| Bioactivity | AF64394 is a GPR3 inverse agonist, with a pIC50 of 7.3. | ||||||||||||
| Target | pIC50: 7.3 (GPR3). | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | AF64394 | ||||||||||||
| CAS | 1637300-25-4 | ||||||||||||
| Formula | C21H20ClN5O | ||||||||||||
| Molar Mass | 393.87 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |