| Reaction Details |
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 | Report a problem with these data |
| Target | Coagulation factor X |
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| Ligand | BDBM12687 |
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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 | 0.25±n/a nM |
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| Citation |  Pinto, DJ; Orwat, MJ; Quan, ML; Han, Q; Galemmo, RA; Amparo, E; Wells, B; Ellis, C; He, MY; Alexander, RS; Rossi, KA; Smallwood, A; Wong, PC; Luettgen, JM; Rendina, AR; Knabb, RM; Mersinger, L; Kettner, C; Bai, S; He, K; Wexler, RR; Lam, PY 1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa. Bioorg Med Chem Lett16:4141-7 (2006) [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 |
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| 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 |
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| Type: | Enzyme |
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| Mol. Mass.: | 54726.60 |
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| Organism: | Homo sapiens (Human) |
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| Description: | n/a |
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| Residue: | 488 |
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| Sequence: | MGRPLHLVLLSASLAGLLLLGESLFIRREQANNILARVTRANSFLEEMKKGHLERECMEE
TCSYEEAREVFEDSDKTNEFWNKYKDGDQCETSPCQNQGKCKDGLGEYTCTCLEGFEGKN
CELFTRKLCSLDNGDCDQFCHEEQNSVVCSCARGYTLADNGKACIPTGPYPCGKQTLERR
KRSVAQATSSSGEAPDSITWKPYDAADLDPTENPFDLLDFNQTQPERGDNNLTRIVGGQE
CKDGECPWQALLINEENEGFCGGTILSEFYILTAAHCLYQAKRFKVRVGDRNTEQEEGGE
AVHEVEVVIKHNRFTKETYDFDIAVLRLKTPITFRMNVAPACLPERDWAESTLMTQKTGI
VSGFGRTHEKGRQSTRLKMLEVPYVDRNSCKLSSSFIITQNMFCAGYDTKQEDACQGDSG
GPHVTRFKDTYFVTGIVSWGEGCARKGKYGIYTKVTAFLKWIDRSMKTRGLPKAKSHAPE
VITSSPLK
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| BDBM12687 |
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| BDBM12658 |
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| Name | BDBM12687 |
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| Synonyms: | 1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-{2-[(dimethylamino)methyl]phenyl}phenyl)-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[4,3-d]pyrimidin-7-one | BMS-740808 Analogue 18 | dihydropyrazolo[4,3-d]pyrimidinone 24a |
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| Type | Small organic molecule |
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| Emp. Form. | C28H24F3N7O2 |
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| Mol. Mass. | 547.5311 |
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| SMILES | CN(C)Cc1ccccc1-c1ccc(cc1)N1CNc2c(nn(c2C1=O)-c1ccc2onc(N)c2c1)C(F)(F)F |
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| Structure | 
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