GSK3739936 is a potent allosteric inhibitor of HIV-1 integrase, exhibiting an IC50 value of 11.1 nM and an EC50 of 1.7 nM. In addition to its inhibitory effects, GSK3739936 demonstrates weak inhibition of cytochrome P450 enzymes (IC50 > 24.3 μM). This compound also showcases favorable pharmacokinetic properties in preclinical models, characterized by rapid absorption, low to moderate clearance rates, and excellent oral bioavailability, making it a promising candidate for further research in HIV therapeutics.
GSK3739936 is a potent allosteric inhibitor of HIV-1 integrase, exhibiting an IC50 value of 11.1 nM and an EC50 of 1.7 nM. In addition to its inhibitory effects, GSK3739936 demonstrates weak inhibition of cytochrome P450 enzymes (IC50 > 24.3 μM). This compound also showcases favorable pharmacokinetic properties in preclinical models, characterized by rapid absorption, low to moderate clearance rates, and excellent oral bioavailability, making it a promising candidate for further research in HIV therapeutics.
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