AF64394 is a GPR3 inverse agonist, with a pIC50 of 7.3.
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[1].
[1]. Jensen T, et al. The identification of GPR3 inverse agonist AF64394; the first small molecule inhibitor of GPR3 receptor function. Bioorg Med Chem Lett. 2014 Nov 15;24(22):5195-8.