2834087-82-8

HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against WT HIV-1 (IIIB) and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (KD=2.50 μM) and inhibitory activity (IC50=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC50s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056)[1].

HIV-1 (WT): 0.03 μM (IC₅₀); HIV-1 (WT): 2.5 μM (Kd); HIV-1 (L100I): 3.04 nM (EC₅₀); HIV-1 (K103N): 2.87 nM (EC₅₀); HIV-1 (Y181C): 10.2 nM (EC₅₀); HIV-1 (Y188L): 13.2 nM (EC₅₀); HIV-1 (E138K): 9.77 nM (EC₅₀); HIV-1 (F227L+V106A): 19.8 nM (EC₅₀); HIV-1 (RES056): 53.3 nM (EC₅₀)

[1] Yanying Sun, et al. Lead Optimization and Avoidance of Metabolic-perturbing Motif Developing Novel Diarylpyrimidines as Potent HIV-1 NNRTIs. J Med Chem. 2022 Dec 8;65(23):15608-15626. DOI:10.1021/acs.jmedchem.2c00576