ledgf

Lavendustin B is a Tyrosine Kinase Inhibitor and an inhibitor of HIV-1 integrase (IN) interaction with its cognate cellular cofactor, lens epithelium-derived growth factor (LEDGF/p75).

Integrase-LEDGF/p75 allosteric inhibitor 1 is an orally active inhibitor that targets integrase-LEDGF/p75 (IN-LEDGF/p75), impeding HIV-1 DNA integration and exhibiting antiviral effects against the HIV-1 recombinant molecular clone NL432 with an EC50 of 3.9 nM.

Pirmitegravir (STP0404) is a potent and selective inhibitor of allosteric integrase (ALLINI) targeting the LEDGF/p75 binding site. Pirmitegravir inhibits PBMC. Pirmitegravir inhibits PBMC.Pirmitegravir has significant antiviral activity and may be useful in the study of HIV virus infection.

(±)-BI-D is an effective ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site (IC50: 2.4–2.9 μM).

GS-9822 is a novel LEDGIN, an inhibitor that targets the binding pocket of LEDGF/p75 which is a cellular cofactor that substantially contributes to HIV integration site selection, displaying a block-and-lock phenotype in cell culture.