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2vwz

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2vwz, resolution 1.65Å ()
Ligands: ,
Activity: Receptor protein-tyrosine kinase, with EC number 2.7.10.1
Related: 2bba, 2vx0, 2vwv, 2vwy, 2vww, 2vx1, 2vwx
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



Contents

EPHB4 KINASE DOMAIN INHIBITOR COMPLEX

Publication Abstract from PubMed

Crystallographic studies of a range of 3-substituted anilinopyrimidine inhibitors of EphB4 have highlighted two alternative C-2 aniline conformations and this discovery has been exploited in the design of a highly potent series of 3,5-disubstituted anilinopyrimidines. The observed range of cellular activities has been rationalised on the basis of physicochemical and structural characteristics.

Inhibitors of the tyrosine kinase EphB4. Part 2: structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines., Bardelle C, Coleman T, Cross D, Davenport S, Kettle JG, Ko EJ, Leach AG, Mortlock A, Read J, Roberts NJ, Robins P, Williams EJ, Bioorg Med Chem Lett. 2008 Nov 1;18(21):5717-21. Epub 2008 Sep 27. PMID:18851911

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

About this Structure

2vwz is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

See Also

Reference

  • Bardelle C, Coleman T, Cross D, Davenport S, Kettle JG, Ko EJ, Leach AG, Mortlock A, Read J, Roberts NJ, Robins P, Williams EJ. Inhibitors of the tyrosine kinase EphB4. Part 2: structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines. Bioorg Med Chem Lett. 2008 Nov 1;18(21):5717-21. Epub 2008 Sep 27. PMID:18851911 doi:10.1016/j.bmcl.2008.09.087
  • Bardelle C, Cross D, Davenport S, Kettle JG, Ko EJ, Leach AG, Mortlock A, Read J, Roberts NJ, Robins P, Williams EJ. 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. 2008 May 1;18(9):2776-80. Epub 2008 Apr 10. PMID:18434142 doi:10.1016/j.bmcl.2008.04.015

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