Reaction Details |
| Report a problem with these data |
Target | Prothrombin |
---|
Ligand | BDBM12659 |
---|
Substrate/Competitor | BDBM12678 |
---|
Meas. Tech. | Enzyme Assay and Determination of the Inhibition Constants. |
---|
Ki | 6300±n/a nM |
---|
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 |
---|
More Info.: | Get all data from this article, Solution Info, Assay Method |
---|
|
Prothrombin |
---|
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
|
|
|
BDBM12659 |
---|
BDBM12678 |
---|
Name | BDBM12659 |
Synonyms: | 1-(3-Aminobenzisoxazol-5-yl)-3-trifluoromethyl-5-[(2-methylsulfonyl-3-fluoro[1,1]biphen-4-yl)aminocarbonyl]-pyrazole, Trifluoroacetic Acid | 1-(3-amino-1,2-benzoxazol-5-yl)-N-[2-fluoro-4-(2-methanesulfonylphenyl)phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide; 2,2,2-trifluoroacetic acid | CHEMBL554926 | Razaxaban Analogue | aminobenzisoxazole 38 |
Type | Small organic molecule |
Emp. Form. | C25H17F4N5O4S |
Mol. Mass. | 559.492 |
SMILES | CS(=O)(=O)c1ccccc1-c1ccc(NC(=O)c2cc(nn2-c2ccc3onc(N)c3c2)C(F)(F)F)c(F)c1 |
Structure |
|