Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode

Richard M Angell; Paul Bamborough; Anne Cleasby; Stuart G Cockerill; Katherine L Jones; Christopher J Mooney; Donald O Somers; Ann L Walker

doi:10.1016/j.bmcl.2007.10.076

Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode

Bioorg Med Chem Lett. 2008 Jan 1;18(1):318-23. doi: 10.1016/j.bmcl.2007.10.076. Epub 2007 Nov 19.

Authors

Richard M Angell¹, Paul Bamborough, Anne Cleasby, Stuart G Cockerill, Katherine L Jones, Christopher J Mooney, Donald O Somers, Ann L Walker

Affiliation

¹ GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.

PMID: 18006306
DOI: 10.1016/j.bmcl.2007.10.076

Abstract

The biphenyl amides (BPAs) are a novel series of p38 MAP kinase inhibitors. The discovery of the series through structure-based focused screening is described, and the binding mode of the compounds is explained with reference to X-ray crystal structures.

MeSH terms

Amides / chemistry
Amides / metabolism
Amides / pharmacology*
Biphenyl Compounds / chemistry
Biphenyl Compounds / metabolism
Biphenyl Compounds / pharmacology*
Crystallography, X-Ray
Models, Molecular
Molecular Conformation
Protein Binding
Protein Kinase Inhibitors / chemistry
Protein Kinase Inhibitors / metabolism
Protein Kinase Inhibitors / pharmacology*
Structure-Activity Relationship
p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors*
p38 Mitogen-Activated Protein Kinases / chemistry
p38 Mitogen-Activated Protein Kinases / metabolism

Substances

Amides
Biphenyl Compounds
Protein Kinase Inhibitors
p38 Mitogen-Activated Protein Kinases

Associated data

PDB/2ZAZ
PDB/2ZB0
PDB/2ZB1