| Reaction Details |
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 | Report a problem with these data |
| Target | Coagulation factor X |
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| Ligand | BDBM12749 |
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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 | 0.2±n/a nM |
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| Citation |  Pinto, DJ; Galemmo, RA; Quan, ML; Orwat, MJ; Clark, C; Li, R; Wells, B; Woerner, F; Alexander, RS; Rossi, KA; Smallwood, A; Wong, PC; Luettgen, JM; Rendina, AR; Knabb, RM; He, K; Wexler, RR; Lam, PY Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties. Bioorg Med Chem Lett16:5584-9 (2006) [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 |
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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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| BDBM12749 |
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| BDBM12658 |
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| Name | BDBM12749 |
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| Synonyms: | 1-(2-amino-4-methoxyphenyl)-6-[4-(2-methanesulfonylphenyl)phenyl]-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one | dihydropyrazolopyridinone analogue 8f |
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| Type | Small organic molecule |
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| Emp. Form. | C27H23F3N4O4S |
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| Mol. Mass. | 556.556 |
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| SMILES | COc1ccc(c(N)c1)-n1nc(c2CCN(C(=O)c12)c1ccc(cc1)-c1ccccc1S(C)(=O)=O)C(F)(F)F |
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| Structure | 
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