Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode.

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Angell RM, Bamborough P, Cleasby A, Cockerill SG, Jones KL, Mooney CJ, Somers DO, Walker AL

Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):318-23. Epub 2007 Nov 19.

PubMed ID

18006306 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
4-{4-[(5-hydroxy-2-methylphenyl)amino]quinolin-7-yl}-1,3-thiazole-2-carbaldehyde	Mitogen-activated protein kinase 14	Ki (nM)	400	7.5	22	Details
4-{4-[(5-hydroxy-2-methylphenyl)amino]quinolin-7-yl}-1,3-thiazole-2-carbaldehyde	Mitogen-activated protein kinase 14	IC 50 (nM)	2500	7.5	22	Details
N-(3-cyanophenyl)-2'-methyl-5'-(5-methyl-1,3,4-oxadiazol-2-yl)-4-biphenylcarboxamide	Mitogen-activated protein kinase 14	Ki (nM)	240	7.5	22	Details
N-(3-cyanophenyl)-2'-methyl-5'-(5-methyl-1,3,4-oxadiazol-2-yl)-4-biphenylcarboxamide	Mitogen-activated protein kinase 14	IC 50 (nM)	1500	7.5	22	Details
N-(cyclopropylmethyl)-2'-methyl-5'-(5-methyl-1,3,4-oxadiazol-2-yl)biphenyl-4-carboxamide	Mitogen-activated protein kinase 14	Ki (nM)	480	7.5	22	Details
N-(cyclopropylmethyl)-2'-methyl-5'-(5-methyl-1,3,4-oxadiazol-2-yl)biphenyl-4-carboxamide	Mitogen-activated protein kinase 14	IC 50 (nM)	3000	7.5	22	Details