Reaction Details |
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Target | Prothrombin |
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Ligand | BDBM14501 |
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Substrate/Competitor | BDBM12678 |
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Meas. Tech. | TF-VIIa Assay |
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IC50 | 150±n/a nM |
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Citation | Parlow, JJ; Case, BL; Dice, TA; Fenton, RL; Hayes, MJ; Jones, DE; Neumann, WL; Wood, RS; Lachance, RM; Girard, TJ; Nicholson, NS; Clare, M; Stegeman, RA; Stevens, AM; Stallings, WC; Kurumbail, RG; South, MS Design, parallel synthesis, and crystal structures of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex. J Med Chem46:4050-62 (2003) [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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BDBM14501 |
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BDBM12678 |
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Name | BDBM14501 |
Synonyms: | N-[(6-carbamimidoylpyridin-3-yl)methyl]-2-{2-oxo-6-phenyl-3-[(2-phenylethyl)amino]-1,2-dihydropyrazin-1-yl}acetamide | Pyrazinone Analog 24d |
Type | Small organic molecule |
Emp. Form. | C27H27N7O2 |
Mol. Mass. | 481.549 |
SMILES | NC(=N)c1ccc(CNC(=O)Cn2c(cnc(NCCc3ccccc3)c2=O)-c2ccccc2)cn1 |
Structure |
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