Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode.
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.
Angell
Richard M
RM
GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.
Bamborough
Paul
P
Cleasby
Anne
A
Cockerill
Stuart G
SG
Jones
Katherine L
KL
Mooney
Christopher J
CJ
Somers
Donald O
DO
Walker
Ann L
AL
D000577:Amides / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001713:Biphenyl Compounds / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D008958:Models, Molecular; D008968:Molecular Conformation; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D048051:p38 Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism
D000577:Amides; D001713:Biphenyl Compounds; D047428:Protein Kinase Inhibitors; D048051:p38 Mitogen-Activated Protein Kinases