Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2R,15R)-2-[(1-amino-4-fluoroisoquinolin-6-yl)amino]-7-(cyclopropanesulfonyl)-4,15,17-trimethyl-13-oxa-4,11-diazatricyclo-[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione | highly potent, selective inhibitor | Homo sapiens | |
(2R,15R)-2-[(1-amino-7-fluoroisoquinolin-6-yl)amino]-7-(cyclopropanesulfonyl)-4,15,17-trimethyl-13-oxa-4,11-diazatricyclo-[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione | - |
Homo sapiens | |
(2R,15R)-2-[(1-amino-8-fluoroisoquinolin-6-yl)amino]-7-(cyclopropanesulfonyl)-4,15,17- trimethyl-13-oxa-4,11-diazatricyclo-[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione | - |
Homo sapiens | |
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-13-oxa-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6,8,10-(21),16,19-hexaene-3,12-dione | - |
Homo sapiens | |
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-3,12-dioxo-13-oxa-4,11- diazatricyclo[14.2.2.16,10]henicosa-1-(18),6,8,10(21),16,19-hexaene-7-carboxamide | - |
Homo sapiens | |
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-7-(trifluoromethoxy)-13-oxa-4,11-diazatricyclo[14.2.2.16,10]-henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione | - |
Homo sapiens | |
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,20-trimethyl-7-(1-methyl-1H-pyrazol-5-yl)-13-oxa-4,11-diazatricyclo-[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione | - |
Homo sapiens | |
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-7-(cyclopropanesulfonyl)-4,15,20-trimethyl-13-oxa-4,11-diazatricyclo[14.2.2.16,10]-henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione | - |
Homo sapiens | |
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-N,N,4,15,17-pentamethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]-henicosa-1(18),6,8,10(21),16,19-hexaene-7-carboxamide | - |
Homo sapiens | |
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-N,N-diethyl-4,15,17-trimethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]-henicosa-1(18),6,8,10(21),16,19-hexaene-7-carboxamide | - |
Homo sapiens | |
diethyl [(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaen-7-yl]phosphonate | - |
Homo sapiens | |
methyl (2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-7-carboxylate | - |
Homo sapiens | |
[(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,20-trimethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]henicosa-1-(18),6,8,10(21),16,19-hexaen-7-yl](ethoxy)phosphinic acid | - |
Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Ca2+ | 5 mM used in assay conditions | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
D-Ile-Pro-Arg-4-nitroanilide + H2O | - |
Homo sapiens | D-Ile-Pro-Arg + 4-nitroaniline | - |
? |
Synonyms | Comment | Organism |
---|---|---|
FVIIa | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00000016 | - |
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-7-(cyclopropanesulfonyl)-4,15,20-trimethyl-13-oxa-4,11-diazatricyclo[14.2.2.16,10]-henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione | at pH 7.4 and 37°C | Homo sapiens | |
0.00000023 | - |
(2R,15R)-2-[(1-amino-7-fluoroisoquinolin-6-yl)amino]-7-(cyclopropanesulfonyl)-4,15,17-trimethyl-13-oxa-4,11-diazatricyclo-[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione | at pH 7.4 and 37°C | Homo sapiens | |
0.00000028 | - |
[(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,20-trimethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]henicosa-1-(18),6,8,10(21),16,19-hexaen-7-yl](ethoxy)phosphinic acid | at pH 7.4 and 37°C | Homo sapiens | |
0.00000043 | - |
(2R,15R)-2-[(1-amino-4-fluoroisoquinolin-6-yl)amino]-7-(cyclopropanesulfonyl)-4,15,17-trimethyl-13-oxa-4,11-diazatricyclo-[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione | at pH 7.4 and 37°C | Homo sapiens | |
0.00000057 | - |
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-N,N-diethyl-4,15,17-trimethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]-henicosa-1(18),6,8,10(21),16,19-hexaene-7-carboxamide | at pH 7.4 and 37°C | Homo sapiens | |
0.00000061 | - |
diethyl [(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaen-7-yl]phosphonate | at pH 7.4 and 37°C | Homo sapiens | |
0.000001 | - |
(2R,15R)-2-[(1-amino-8-fluoroisoquinolin-6-yl)amino]-7-(cyclopropanesulfonyl)-4,15,17- trimethyl-13-oxa-4,11-diazatricyclo-[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione | at pH 7.4 and 37°C | Homo sapiens | |
0.0000022 | - |
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,20-trimethyl-7-(1-methyl-1H-pyrazol-5-yl)-13-oxa-4,11-diazatricyclo-[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione | at pH 7.4 and 37°C | Homo sapiens | |
0.0000025 | - |
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-N,N,4,15,17-pentamethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]-henicosa-1(18),6,8,10(21),16,19-hexaene-7-carboxamide | at pH 7.4 and 37°C | Homo sapiens | |
0.0000055 | - |
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-7-(trifluoromethoxy)-13-oxa-4,11-diazatricyclo[14.2.2.16,10]-henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dione | at pH 7.4 and 37°C | Homo sapiens | |
0.0000087 | - |
methyl (2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-3,12-dioxo-13-oxa-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-7-carboxylate | at pH 7.4 and 37°C | Homo sapiens | |
0.000015 | - |
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-3,12-dioxo-13-oxa-4,11- diazatricyclo[14.2.2.16,10]henicosa-1-(18),6,8,10(21),16,19-hexaene-7-carboxamide | at pH 7.4 and 37°C | Homo sapiens | |
0.00002 | - |
(2R,15R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,15,17-trimethyl-13-oxa-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6,8,10-(21),16,19-hexaene-3,12-dione | at pH 7.4 and 37°C | Homo sapiens |