Reaction Details |
| Report a problem with these data |
Target | Prothrombin |
---|
Ligand | BDBM50123494 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEBML_208518 |
---|
Ki | 5.2±n/a nM |
---|
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] |
---|
More Info.: | Get all data from this article, 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
|
|
|
BDBM50123494 |
---|
n/a |
---|
Name | BDBM50123494 |
Synonyms: | 2-[6-Chloro-3-(2,2-difluoro-2-pyridin-2-yl-ethylamino)-2-oxo-2H-pyrazin-1-yl]-N-(3-fluoro-pyridin-2-ylmethyl)-acetamide | CHEMBL30054 |
Type | Small organic molecule |
Emp. Form. | C19H16ClF3N6O2 |
Mol. Mass. | 452.818 |
SMILES | Fc1cccnc1CNC(=O)Cn1c(Cl)cnc(NCC(F)(F)c2ccccn2)c1=O |
Structure |
|