Reaction Details |
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Target | Prothrombin |
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Ligand | BDBM50126308 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_208518 |
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Ki | 1.8±n/a nM |
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Citation | Burgey, CS; Robinson, KA; Lyle, TA; Nantermet, PG; Selnick, HG; Isaacs, RC; Lewis, SD; Lucas, BJ; Krueger, JA; Singh, R; Miller-Stein, C; White, RB; Wong, B; Lyle, EA; Stranieri, MT; Cook, JJ; McMasters, DR; Pellicore, JM; Pal, S; Wallace, AA; Clayton, FC; Bohn, D; Welsh, DC; Lynch, JJ; Yan, Y; Chen, Z; Kuo, L; Gardell, SJ; Shafer, JA; Vacca, JP Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides. Bioorg Med Chem Lett13:1353-7 (2003) [PubMed] |
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More Info.: | Get all data from this article, 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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BDBM50126308 |
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n/a |
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Name | BDBM50126308 |
Synonyms: | 2-{6-Chloro-3-[2,2-difluoro-2-(1-oxy-pyridin-2-yl)-ethylamino]-2-oxo-2H-pyrazin-1-yl}-N-[2-(2,2,2-trifluoro-ethoxy)-benzyl]-acetamide | CHEMBL286720 |
Type | Small organic molecule |
Emp. Form. | C22H19ClF5N5O4 |
Mol. Mass. | 547.862 |
SMILES | [O-][n+]1ccccc1C(F)(F)CNc1ncc(Cl)n(CC(=O)NCc2ccccc2OCC(F)(F)F)c1=O |
Structure |
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