Reaction Details |
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Target | Coagulation factor X |
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Ligand | BDBM12728 |
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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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Ki | 2.8±n/a nM |
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Citation | Fevig, JM; Cacciola, J; Buriak, J; Rossi, KA; Knabb, RM; Luettgen, JM; Wong, PC; Bai, SA; Wexler, RR; Lam, PY Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa. Bioorg Med Chem Lett16:3755-60 (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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BDBM12728 |
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BDBM12658 |
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Name | BDBM12728 |
Synonyms: | 1-(4-methoxyphenyl)-4-methyl-6-{4-[2-(pyrrolidin-1-ylmethyl)phenyl]phenyl}-3-(trifluoromethyl)-1H,6H,7H-pyrazolo[3,4-d]pyridazin-7-one | pyrazolo[3,4-d]pyridazinone 46 |
Type | Small organic molecule |
Emp. Form. | C31H28F3N5O2 |
Mol. Mass. | 559.5815 |
SMILES | COc1ccc(cc1)-n1nc(c2c(C)nn(-c3ccc(cc3)-c3ccccc3CN3CCCC3)c(=O)c12)C(F)(F)F |
Structure |
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