NBD-14189

NBD-14189 is a potent HIV-1 entry antagonist with an IC50 of 89 nM against the HIV-1HXB2 pseudovirus. NBD-14189 binds to HIV-1 gp120 and shows potent antiviral activity (EC50<200 nM)[1][2].

Signaling Pathways >> Anti-infection >> HIV

Research Areas >> Infection

HIV-1

NBD-14189 has anti-HIV-1 activity (IC50=0.089 μM) and cytotoxicity (CC50=21.9 μM) in single-cycle (TZM-bl cells) assays. NBD-14189 has anti-HIV-1 activity (IC50=0.18 μM) and cytotoxicity (CC50=22.1 μM) in multi-cycle (MT-2 cells) assays[1]. NBD-14189 (0-50 μM) prevents HIV-1 mediated cell-cell fusion with an IC50 of 9.4 μM in indicator cells TZM-bl cells were cocultured with Env- and Tat-expressing HL2/3 cells[1]. NBD-14189 shows weak or no inhibition of the hERG current, with an IC50 of 3.0 μM, respectively[1].

[1]. Francesca Curreli, et al. Structure-based lead optimization to improve antiviral potency and ADMET properties of phenyl-1H-pyrrole-carboxamide entry inhibitors targeted to HIV-1 gp120. Eur J Med Chem. 2018 Jun 25;154:367-391.

[2]. Natalie Losada, et al. HIV-1 gp120 Antagonists Also Inhibit HIV-1 Reverse Transcriptase by Bridging the NNRTI and NRTI Sites. J Med Chem. 2021 Nov 25;64(22):16530-16540.