2VWW

ephB4 kinase domain inhibitor complex

Summary for 2VWW

• Entry DOI: 10.2210/pdb2vww/pdb
• Related: 2BBA 2VWU 2VWV 2VWX 2VWY 2VWZ 2VX0 2VX1
• Descriptor: EPHRIN TYPE-B RECEPTOR 4, N'-(5-CHLORO-1,3-BENZODIOXOL-4-YL)-N-(3,4,5- TRIMETHOXYPHENYL)PYRIMIDINE-2,4-DIAMINE (3 entities in total)
• Functional Keywords: tyrosine-protein kinase, receptor tyrosine kinase, kinase, mutant, membrane, receptor, transferase, atp-binding, polymorphism, glycoprotein, transmembrane, phosphoprotein, unphosphorylated, nucleotide-binding
• Biological source: HOMO SAPIENS (HUMAN)
• Total number of polymer chains: 1
• Total formula weight: 34365.66

Authors

Read, J.,Brassington, C.A.,Green, I.,McCall, E.J.,Valentine, A.L.,Barratt, D.,Leach, A.G.,Kettle, J.G. (deposition date: 2008-06-27, release date: 2008-07-08, Last modification date: 2023-12-13)

Primary citation

Bardelle, C.,Cross, D.,Davenport, S.,Kettle, J.G.,Ko, E.J.,Leach, A.G.,Mortlock, A.,Read, J.,Roberts, N.J.,Robins, P.,Williams, E.J.
Inhibitors of the Tyrosine Kinase Ephb4. Part 1: Structure-Based Design and Optimization of a Series of 2,4-Bis-Anilinopyrimidines
Bioorg.Med.Chem.Lett., 18:2776-, 2008

PubMed Abstract: A series of bis-anilinopyrimidines have been identified as potent inhibitors of the tyrosine kinase EphB4. Structural information from two alternative series identified from screening efforts was combined to identify the initial leads.

PubMed: 18434142
DOI: 10.1016/J.BMCL.2008.04.015

Experimental method

X-RAY DIFFRACTION (1.9 Å)