Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.21.22 extracted from

  • Meng, D.; Andre, P.; Bateman, T.J.; Berger, R.; Chen, Y.H.; Desai, K.; Dewnani, S.; Ellsworth, K.; Feng, D.; Geissler, W.M.; Guo, L.; Hruza, A.; Jian, T.; Li, H.; Metzger, J.; Parker, D.L.; Reichert, P.; Sherer, E.C.; Smith, C.J.; Sonatore, L.M.; Tschirret-Guth, R.; Wu, J.; Xu, J.; Zhang, T.; Campeau, L.C.; Orr,
    Development of a novel tricyclic class of potent and selective FIXa inhibitors (2015), Bioorg. Med. Chem. Lett., 25, 5437-5443 .
    View publication on PubMed
Search for more literature for 3.4.21.22

Inhibitors

Inhibitors Comment Organism Structure
(2E)-3-[(7S)-7-[2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamido]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]prop-2-enoic acid
-
 Homo sapiens
(7S)-2-methyl-7-phenyl-7-[4-(4H-1,2,4-triazol-4-yl)benzamido]-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxylic acid
-
 Homo sapiens
(7S)-2-methyl-7-phenyl-7-[[5-(4H-1,2,4-triazol-4-yl)pyridine-2-carbonyl]amino]-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxylic acid
-
 Homo sapiens
(7S)-7-[2-chloro-4-(1H-tetrazol-1-yl)benzamido]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxylic acid
-
 Homo sapiens
(7S)-7-[2-chloro-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamido]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxylic acid
-
 Homo sapiens
(7S)-7-[2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamido]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxamide
-
 Homo sapiens
1-(3-chloro-4-[[(2R)-2,8-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]carbamoyl]phenyl)-1H-benzimidazole-5-carboxylic acid
-
 Homo sapiens
2,6-dichloro-4-(3-methyl-1H-1,2,4-triazol-1-yl)-N-[(2R)-8-methyl-2-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]benzamide
-
 Homo sapiens
2,6-dichloro-N-((R)-2-((S)-1-hydroxyethyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl)-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
 Homo sapiens
2,6-dichloro-N-[(2R)-10-hydroxy-2,7-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
 Homo sapiens
2,6-dichloro-N-[(2R)-2,8-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
 Homo sapiens
2,6-dichloro-N-[(2R)-2-(3,4-difluorophenyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
 Homo sapiens
2,6-dichloro-N-[(2R)-2-(3-fluorophenyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
 Homo sapiens
2,6-dichloro-N-[(2R)-2-(4-fluorophenyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
 Homo sapiens
2,6-dichloro-N-[(2R)-8-methyl-2-(3-methylphenyl)-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
 Homo sapiens
2,6-dichloro-N-[(2R)-8-methyl-2-[1-(propan-2-yl)-1H-1,2,3-triazol-4-yl]-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
 Homo sapiens
2,6-dichloro-N-[(3R)-3,7-dimethyl-2,3,4,9-tetrahydro-1H-carbazol-3-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
 Homo sapiens
2-chloro-N-[(2R)-2-(3-methoxyphenyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
 Homo sapiens
2-chloro-N-[(2R)-8-methyl-2-phenyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide
-
 Homo sapiens
2-chloro-N-[(7S)-10-cyclopropyl-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide
-
 Homo sapiens
2-chloro-N-[(7S)-10-[(E)-(hydroxyimino)methyl]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide
-
 Homo sapiens
2-chloro-N-[(7S)-2-methyl-7-phenyl-10-(2,2,2-trifluoro-1-hydroxyethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide
-
 Homo sapiens
2-chloro-N-[(7S)-2-methyl-7-phenyl-10-(2H-tetrazol-5-yl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide
-
 Homo sapiens
3-[(7R)-7-[2-chloro-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamido]-2-methyl-7-phenyl-4a,6,7,8,9,10a-hexahydropyrido[1,2-a]indol-10-yl]propanoic acid
-
 Homo sapiens
4-cyano-2-fluoro-N-(10-hydroxy-2,7-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl)benzamide
-
 Homo sapiens
N-[(7S)-10-(5-aminopyridin-3-yl)-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamide
-
 Homo sapiens
N-[2-(5,6-dimethyl-1H-benzimidazol-2-yl)ethyl]-4-(4H-1,2,4-triazol-4-yl)benzamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
FIXa
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000006
-
 (7S)-2-methyl-7-phenyl-7-[4-(4H-1,2,4-triazol-4-yl)benzamido]-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxylic acid pH and temperature not specified in the publication Homo sapiens
0.0000006
-
 (7S)-7-[2-chloro-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamido]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxylic acid pH and temperature not specified in the publication Homo sapiens
0.0000008
-
 (2E)-3-[(7S)-7-[2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamido]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]prop-2-enoic acid pH and temperature not specified in the publication Homo sapiens
0.0000012
-
 (7S)-7-[2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamido]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000016
-
 N-[(7S)-10-(5-aminopyridin-3-yl)-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-2-chloro-4-(4H-1,2,4-triazol-4-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000018
-
 2,6-dichloro-N-[(2R)-8-methyl-2-(3-methylphenyl)-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000021
-
 2-chloro-N-[(2R)-8-methyl-2-phenyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000024
-
 2-chloro-N-[(7S)-10-[(E)-(hydroxyimino)methyl]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000024
-
 2-chloro-N-[(7S)-2-methyl-7-phenyl-10-(2H-tetrazol-5-yl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000025
-
 (7S)-2-methyl-7-phenyl-7-[[5-(4H-1,2,4-triazol-4-yl)pyridine-2-carbonyl]amino]-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxylic acid pH and temperature not specified in the publication Homo sapiens
0.0000026
-
 2-chloro-N-[(7S)-2-methyl-7-phenyl-10-(2,2,2-trifluoro-1-hydroxyethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000027
-
 3-[(7R)-7-[2-chloro-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamido]-2-methyl-7-phenyl-4a,6,7,8,9,10a-hexahydropyrido[1,2-a]indol-10-yl]propanoic acid pH and temperature not specified in the publication Homo sapiens
0.0000029
-
 2-chloro-N-[(7S)-10-[(E)-(hydroxyimino)methyl]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.000003
-
 2-chloro-N-[(2R)-2-(3-methoxyphenyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000031
-
 2,6-dichloro-N-[(2R)-2-(3-fluorophenyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000042
-
 2,6-dichloro-N-[(2R)-2-(4-fluorophenyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000045
-
 2,6-dichloro-4-(3-methyl-1H-1,2,4-triazol-1-yl)-N-[(2R)-8-methyl-2-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]benzamide pH and temperature not specified in the publication Homo sapiens
0.000005
-
 2,6-dichloro-N-[(2R)-8-methyl-2-[1-(propan-2-yl)-1H-1,2,3-triazol-4-yl]-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000051
-
 2-chloro-N-[(7S)-10-cyclopropyl-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000055
-
 2-chloro-N-[(7S)-2-methyl-7-phenyl-10-(2,2,2-trifluoro-1-hydroxyethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000059
-
 2-chloro-N-[(2R)-8-methyl-2-phenyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000063
-
 1-(3-chloro-4-[[(2R)-2,8-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]carbamoyl]phenyl)-1H-benzimidazole-5-carboxylic acid pH and temperature not specified in the publication Homo sapiens
0.0000066
-
 2,6-dichloro-N-[(2R)-2-(3-fluorophenyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000069
-
 2-chloro-N-[(2R)-8-methyl-2-phenyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.000008
-
 2-chloro-N-[(7S)-10-cyclopropyl-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000084
-
 2-chloro-N-[(7S)-10-cyclopropyl-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indol-7-yl]-4-(4H-1,2,4-triazol-4-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000086
-
 (7S)-7-[2-chloro-4-(1H-tetrazol-1-yl)benzamido]-2-methyl-7-phenyl-6,7,8,9-tetrahydropyrido[1,2-a]indole-10-carboxylic acid pH and temperature not specified in the publication Homo sapiens
0.0000102
-
 2,6-dichloro-N-[(2R)-10-hydroxy-2,7-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000102
-
 2,6-dichloro-N-[(2R)-2,8-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000105
-
 1-(3-chloro-4-[[(2R)-2,8-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]carbamoyl]phenyl)-1H-benzimidazole-5-carboxylic acid pH and temperature not specified in the publication Homo sapiens
0.0000105
-
 2,6-dichloro-N-[(2R)-2-(3,4-difluorophenyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000117
-
 2,6-dichloro-N-[(3R)-3,7-dimethyl-2,3,4,9-tetrahydro-1H-carbazol-3-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000121
-
 2,6-dichloro-N-[(2R)-10-hydroxy-2,7-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000125
-
 2,6-dichloro-N-((R)-2-((S)-1-hydroxyethyl)-8-methyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl)-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
0.0000138
-
 3-[(7R)-7-[2-chloro-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamido]-2-methyl-7-phenyl-4a,6,7,8,9,10a-hexahydropyrido[1,2-a]indol-10-yl]propanoic acid pH and temperature not specified in the publication Homo sapiens
0.0000348
-
 1-(3-chloro-4-[[(2R)-2,8-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl]carbamoyl]phenyl)-1H-benzimidazole-5-carboxylic acid pH and temperature not specified in the publication Homo sapiens
0.0002676
-
 2,6-dichloro-N-[(3R)-3,7-dimethyl-2,3,4,9-tetrahydro-1H-carbazol-3-yl]-4-(3-methyl-1H-1,2,4-triazol-1-yl)benzamide pH and temperature not specified in the publication Homo sapiens
2
-
 4-cyano-2-fluoro-N-(10-hydroxy-2,7-dimethyl-1,2,3,4-tetrahydropyrido[1,2-b]indazol-2-yl)benzamide pH and temperature not specified in the publication Homo sapiens
9
-
 N-[2-(5,6-dimethyl-1H-benzimidazol-2-yl)ethyl]-4-(4H-1,2,4-triazol-4-yl)benzamide pH and temperature not specified in the publication Homo sapiens