Reaction Details |
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Target | Coagulation factor X |
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Ligand | BDBM12709 |
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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 | 1.8±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, Inhibition_Run data, 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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BDBM12709 |
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BDBM12658 |
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Name | BDBM12709 |
Synonyms: | methyl 6-[2-fluoro-4-(2-sulfamoylphenyl)phenyl]-1-(4-methoxyphenyl)-7-oxo-1H,6H,7H-pyrazolo[4,3-d]pyrimidine-3-carboxylate | pyrazolo[4,3-d]pyrimidinone 21 |
Type | Small organic molecule |
Emp. Form. | C26H20FN5O6S |
Mol. Mass. | 549.53 |
SMILES | COC(=O)c1nn(-c2ccc(OC)cc2)c2c1ncn(-c1ccc(cc1F)-c1ccccc1S(N)(=O)=O)c2=O |
Structure |
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