TAK-220 is a selective and orally bioavailable CCR5 antagonist (IC50s: 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively).
Fuscin is a quinonoid fungal metabolite originally isolated from O. fuscum that has diverse biological activities. It inhibits binding of the ADP/ATP translocase inhibitor atractyloside to rat liver mitochondria in an ADP-dependent manner when used at a concentration of 50 μM in a radioligand binding assay. Fuscin (20 μM) reduces the glutathione content of rat liver mitochondria to 28% of controls and inhibits NADH oxidation in sonicated pigeon heart mitochondria preparations in a concentration-dependent manner. It competes with macrophage inflammatory protein 1α (MIP-1α) for binding to CCR5 chemokine receptors in vitro with an IC50 value of 21 μM.