EUB0000306b_FAAH

Functional proteomic screen, testet at 10 µM and 100 µM, PF-04457845 showed exquisite selectivity for FAAH relative to other mammalian serine hydrolases (no targets up to 100 µM); Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest targets as % of contr.: KIT(L576P) (0%), TAOK3 (42%), PIK3CA (45%); Screened against 45 GPCR targets (PDSP screen) at 10 µM, closest targets: Ki(HTR2A) = 248.71 nM, Ki(TMEM97) = 436.72 nM, Ki(SIGMAR1) = 472.06 nM, Ki(ADRA2C) = 595.66 nM, Ki(GABA/ PBR) = 1140.08 nM; Screened in CEREP ligand profiling, panel of 68 ion channels, GPCRS and transporters at 10 µM, closest target: Ki(HTR2A) =1.6 µM;