Reaction Details |
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Target | Prothrombin |
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Ligand | BDBM12669 |
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Substrate/Competitor | BDBM12678 |
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Meas. Tech. | Enzyme Assay and Determination of the Inhibition Constants. |
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Ki | 200±n/a nM |
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Citation | Quan, ML; Lam, PY; Han, Q; Pinto, DJ; He, MY; Li, R; Ellis, CD; Clark, CG; Teleha, CA; Sun, JH; Alexander, RS; Bai, S; Luettgen, JM; Knabb, RM; Wong, PC; Wexler, RR Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor. J Med Chem48:1729-44 (2005) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Prothrombin |
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Name: | Prothrombin |
Synonyms: | Activation peptide fragment 1 | Activation peptide fragment 2 | Coagulation factor II | F2 | Prothrombin precursor | THRB_HUMAN | Thrombin heavy chain | Thrombin light chain |
Type: | Protein |
Mol. Mass.: | 70029.57 |
Organism: | Homo sapiens (Human) |
Description: | P00734 |
Residue: | 622 |
Sequence: | MAHVRGLQLPGCLALAALCSLVHSQHVFLAPQQARSLLQRVRRANTFLEEVRKGNLEREC
VEETCSYEEAFEALESSTATDVFWAKYTACETARTPRDKLAACLEGNCAEGLGTNYRGHV
NITRSGIECQLWRSRYPHKPEINSTTHPGADLQENFCRNPDSSTTGPWCYTTDPTVRRQE
CSIPVCGQDQVTVAMTPRSEGSSVNLSPPLEQCVPDRGQQYQGRLAVTTHGLPCLAWASA
QAKALSKHQDFNSAVQLVENFCRNPDGDEEGVWCYVAGKPGDFGYCDLNYCEEAVEEETG
DGLDEDSDRAIEGRTATSEYQTFFNPRTFGSGEADCGLRPLFEKKSLEDKTERELLESYI
DGRIVEGSDAEIGMSPWQVMLFRKSPQELLCGASLISDRWVLTAAHCLLYPPWDKNFTEN
DLLVRIGKHSRTRYERNIEKISMLEKIYIHPRYNWRENLDRDIALMKLKKPVAFSDYIHP
VCLPDRETAASLLQAGYKGRVTGWGNLKETWTANVGKGQPSVLQVVNLPIVERPVCKDST
RIRITDNMFCAGYKPDEGKRGDACEGDSGGPFVMKSPFNNRWYQMGIVSWGEGCDRDGKY
GFYTHVFRLKKWIQKVIDQFGE
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BDBM12669 |
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BDBM12678 |
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Name | BDBM12669 |
Synonyms: | 1-(3-Aminobenzisoxazol-5-yl)-3-trifluoromethyl-5-[[(2-methoxy-4-(2-methylimidazol-1-yl)phenyl]aminocarbonyl]pyrazole, Bis(trifluoroacetic acid) Salt | 1-(3-amino-1,2-benzoxazol-5-yl)-N-[2-methoxy-4-(2-methyl-1H-imidazol-1-yl)phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide; bis(2,2,2-trifluoroacetic acid) | Razaxaban Analogue | aminobenzisoxazole 45 |
Type | Small organic molecule |
Emp. Form. | C23H18F3N7O3 |
Mol. Mass. | 497.4293 |
SMILES | COc1cc(ccc1NC(=O)c1cc(nn1-c1ccc2onc(N)c2c1)C(F)(F)F)-n1ccnc1C |
Structure |
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