenyl)methyl]-1-[(2R)-4-(morpholin-4-yl)-4-oxo-2-[(phenylmethanesulfonyl)amino]butanoyl]-L-prolinamide | - |
Homo sapiens | |
| N-[(4-carbamimidoylphenyl)methyl]-1-[(2R)-4-oxo-2-[(phenylmethanesulfonyl)amino]-4-[4-(propan-2-yl)piperazin-1-yl]butanoyl]-L-prolinamide | - |
Homo sapiens | |
| N-[(4-carbamimidoylphenyl)methyl]-1-[(2R)-4-oxo-2-[(phenylmethanesulfonyl)amino]-4-[4-(pyrimidin-2-yl)piperazin-1-yl]butanoyl]-L-prolinamide | - |
Homo sapiens | |
| N-[(4-carbamimidoylphenyl)methyl]-1-[(2R)-4-[4-(3,5-dimethylphenyl)piperazin-1-yl]-4-oxo-2-[(phenylmethanesulfonyl)amino]butanoyl]-L-prolinamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-2-aminobutanoylamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-alaninamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-argininamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-isoleucinamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-leucinamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-norvalinamide | inhibitor suppresses replication of H1 and H3 influenza viruses in a HAT-expressing MDCK cell model | Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-phenylalaninamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-serinamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-valinamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-arginyl-N1-[(4-carbamimidoylphenyl)methyl]-L-aspartamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-arginyl-N6-[(benzyloxy)carbonyl]-N-[(4-carbamimidoylphenyl)methyl]-L-lysinamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-homoarginyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-homophenylalanyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-D-lysyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-N-tert-butoxy-D-asparaginyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-N6-(benzyloxycarbonyl)-D-lysyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| N2-(phenylmethanesulfonyl)-O-(tert-butyl)-D-glutamyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | - |
Homo sapiens | |
| tert-butyl N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-alpha-asparaginate | - |
Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | O60235 | - |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| D-cyclohexylalanine-Pro-Arg-AMC + H2O | - |
Homo sapiens | D-cyclohexylalanine-Pro-Arg + 7-amino-4-methylcoumarin | - |
? | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.000013 | - |
N2-(phenylmethanesulfonyl)-D-homoarginyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000014 | - |
N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-2-aminobutanoylamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000015 | - |
N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-norvalinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000017 | - |
5-oxo-N-(phenylmethanesulfonyl)-5-[4-(pyrimidin-2-yl)piperazin-1-yl]-D-norvalyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000019 | - |
N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000022 | - |
N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-valinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000023 | - |
N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-isoleucinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.00003 | - |
N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-alaninamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000034 | - |
N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-serinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000034 | - |
N2-(phenylmethanesulfonyl)-D-arginyl-N6-[(benzyloxy)carbonyl]-N-[(4-carbamimidoylphenyl)methyl]-L-lysinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000036 | - |
N2-(phenylmethanesulfonyl)-O-(tert-butyl)-D-glutamyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000038 | - |
5-[4-[(benzyloxy)carbonyl]piperazin-1-yl]-5-oxo-N-(phenylmethanesulfonyl)-D-norvalyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000038 | - |
N2-(phenylmethanesulfonyl)-N-tert-butoxy-D-asparaginyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.00004 | - |
N2-(phenylmethanesulfonyl)-D-lysyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000043 | - |
N-[(4-carbamimidoylphenyl)methyl]-1-[(2R)-4-oxo-2-[(phenylmethanesulfonyl)amino]-4-[4-(pyrimidin-2-yl)piperazin-1-yl]butanoyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000047 | - |
N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-leucinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000053 | - |
N2-(phenylmethanesulfonyl)-N6-(benzyloxycarbonyl)-D-lysyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000057 | - |
N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-phenylalaninamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000063 | - |
N2-(phenylmethanesulfonyl)-D-homophenylalanyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000068 | - |
5-oxo-N-(phenylmethanesulfonyl)-5-(piperazin-1-yl)-D-norvalyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000073 | - |
N-[(4-carbamimidoylphenyl)methyl]-1-[(2R)-4-[4-(3,5-dimethylphenyl)piperazin-1-yl]-4-oxo-2-[(phenylmethanesulfonyl)amino]butanoyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000076 | - |
N-(phenylmethanesulfonyl)-D-valyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000098 | - |
N-(phenylmethanesulfonyl)-D-phenylalanyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000108 | - |
N-(phenylmethanesulfonyl)-D-cyclohexylalanyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.00012 | - |
N-(phenylmethanesulfonyl)-D-leucyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000135 | - |
benzyl 4-[(3R)-4-[(2S)-2-[[(4-carbamimidoylphenyl)methyl]carbamoyl]pyrrolidin-1-yl]-4-oxo-3-[(phenylmethanesulfonyl)amino]butanoyl]piperazine-1-carboxylate | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000168 | - |
N-(phenylmethanesulfonyl)-4-carbamimidoyl-D-phenylalanyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000183 | - |
N-[(4-carbamimidoylphenyl)methyl]-1-[(2R)-4-(morpholin-4-yl)-4-oxo-2-[(phenylmethanesulfonyl)amino]butanoyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.00021 | - |
N-[(4-carbamimidoylphenyl)methyl]-1-[(2R)-4-oxo-2-[(phenylmethanesulfonyl)amino]-4-[4-(propan-2-yl)piperazin-1-yl]butanoyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000311 | - |
N-(phenylmethanesulfonyl)-4-cyano-D-phenylalanyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000422 | - |
N2-(phenylmethanesulfonyl)-D-arginyl-N1-[(4-carbamimidoylphenyl)methyl]-L-aspartamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000457 | - |
N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-argininamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.000512 | - |
tert-butyl N2-(phenylmethanesulfonyl)-D-arginyl-N-[(4-carbamimidoylphenyl)methyl]-L-alpha-asparaginate | pH 9.5, temperature not specified in the publication | Homo sapiens | |
| 0.001425 | - |
N-(phenylmethanesulfonyl)-D-alpha-aspartyl-N-[(4-carbamimidoylphenyl)methyl]-L-prolinamide | pH 9.5, temperature not specified in the publication | Homo sapiens | |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
