Ensartinib dihydrochloride is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations.

Potent, high affinity apelin receptor agonist (IC50 = 0.27 nM; Kd = 0.51 nM). Exhibits no binding GPR15 and GPR25. Activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. Also potentiates the TGFβ pathway, priming hESCs toward the endoderm lineage. Stimulates angiogenesis in HUVEC cells. Relaxes mouse aortic vessels. Functions as an anorexigenic hormone through activation of the AVP and CRH neurons in the PVN.

UK-396082 is a potent and selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (activated TAFI; TAFIa) with Ki of 10 nM.