Structural highlights
2xvd is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
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| Ligands: | , |
| Related: | 2x9f, 2bba, 2vwu, 2vx0, 2vwv, 2vwz, 2vwy, 2vww, 2vwx, 2vx1 |
| Activity: | Receptor protein-tyrosine kinase, with EC number 2.7.10.1 |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
Publication Abstract from PubMed
Optimization of our bis-anilino-pyrimidine series of EphB4 kinase inhibitors led to the discovery of compound 12 which incorporates a key m-hydroxymethylene group on the C4 aniline. 12 displays a good kinase selectivity profile, good physical properties and pharmacokinetic parameters, suggesting it is a suitable candidate to investigate the therapeutic potential of EphB4 kinase inhibitors.
Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series.,Barlaam B, Ducray R, Lambert-van der Brempt C, Ple P, Bardelle C, Brooks N, Coleman T, Cross D, Kettle JG, Read J Bioorg Med Chem Lett. 2011 Apr 15;21(8):2207-11. PMID:21441027[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Barlaam B, Ducray R, Lambert-van der Brempt C, Ple P, Bardelle C, Brooks N, Coleman T, Cross D, Kettle JG, Read J. Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2207-11. PMID:21441027 doi:10.1016/j.bmcl.2011.03.009
