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Coagulation factor IX Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
RazaxabanKi9000.0 [1]
2-[3-(Aminomethyl)phenyl]-N-[2-fluoro-4-(2-methylsulfonylphenyl)phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide;hydrochlorideKi2200.0 [1]
2-Chloro-N-[(2R)-2-(5,6-dimethyl-1H-benzimidazol-2-yl)-2-phenylethyl]-4-(1,2,4-triazol-4-yl)benzamideKi15.7 [1], 16.0 [2]
2,6-Dichloro-N-[(2R)-2-(3-fluorophenyl)-2-(2-methyl-3H-benzimidazol-5-yl)ethyl]-4-(3-methyl-1,2,4-triazol-1-yl)benzamideIC509.99 [1]
2,6-Dichloro-N-[(2R)-2-(3-fluorophenyl)-2-(2-methyl-3H-benzimidazol-5-yl)ethyl]-4-(3-methyl-1,2,4-triazol-1-yl)benzamideKi9.1 [1]
CID 23646208Ki660.0 [1]
N-[4-(Benzimidazol-1-yl)-2-fluorophenyl]-2-(3-carbamimidoylphenyl)-5-(trifluoromethyl)pyrazole-3-carboxamideKi13.0 [1]
N-[(1S)-1-[4-(3-Amino-1H-indazol-6-yl)pyridin-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexane-1-carboxamideKi34860.0 [1]
Benzo[b]thiophene-2-carboximidamide, 4-iodo-Ki950.0 [1]
2-[3-(Aminomethyl)phenyl]-N-[2-fluoro-4-(2-methylsulfonylphenyl)phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamideKi2200.0 [1]
LetaxabanIC504500.0 [1]
Bms-740808Ki2800.0 [1]
2-(3-Carbamimidoylphenyl)-5-methyl-N-[4-(2-sulfamoylphenyl)phenyl]pyrazole-3-carboxamideKi1900.0 [1]
Unii-vwj4vvz3OUKi27000.0 [1]
2-(2-Hydroxy-biphenyl)-1h-benzoimidazole-5-carboxamidineKi99.0 [1]
Bms-344577Ki18000.0 [1]
Methyl N-[4-[5-chloro-2-[(1S)-1-[[(E)-3-[5-chloro-2-(tetrazol-1-yl)phenyl]prop-2-enoyl]amino]-2-phenylethyl]-1H-imidazol-4-yl]phenyl]carbamateKi27100.0 [1]
2-[2-(Aminomethyl)phenyl]-N-[2-fluoro-4-(2-sulfamoylphenyl)phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamideKi12000.0 [1]
3-[6-[4-[2-[(Dimethylamino)methyl]phenyl]phenyl]-7-oxo-3-(trifluoromethyl)-4,5-dihydropyrazolo[3,4-c]pyridin-1-yl]benzamideKi1800.0 [1]
2-(3-Amino-1,2-benzoxazol-5-yl)-N-[4-[2-[(dimethylamino)methyl]phenyl]-2-fluorophenyl]-5-(trifluoromethyl)pyrazole-3-carboxamideKi12000.0 [1]
2-(3-Amino-1,2-benzoxazol-5-yl)-N-[2-fluoro-4-(2-methylsulfonylphenyl)phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamideKi3500.0 [1]
N-[(1S)-1-[4-(3-Amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexane-1-carboxamideKi34900.0 [1]
CID 15511974Ki6700.0 [1]
1-(3-Amino-1,2-benzoxazol-5-yl)-6-[4-[2-[(dimethylamino)methyl]phenyl]phenyl]-5-methyl-3-(trifluoromethyl)pyrazolo[4,3-d]pyrimidin-7-oneKi37000.0 [1]
[2-[(2-Carbamimidoyl-1-benzothiophen-4-yl)oxy]-2-phenylethyl] N-[2-[(2-methylpropylamino)methyl]phenyl]carbamateKi2.0 [1]
Methyl N-[(14S)-14-[[(E)-3-[5-chloro-2-(tetrazol-1-yl)phenyl]prop-2-enoyl]amino]-9-oxo-8,16,18-triazatricyclo[13.2.1.02,7]octadeca-1(17),2(7),3,5,15-pentaen-5-yl]carbamateKi27100.0 [1]
(2R)-2-[(1-Aminoisoquinolin-6-yl)amino]-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(19),6(21),7,9,16(20),17-hexaene-3,12-dioneKi35000.0 [1]
(2R)-2-[(1-Aminoisoquinolin-6-yl)amino]-7-ethylsulfonyl-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(19),6,8,10(21),16(20),17-hexaene-3,12-dioneKi35000.0 [1]
(2R)-2-[(1-Aminoisoquinolin-6-yl)amino]-7-ethylsulfonyl-17-methyl-4,11-diazatricyclo[14.2.2.16,10]henicosa-1(18),6,8,10(21),16,19-hexaene-3,12-dioneKi16000.0 [1]
Methyl N-[4-[2-[(1S)-1-[[(E)-3-[5-chloro-2-(tetrazol-1-yl)phenyl]prop-2-enoyl]amino]-2-phenylethyl]-1H-imidazol-5-yl]phenyl]carbamateKi60000.0 [1]
Methyl N-[(12E,15S)-15-[[(E)-3-[5-chloro-2-(tetrazol-1-yl)phenyl]prop-2-enoyl]amino]-9-oxo-8,17,19-triazatricyclo[14.2.1.02,7]nonadeca-1(18),2(7),3,5,12,16-hexaen-5-yl]carbamateKi27100.0 [1]
1-(4-Methoxyphenyl)-7-oxo-6-[4-[2-(pyrrolidin-1-ylmethyl)phenyl]phenyl]pyrazolo[4,3-d]pyrimidine-3-carboxamideKi41000.0 [1]
2-[2-[(4-Carbamimidoylphenyl)carbamoyl]-6-methoxypyridin-3-yl]-5-(2,2-dimethylpropylcarbamoyl)benzoic acidIC5051.0 [1]
5-(2-(2-Fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)acetyl)-1-(4-methoxyphenyl)-1H-pyrazole-3-carboxamideKi15000.0 [1]
3-[3-[4-(Benzimidazol-1-yl)-2-fluoroanilino]-2-(5-carbamimidoyl-1H-indol-3-yl)-3-oxopropyl]benzoic acidKi59.0 [1]
2-[3-(6-Carbamimidoyl-4-methyl-4-phenyl-2,3-dihydro-1H-quinolin-2-yl)-5-(3-methylbutanoylamino)phenyl]-5-carbamoylbenzoic acidKi20000.0 [1]
(3R,4R)-3-N-(5-Chloropyridin-2-yl)-4-N-[2-fluoro-4-(2-oxopyridin-1-yl)phenyl]-1-propan-2-ylpyrrolidine-3,4-dicarboxamideKi33000.0 [1]
4-Hydroxybutyl (Z)-2-cyano-3-[(2-methyl-1-benzofuran-5-yl)amino]-3-[[(3S)-2-oxo-1-(2-oxo-2-pyrrolidin-1-ylethyl)azepan-3-yl]amino]prop-2-enoateKi10000.0 [1]
N-[(3R)-1-(3-Amino-4-chloro-[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-[3-(difluoromethyl)-1,2,4-triazol-4-yl]benzamideIC5045.0 [1]
N-[(3R)-1-(3-Amino-4-chloro-[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-(1-methyl-5-oxo-1,2,4-triazol-4-yl)benzamideIC5015.0 [1]
N-[(3R)-1-(3-Amino-4-chloro-1,2-benzoxazol-7-yl)pyrrolidin-3-yl]-2-chloro-4-(1,2,4-triazol-4-yl)benzamideIC5032.0 [1]
N-[(3R)-1-(3-Amino-4-chloro-[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-imidazo[4,5-b]pyridin-1-ylbenzamideIC5013.0 [1]
N-[1-(3-Amino-5-chloro-1,2-benzoxazol-7-yl)pyrrolidin-3-yl]-2-chloro-4-(1,2,4-triazol-4-yl)benzamideIC5018.0 [1]
N-[(3R)-1-(3-Amino-4-chloro-[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-4-(benzimidazol-1-yl)-2-chlorobenzamideIC5032.0 [1]
N-[(3R)-1-(3-Amino-4-chloro-[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-(3-methyl-1,2,4-triazol-1-yl)benzamideIC5033.0 [1]
N-[(3R)-1-(3-Amino-4,5-dichloro-1,2-benzoxazol-7-yl)pyrrolidin-3-yl]-2-chloro-4-(1,2,4-triazol-4-yl)benzamideIC5047.0 [1]
N-[(3R)-1-(3-Amino-4-fluoro-1,2-benzoxazol-7-yl)pyrrolidin-3-yl]-2-chloro-4-(1,2,4-triazol-4-yl)benzamideIC50172.0 [1]
N-[(3R)-1-(3-Amino-4-chloro-[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-[4-(2-hydroxyethyl)imidazol-1-yl]benzamideIC5013.0 [1]
N-[(3R)-1-(3-Amino-4-chloro-[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-pyrimidin-5-ylbenzamideIC5026.0 [1]
N-[(3R)-1-(3-Amino-4-chloro-5-methyl-1,2-benzoxazol-7-yl)pyrrolidin-3-yl]-2-chloro-4-(1,2,4-triazol-4-yl)benzamideIC5062.0 [1]
N-[(3R)-1-(3-Amino-4-chloro-[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-(1-methyl-2-oxopyrimidin-5-yl)benzamideIC5036.0 [1]
N-[1-(3-Amino-[1,2]oxazolo[5,4-c]pyridin-7-yl)pyrrolidin-3-yl]-2-chloro-4-(1,2,4-triazol-4-yl)benzamideIC5089.0 [1]
N-[[(3S,3Ar)-1-oxo-7-(3-oxomorpholin-4-yl)-3a,4-dihydro-3H-[1,3]oxazolo[4,3-c][1,4]benzothiazin-3-yl]methyl]-5-chlorothiophene-2-carboxamideIC50100000.0 [1]
N-[[(3S,3As)-1-oxo-7-(3-oxomorpholin-4-yl)-3,3a,4,5-tetrahydro-[1,3]oxazolo[3,4-a]quinolin-3-yl]methyl]-5-chlorothiophene-2-carboxamideIC50100000.0 [1]
N-[[(3S,3As)-1-oxo-7-(3-oxomorpholin-4-yl)-3,3a,4,5-tetrahydro-[1,3]oxazolo[3,4-a]quinoxalin-3-yl]methyl]-5-chlorothiophene-2-carboxamideIC50100000.0 [1]
N-[(1S)-1-[4-(3-Amino-1H-indazol-6-yl)-5-chloro-1H-imidazol-2-yl]-2-phenylethyl]-4-(aminomethyl)cyclohexane-1-carboxamide;2,2,2-trifluoroacetic acidKi34900.0 [1]
N-[2-(1H-Benzimidazol-2-yl)ethyl]-4-(1,2,4-triazol-4-yl)benzamideKi114000.0 [1]
N-[2-(6-Methyl-1H-benzimidazol-2-yl)ethyl]-4-(1,2,4-triazol-4-yl)benzamideKi8520.0 [1]
N-[2-(6-Chloro-1H-benzimidazol-2-yl)ethyl]-4-(1,2,4-triazol-4-yl)benzamideKi7760.0 [1]
4-(1,2,4-Triazol-4-yl)-N-[2-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]ethyl]benzamideKi32200.0 [1]
N-[2-(6-Methoxy-1H-benzimidazol-2-yl)ethyl]-4-(1,2,4-triazol-4-yl)benzamideKi86600.0 [1]
N-[2-(4-Methyl-1H-benzimidazol-2-yl)ethyl]-4-(1,2,4-triazol-4-yl)benzamideKi145000.0 [1]
N-[2-(6-Carbamimidoyl-1H-benzimidazol-2-yl)ethyl]-4-(1,2,4-triazol-4-yl)benzamideKi54200.0 [1]
2-Chloro-N-[2-(7-hydroxy-4-methyl-1H-benzimidazol-2-yl)ethyl]-4-(1,2,4-triazol-4-yl)benzamideKi131000.0 [1]
N-[2-(5,6-Dimethyl-1H-benzimidazol-2-yl)ethyl]-2-(1,2,4-triazol-4-yl)benzamideKi145000.0 [1]
N-[2-(5,6-Dimethyl-1H-benzimidazol-2-yl)ethyl]-3-(1,2,4-triazol-4-yl)benzamideKi145000.0 [1]
4-Cyano-N-[2-(5,6-dimethyl-1H-benzimidazol-2-yl)ethyl]-2-fluorobenzamideKi145000.0 [1]
N-[2-(5,6-Dimethyl-1H-benzimidazol-2-yl)ethyl]-2-fluoro-4-(1,2,4-triazol-4-yl)benzamideKi2040.0 [1]
N-[2-(5,6-Dimethyl-1H-benzimidazol-2-yl)ethyl]-3-fluoro-4-(1,2,4-triazol-4-yl)benzamideKi18800.0 [1]
2-Chloro-N-[2-(5,6-dimethyl-1H-benzimidazol-2-yl)ethyl]benzamideKi145000.0 [1]
2-Chloro-N-[2-(5,6-dimethyl-1H-benzimidazol-2-yl)ethyl]-4-(1,2,4-triazol-4-yl)benzamideKi260.0 [1]
2-Chloro-N-[2-(5,6-dimethyl-1H-benzimidazol-2-yl)ethyl]-4-(1,2,4-triazol-1-yl)benzamideKi2120.0 [1]
2-Chloro-N-[2-(5,6-dimethyl-1H-benzimidazol-2-yl)ethyl]-4-(triazol-1-yl)benzamideKi130000.0 [1]
2-Chloro-N-[2-(5,6-dimethyl-1H-benzimidazol-2-yl)ethyl]-4-(triazol-2-yl)benzamideKi145000.0 [1]
2-Chloro-N-[2-(5,6-dimethyl-1H-benzimidazol-2-yl)ethyl]-4-imidazol-1-ylbenzamideKi5580.0 [1]
N-(10-Hydroxy-2,7-dimethyl-3,4-dihydro-1H-pyrido[1,2-b]indazol-2-yl)-4-(triazol-1-yl)benzamideKi462.0 [1]
4-Cyano-2-fluoro-N-(10-hydroxy-2,7-dimethyl-3,4-dihydro-1H-pyrido[1,2-b]indazol-2-yl)benzamideKi2000.0 [1]
4-Fluoro-N-(10-hydroxy-2,7-dimethyl-3,4-dihydro-1H-pyrido[1,2-b]indazol-2-yl)benzamideKi18300.0 [1]
4-Cyano-N-(10-hydroxy-2,7-dimethyl-3,4-dihydro-1H-pyrido[1,2-b]indazol-2-yl)benzamideKi20600.0 [1]
2-Chloro-N-(10-hydroxy-2,7-dimethyl-3,4-dihydro-1H-pyrido[1,2-b]indazol-2-yl)benzamideKi6340.0 [1]
2-Chloro-N-(10-hydroxy-2,7-dimethyl-3,4-dihydro-1H-pyrido[1,2-b]indazol-2-yl)-4-(1,2,4-triazol-4-yl)benzamideKi90.0 [1]
2-Chloro-N-(10-hydroxy-2,7-dimethyl-3,4-dihydro-1H-pyrido[1,2-b]indazol-2-yl)-4-(1,2,4-triazol-1-yl)benzamideKi156.0 [1]
2-Chloro-N-(10-hydroxy-2,7-dimethyl-3,4-dihydro-1H-pyrido[1,2-b]indazol-2-yl)-4-(triazol-1-yl)benzamideKi937.0 [1]
2-Chloro-N-(10-hydroxy-2,7-dimethyl-3,4-dihydro-1H-pyrido[1,2-b]indazol-2-yl)-4-(triazol-2-yl)benzamideKi30300.0 [1]
2-Chloro-N-(10-hydroxy-2,7-dimethyl-3,4-dihydro-1H-pyrido[1,2-b]indazol-2-yl)-4-imidazol-1-ylbenzamideKi595.0 [1]
2-Chloro-N-(10-hydroxy-2,7-dimethyl-3,4-dihydro-1H-pyrido[1,2-b]indazol-2-yl)-4-pyrazol-1-ylbenzamideKi4400.0 [1]
2-Chloro-N-[(2S)-1-(5,6-dimethyl-1H-benzimidazol-2-yl)propan-2-yl]-4-(1,2,4-triazol-4-yl)benzamideKi55400.0 [1]
2-Chloro-N-[(2R)-1-(5,6-dimethyl-1H-benzimidazol-2-yl)propan-2-yl]-4-(1,2,4-triazol-4-yl)benzamideKi35000.0 [1]
2-Chloro-N-[2-(5,6-dimethyl-1H-benzimidazol-2-yl)propyl]-4-(1,2,4-triazol-4-yl)benzamideKi340.0 [1]
2-Chloro-N-[(2S)-2-(5,6-dimethyl-1H-benzimidazol-2-yl)-2-phenylethyl]-4-(1,2,4-triazol-4-yl)benzamideKi520.0 [1]
Methyl N-[4-[2-[(1S)-1-[[4-(aminomethyl)cyclohexanecarbonyl]amino]-2-phenylethyl]pyridin-4-yl]phenyl]carbamateKi34860.0 [1]
2-Chloro-N-[(2R)-2-(5,6-dimethyl-1H-benzimidazol-2-yl)-2-phenylethyl]-6-methoxy-4-(1,2,4-triazol-4-yl)benzamideKi14.8 [1]
2,6-Dichloro-N-[(2R)-2-(8-fluoro-5-methylquinolin-2-yl)-2-(3-fluorophenyl)ethyl]-4-(3-methyl-1,2,4-triazol-1-yl)benzamideKi10.4 [1]
2,6-Dichloro-N-[(2S)-2-(3-fluorophenyl)-2-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)ethyl]-4-(3-methyl-1,2,4-triazol-1-yl)benzamideKi3.7 [1]
2,6-Dichloro-N-[(2R)-2-(5,6-dimethyl-1H-benzimidazol-2-yl)-2-phenylethyl]-4-(3-methyl-1,2,4-triazol-1-yl)benzamideKi20.8 [1]
2,6-Dichloro-N-[(2R)-2-(8-fluoro-5-methyl-4-oxo-1H-quinolin-2-yl)-2-(3-fluorophenyl)ethyl]-4-(3-methyl-1,2,4-triazol-1-yl)benzamideKi3.3 [1]
2-Chloro-N-[(2R)-2-(5,6-dimethyl-1H-benzimidazol-2-yl)-2-phenylethyl]-4-(1,2,4-triazol-4-yl)-6-(trifluoromethyl)benzamideKi21.8 [1]
2-Chloro-N-[(2R)-2-(5,6-dimethyl-1H-benzimidazol-2-yl)-2-pyridin-3-ylethyl]-4-(1,2,4-triazol-4-yl)benzamideKi15.4 [1]
2-Chloro-N-[(2R)-2-(5,6-dimethyl-1H-benzimidazol-2-yl)-2-phenylethyl]-6-methyl-4-(1,2,4-triazol-4-yl)benzamideKi8.0 [1]
2-Chloro-N-[(2R)-2-(5,6-dimethyl-1H-benzimidazol-2-yl)-2-phenylethyl]-6-fluoro-4-(1,2,4-triazol-4-yl)benzamideKi15.2 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Coagulation factor IX Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/coagulation-factor-ix-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 9). Quest Database™ Coagulation factor IX Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/coagulation-factor-ix-inhibitors-ic50-ki.
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