AF64394 is a selective GPR3 Inverse Agonist. It is the first small molecule inhibitor of GPR3 receptor function.
AF64394 is a GPR3 inverse agonist, with a pIC50 of 7.3. AF34394 and related compounds are only of modest potency and are relatively lipophilic (e.g., AF34394 clogP=5.2, LLE=2.1, and 14b clog P=3.1 and LLE=3.2) the series shows promising SAR and represents an excellent start point for further optimization.
Synonyms:
[1,2,4]Triazolo[1,5-a]pyrimidin-7-amine, N-[[4-chloro-2-(1-methylethoxy)phenyl]methyl]-5-phenyl-;
N-[[4-Chloro-2-(1-methylethoxy)phenyl]methyl]-5-phenyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine;