Reaction Details |
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Target | Coagulation factor X |
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Ligand | BDBM18971 |
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Substrate/Competitor | BDBM12500 |
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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 | 11±n/a nM |
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Citation | Lam, PY; Clark, CG; Li, R; Pinto, DJ; Orwat, MJ; Galemmo, RA; Fevig, JM; Teleha, CA; Alexander, RS; Smallwood, AM; Rossi, KA; Wright, MR; Bai, SA; He, K; Luettgen, JM; Wong, PC; Knabb, RM; Wexler, RR Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants. J Med Chem46:4405-18 (2003) [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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BDBM18971 |
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BDBM12500 |
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Name | BDBM18971 |
Synonyms: | 1-(4-methoxyphenyl)-3-methyl-N-[4-(2-sulfamoylphenyl)phenyl]-1H-pyrazole-5-carboxamide | CHEMBL139788 | pyrazole-based inhibitor, 22a |
Type | Small organic molecule |
Emp. Form. | C24H22N4O4S |
Mol. Mass. | 462.521 |
SMILES | COc1ccc(cc1)-n1nc(C)cc1C(=O)Nc1ccc(cc1)-c1ccccc1S(N)(=O)=O |
Structure |
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