JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively.
JAK-IN-21 (Example 4) doses not inhibit CYPs and shows good liver microsome stability[1].
JAK-IN-21 (Example 4) shows low bioavailability (F=1.9%)[1].
References:
[1]. Zhaokui WAN, et al. Benzamides of pyrazolyl-amino-pyrimidinyl derivatives, and compositions and methods thereof. Patent WO2020119819.