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HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability[1]. | [IC 50]
HIV-1 (WT): 1.7 nM (EC50); HIV-1 (L100I): 4 nM (EC50); HIV-1 (K103N): 2 nM (EC50); HIV-1 (Y181C): 6 nM (EC50); HIV-1 (E138K): 9 nM (EC50) | [References]
[1] Ding L, et al. Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. J Med Chem. 2022;6 DOI:10.1021/acs.jmedchem.1c01676 |
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