Aprepitant 126(ZZ) Selective for Bcr-abl over a

Selective for Bcr-abl over a panel of serine

Epub 2014 Mar 17

4-bis(3-methylthiophen-2-yl)but-3-en-1-yl)piperidine-3-carboxylic acid hydrochloride

ALK5 and ALK7 (IC50≥500 nM) and increases selectivity for BMP signaling versus AMP-activated protein kinase

Aprepitant 126(ZZ) Selective for Bcr-abl over aAprepitant is a small molecule, high affinity substance P antagonist (SPA) with antiemetic activity. Crossing the blood brain barrier, aprepitant binds selectively to the human substance P neurokinin 1 receptor in the central nervous system (CNS), thereby inhibiting receptor binding of endogenous substance P and substance P induced emesis. This agent has little or no affinity for serotonin type 3 (5 HT3), dopamine, and corticosteroid receptors.