Reaction Details |
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Target | Coagulation factor X |
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Ligand | BDBM12688 |
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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 | 0.26±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 |
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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BDBM12688 |
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BDBM12658 |
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Name | BDBM12688 |
Synonyms: | 1-(3-amino-1,2-benzoxazol-5-yl)-N-(4-{2-[(dimethylamino)methyl]phenyl}-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide | Aminobenzisoxazole 2g | BMS-740808 Analogue 15 |
Type | Small organic molecule |
Emp. Form. | C27H22F4N6O2 |
Mol. Mass. | 538.4962 |
SMILES | CN(C)Cc1ccccc1-c1ccc(NC(=O)c2cc(nn2-c2ccc3onc(N)c3c2)C(F)(F)F)c(F)c1 |
Structure |
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