MF63 is a selective mPGES-1 inhibitor with an IC50 of 0.9 nM and 1.3 nM for pig mPGES-1 and human mPGES-1 enzyme respectively.
Atazanavir sulfate (BMS-232632, Reyataz) is an azapeptide inhibitor of HIV-1 protease. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM.
Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin with IC50 values of 90 and 40 nM, targeting the lipid kinase VPS34 with IC50 value of 19 nM in vitro.
AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor with IC50 and Ki of 104 nM and 38 nM, without significant inhibition on 26 other kinases tested.
Pamiparib (BGB-290) is an orally active, potent, highly selective inhibitor of PARP1 and PARP2 with IC50 values of 0.9 nM and 0.5 nM, respectively.
AZD-5069 is a potent CXCR2 chemokine receptor antagonist, and is claimed to be useful in the treatment of inflammatory diseases.
SB 657510 slows development of diabetes-associated atherosclerosis in mouse model of diabetes.
TAK-779 is a potent and selective nonpeptide antagonist of CCR5, with a Ki of 1.1 nM for CCR5.
AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM).
Aconine inhibits NF-κB activation induced by the activator ligand of nuclear factor κB receptor.