A potent and selective, brain penetrant FAAH inhibitor with IC50 of 11 nM.

BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions.

JNJ-42165279 is a potent and selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH), with an IC50 of 70nM.

LY2183240 is a novel and highly potent blocker of anandamide uptake (IC50 = 270 pM).

URB597 is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets.

PKM-833 (PKM833) is a potent, selective, and orally active FAAH inhibitor with IC50 of 8.8 and 10 nM against human and rat FAAH, respectively.PKM‐833 showed human and rat K inact/K i values with 34 300 ± 10 800 and 128 000 ± 39 800 mol-1 L−1 s-1, respectively.PKM-833 does not inhibit human MAGL and a panel of 137 molecular targets, exhibits weak inhibitory effects (>50%) in five receptor binding assays [PFA, 5‐HT2B, sigma, Na+ channel and Cl‐ channel (GABA gated) at 20 uM.PKM-833 showed excellent brain penetration and good oral bioavailability, and elevated anandamide (AEA) concentrations in the rat brain.PKM-833 significantly attenuated formalin-induced pain responses (3 mg/kg) and improved mechanical allodynia in CFA-induced inflammatory pain (0.3-3 mg/kg) in rat models, without significant side effects on catalepsy and motor coordination up to 30 mg/kg.

Carpro-AM1 is a dual-acting FAAH/substrate-selective COX inhibitor with an IC50 value of 94 nM for FAAH.