Reaction Details |
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Target | Coagulation factor X |
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Ligand | BDBM12675 |
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Substrate/Competitor | BDBM12658 |
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Meas. Tech. | Enzyme Assay and Determination of the Inhibition Constants. |
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pH | 7±n/a |
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Temperature | 295.15±n/a K |
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Ki | 0.17±n/a nM |
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Citation | Quan, ML; Lam, PY; Han, Q; Pinto, DJ; He, MY; Li, R; Ellis, CD; Clark, CG; Teleha, CA; Sun, JH; Alexander, RS; Bai, S; Luettgen, JM; Knabb, RM; Wong, PC; Wexler, RR Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor. J Med Chem48:1729-44 (2005) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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Coagulation factor X |
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Name: | Coagulation factor X |
Synonyms: | Activated coagulation factor X (FXa) | Activated factor Xa heavy chain | Coagulation factor X precursor | Coagulation factor Xa | F10 | FA10_HUMAN | Factor X heavy chain | Factor X light chain | Factor Xa | Stuart factor | Stuart-Prower factor |
Type: | Enzyme |
Mol. Mass.: | 54726.60 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 488 |
Sequence: | MGRPLHLVLLSASLAGLLLLGESLFIRREQANNILARVTRANSFLEEMKKGHLERECMEE
TCSYEEAREVFEDSDKTNEFWNKYKDGDQCETSPCQNQGKCKDGLGEYTCTCLEGFEGKN
CELFTRKLCSLDNGDCDQFCHEEQNSVVCSCARGYTLADNGKACIPTGPYPCGKQTLERR
KRSVAQATSSSGEAPDSITWKPYDAADLDPTENPFDLLDFNQTQPERGDNNLTRIVGGQE
CKDGECPWQALLINEENEGFCGGTILSEFYILTAAHCLYQAKRFKVRVGDRNTEQEEGGE
AVHEVEVVIKHNRFTKETYDFDIAVLRLKTPITFRMNVAPACLPERDWAESTLMTQKTGI
VSGFGRTHEKGRQSTRLKMLEVPYVDRNSCKLSSSFIITQNMFCAGYDTKQEDACQGDSG
GPHVTRFKDTYFVTGIVSWGEGCARKGKYGIYTKVTAFLKWIDRSMKTRGLPKAKSHAPE
VITSSPLK
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BDBM12675 |
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BDBM12658 |
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Name | BDBM12675 |
Synonyms: | 1-(3-amino-1,2-benzoxazol-5-yl)-N-(2-fluoro-4-{2-[(methylamino)methyl]-1H-imidazol-1-yl}phenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide; bis(2,2,2-trifluoroacetic acid) | N-[4-(2-{[Methylamino]methyl}-1H-imidazol-1-yl)-2-fluorophenyl]-1-(3-amino-1,2-benzisoxazol-5-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide, Bis(trifluoroacetic acid) Salt | Razaxaban Analogue | aminobenzisoxazole 12 |
Type | Small organic molecule |
Emp. Form. | C23H18F4N8O2 |
Mol. Mass. | 514.435 |
SMILES | CNCc1nccn1-c1ccc(NC(=O)c2cc(nn2-c2ccc3onc(N)c3c2)C(F)(F)F)c(F)c1 |
Structure |
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