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Literature summary extracted from

  • Priestley, E.S.; Cheney, D.L.; DeLucca, I.; Wei, A.; Luettgen, J.M.; Rendina, A.R.; Wong, P.C.; Wexler, R.R.
    Structure-based design of macrocyclic coagulation factor VIIa inhibitors (2015), J. Med. Chem., 58, 6225-6236 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.21 (2R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6(21),7,9,16,19-hexaene-3,12-dione
-
 Homo sapiens
3.4.21.21 (2R)-2-[(1-aminoisoquinolin-6-yl)amino]-7-(propane-2-sulfonyl)-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6(21),7,9,16,19-hexaene-3,12-dione
-
 Homo sapiens
3.4.21.21 (2S)-2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6(21),7,9,16,19-hexaene-3,12-dione
-
 Homo sapiens
3.4.21.21 (R)-2-(1-aminoisoquinolin-6-ylamino)-7-ethanesulfonyl-20-methyl-4,11-diaza-tricyclo[14.2.2.16,10]henicosa-1(19),6,8,10-(21),16(20),17-hexaene-3,12-dione
-
 Homo sapiens
3.4.21.21 (R)-2-(1-aminoisoquinolin-6-ylamino)-7-ethanesulfonyl-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(19),6,8,10(21),16-(20),17-hexaene-3,12-dione
-
 Homo sapiens
3.4.21.21 2-(1-aminoisoquinolin-6-ylamino)-16-oxa-4,11-diazatricyclo-[15.2.2.16,10]docosa-1(20),6,8,10(22),17(21),18-hexaene-3,12-dione trifluoroacetic acid
-
 Homo sapiens
3.4.21.21 2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[13.2.2.16,10]icosa-1(17),6(20),7,9,15,18-hexaene-3,12-dione
-
 Homo sapiens
3.4.21.21 2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6(21),7,9,16,19-hexaene-3,12-dione
-
 Homo sapiens
3.4.21.21 2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[15.2.2.16,10]docosa-1(19),6(22),7,9,17,20-hexaene-3,12-dione
-
 Homo sapiens
3.4.21.21 4-((R)-7-ethanesulfonyl-3,12-dioxo-4,11-diaza-tricyclo-[14.2.2.16,10]henicosa-1(19),6,8,10(21),16(20),17-hexaen-2-ylamino)benzamidine trifluoroacetic acid
-
 Homo sapiens
3.4.21.21 N-[3-[(2R)-1-[(2R)-2-[(1-aminoisoquinolin-6-yl)amino]-2-phenylacetyl]pyrrolidin-2-yl]-4-(propane-2-sulfonyl)phenyl]acetamide
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.21 Homo sapiens
-
-
-

Synonyms

EC Number Synonyms Comment Organism
3.4.21.21 FVIIa
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.21 0.0000007
-
 4-((R)-7-ethanesulfonyl-3,12-dioxo-4,11-diaza-tricyclo-[14.2.2.16,10]henicosa-1(19),6,8,10(21),16(20),17-hexaen-2-ylamino)benzamidine trifluoroacetic acid pH and temperature not specified in the publication Homo sapiens
3.4.21.21 0.0000016
-
 (R)-2-(1-aminoisoquinolin-6-ylamino)-7-ethanesulfonyl-20-methyl-4,11-diaza-tricyclo[14.2.2.16,10]henicosa-1(19),6,8,10-(21),16(20),17-hexaene-3,12-dione pH and temperature not specified in the publication Homo sapiens
3.4.21.21 0.0000052
-
 (2R)-2-[(1-aminoisoquinolin-6-yl)amino]-7-(propane-2-sulfonyl)-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6(21),7,9,16,19-hexaene-3,12-dione pH and temperature not specified in the publication Homo sapiens
3.4.21.21 0.000008
-
 (R)-2-(1-aminoisoquinolin-6-ylamino)-7-ethanesulfonyl-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(19),6,8,10(21),16-(20),17-hexaene-3,12-dione pH and temperature not specified in the publication Homo sapiens
3.4.21.21 0.00003
-
 (2R)-2-[(1-aminoisoquinolin-6-yl)amino]-7-(propane-2-sulfonyl)-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6(21),7,9,16,19-hexaene-3,12-dione pH and temperature not specified in the publication Homo sapiens
3.4.21.21 0.0004
-
 (2R)-2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6(21),7,9,16,19-hexaene-3,12-dione pH and temperature not specified in the publication Homo sapiens
3.4.21.21 0.00092
-
 2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6(21),7,9,16,19-hexaene-3,12-dione pH and temperature not specified in the publication Homo sapiens
3.4.21.21 0.0046
-
 2-(1-aminoisoquinolin-6-ylamino)-16-oxa-4,11-diazatricyclo-[15.2.2.16,10]docosa-1(20),6,8,10(22),17(21),18-hexaene-3,12-dione trifluoroacetic acid pH and temperature not specified in the publication Homo sapiens
3.4.21.21 0.0046
-
 2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[13.2.2.16,10]icosa-1(17),6(20),7,9,15,18-hexaene-3,12-dione pH and temperature not specified in the publication Homo sapiens
3.4.21.21 0.0061
-
 2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[15.2.2.16,10]docosa-1(19),6(22),7,9,17,20-hexaene-3,12-dione pH and temperature not specified in the publication Homo sapiens
3.4.21.21 0.01
-
 2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[13.2.2.16,10]icosa-1(17),6(20),7,9,15,18-hexaene-3,12-dione pH and temperature not specified in the publication Homo sapiens
3.4.21.21 0.018
-
 (2S)-2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6(21),7,9,16,19-hexaene-3,12-dione Ki above 0.018 mM, pH and temperature not specified in the publication Homo sapiens
3.4.21.21 0.054
-
 (2S)-2-[(1-aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6(21),7,9,16,19-hexaene-3,12-dione pH and temperature not specified in the publication Homo sapiens