Reaction Details |
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Target | Coagulation factor X |
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Ligand | BDBM19021 |
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Substrate/Competitor | BDBM12500 |
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Meas. Tech. | Enzyme Assay and Determination of the Inhibition Constants. |
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Ki | 0.47±n/a nM |
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Citation | Pinto, DJ; Orwat, MJ; Koch, S; Rossi, KA; Alexander, RS; Smallwood, A; Wong, PC; Rendina, AR; Luettgen, JM; Knabb, RM; He, K; Xin, B; Wexler, RR; Lam, PY Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa. J Med Chem50:5339-56 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, 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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BDBM19021 |
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BDBM12500 |
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Name | BDBM19021 |
Synonyms: | 1-{4-[1-(4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-6-yl]phenyl}azepan-2-one | trifluoromethylpyrazole analogue, 38b |
Type | Small organic molecule |
Emp. Form. | C26H25F3N4O3 |
Mol. Mass. | 498.4969 |
SMILES | COc1ccc(cc1)-n1nc(c2CCN(C(=O)c12)c1ccc(cc1)N1CCCCCC1=O)C(F)(F)F |
Structure |
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