PH-797804

PH-797804 is a highly selective and potent small molecule inhibitor of p38 mitogen-activated protein kinase (MAPK), specifically targeting the alpha (p38α) and beta (p38β) isoforms. It acts as an ATP-competitive inhibitor with high selectivity for p38α over other kinases, including JNK2. The compound is a diarylpyridinone derivative and exists as two atropisomers; the active form is the aS isomer, which demonstrates significantly greater potency than its counterpart. Developed by Pfizer, PH-797804 was investigated primarily for inflammatory diseases such as osteoarthritis, rheumatoid arthritis, chronic obstructive pulmonary disease (COPD), musculoskeletal pain, and neuropathic pain. Despite promising preclinical and early clinical results showing strong anti-inflammatory effects through inhibition of cytokine production in human whole blood assays, development was discontinued before reaching approval[1][3][5][6][7][8].

Other names

10 mg-Pfizer-Chronic Obstructive Pulmonary Disease3-(3-Bromo-4-((2,4-difluorobenzyl)oxy)-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide