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TargetProthrombin
LigandBDBM12676
Substrate/CompetitorBDBM12678
Meas. Tech.Enzyme Assay and Determination of the Inhibition Constants.
pH7±n/a
Temperature295.15±n/a K
Ki 540±n/a nM
Citation Fevig, JMCacciola, JBuriak, JRossi, KAKnabb, RMLuettgen, JMWong, PCBai, SAWexler, RRLam, 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
More Info.:Get all data from this article,  Inhibition_Run data,   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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM12676
BDBM12678
NameBDBM12676
Synonyms:1-(3-Aminobenzisoxazol-5-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide Hydrochloride Salt | 1-(3-amino-1,2-benzoxazol-5-yl)-N-(4-{2-[(dimethylamino)methyl]-1H-imidazol-1-yl}-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide | BMS-561389 | CHEMBL206335 | CHEMBL558198 | DPC 906 | Razaxaban
TypeSmall organic molecule
Emp. Form.C24H20F4N8O2
Mol. Mass.528.4616
SMILESCN(C)Cc1nccn1-c1ccc(NC(=O)c2cc(nn2-c2ccc3onc(N)c3c2)C(F)(F)F)c(F)c1
Structure
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