JTP-0157602 (JTP0157602) is a novel non-catalytic site integrase inhibitor of HIV-1 integrase (IN), inhibits the interaction between LEDGF IBD and IN with IC50 of 4.2 nM.JTP-0157602 exhibits potent antiviral activity against HIV-1 with EC90 of 138 nM.JTP-0157602 retained potent antiviral activity (EC50=1-6 nM) against a broad panel of recombinant viruses with INSTI-related resistant mutations, including multiple substitutions that emerged in clinical studies of INSTIs (IN strand transfer inhibitors (INSTIs).JTP-0157602 inhibited HIV-1 replication mainly during the late-phase of the replication cycle.JTP-0157602 binds to the LEDGF/p75 binding pocket of HIV-1 integrase (IN).

HIV-1 Integrase inhibitor GS-B (GS-B) is a novel non-catalytic site integrase inhibitor of HIV-1 integrase (IN), inhibits the interaction between LEDGF IBD and IN with IC50 of 8.1 nM.GS-B displays antiviral potency in MT-4, MT-2, and human PBMCs with EC50 values of 18, 10, and 21 nM, respectively.

HIV-1 inhibitor 5b is a novel anti-HIV-1 compound that inhibits HIV-1 JR-CSF with EC50 of 1 nM without significant cytotoxicity (CC50>20 uM), also shows potency against NRTI- and NNRTI-resistant HIV-1 (EC50=1-3 nM); shows a chemical backbone similar to the clinically used integrase (IN) strand transfer inhibitor (INSTI) elvitegravir, but has no detectable INSTI activity; various drug-resistant HIV-1 strains did not display cross resistance to HIV-1 inhibitor 5b; remains its anti-HIV-1 activity even after the viral integration stage, significantly suppresses p24 antigen production in HIV-1 latently infected cells exposed with TNF-alpha; demonstrates favorable pharmacokinetic profiles in mice.

GSK3739936 (BMS-986180) is a potent, allosteric HIV-1 integrase (ALLINI), shows excellent potency in vitro against majority of the 124/125 variants (EC50=1.7 nM).

GRL-079 is a novel potent, nonpeptidic HIV-1 protease inhibitor with 2.5-30 nM against wild-type HIV-1NL4-3, 0.3-6.7 nM against HIV-2EHO, and 0.9-90 nM against laboratory-selected-PI-resistant HIV-1 and clinical HIV-1 variants resistant to multiple FDA-approved PIs (HIVMDR).

FD028 is a small-molecule HIV-1 inactivator by conjugating FD016 (gp120-CD4 binding inhibitor) with FD017 (HIV-1 fusion inhibitor), inactivates cell-free virions (IC50=0.7 uM) of by targeting both HIV-1 gp120 and gp41.FD028 is not significantly toxic and has broad-spectrum HIV-1 inhibitory and inactivation activity, including T20-resistant viruses and T2635-resistant viruses.

FC-8052 (FC8052) is a highly potent inhibitor of HIV-1 Nef-effector kinase, binds to recombinant Nef in vitro with Kd of 10 pM; FC-8052 inhibits Nef-dependent HIV-1 replication in PBMCs in the subnanomolar range.

Ciapavir (SBI-0953294, cIAP1 antagonist for viral reactivation) is a bivalent, next-generation, Smac mimetic and antagonist of cIAP1 as latency-reversing agent (LRA), specifically and potently promote HIV-1 latency reversal activity both in vivo.Ciapavir's latency reversal activity is dependent on the NIK-dependent NF-κB signaling.Ciapavir exhibits substantially greater potency and efficacy as an LRA, inducing comparable levels of latency reversal at concentrations 10- to 1,000-fold lower than the first-generation molecule SBI-0637142, without an increase in cytotoxicity.Ciapavir does not trigger cytokine release or T cell activation.Ciapavir is capable of increasing latent HIV-1 expression in ART-treated BLT mice in vivo and may therefore prove useful in "shock and kill" approaches to HIV-1 cure.

ACAi-028 is a small molecule inhibiting HIV-1 replication (EC50=0.55 uM) that targets a hydrophobic pocket in the N-terminal domain of capsid (CA-NTD).ACAi-028 binds directly and noncovalently to HIV-1 capsid monomer.ACAi-028 inhibits the early stage of the HIV-1 life cycle and does not affect the late stage, also prevents multiple-round HIV-1 infection using HIV-1 strains (HIV-1NL4-3 and HIV-1LAI), except for HIV-2 strain (HIV-2ROD).ACAi-028 inhibits the replication of various types of HIV-1 strains (HIV-1104pre and HIV-1MDR/B) in PBMCs and HIV-1ATVR5μM in MT-4 cells, with negligible cytotoxicity.

A small molecule CD4-mimetic that binds gp120 and blocks CD4 binding, inhibits HIV-1 entry.

AIC-292 is a potent and selective inhibitor of HIV-1 nonnucleoside reverse transcriptase. AIC-292 inhibits wild-type HIV-1 laboratory strains at low nanomolar concentrations. AIC-292 displays potent antiviral in vivo efficacy in a mouse xenograft model. AIC-292 has the potential for the research of HIV-1 infection.

Darunavir ethanolate is an HIV protease inhibitor,showed potent activity against COVID-19(SARS-COV-2).

Nelfinavir(AG-1341) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection.

Epicoccone B, firstly reported from C. globosum, exhibits the DPPH free radical scavenging ability with IC50 value of 10.8 μM, and has potent α-glucosidase inhibition with IC50 value of 27.3 μM. Anti-HIV activity.

HIV-1 inhibitor-11, a fused pyridine ring derivative, is a HIV-1 inhibitor. WO2021104413A1 ( compound 1-1b).

HIV-1 inhibitor-12 is potent HIV-1 inhibitor. HIV-1 inhibitor-12 inhibits HIV-1 capsid protein polymerization with an IC50 of 9 nM (WO2021104413A1, compound 1-1a).

NBD-14270, a pyridine analogue, is a potent HIV-1 entry antagonist with an IC50 of 180 nM against 50 HIV-1 Env-pseudotyped viruses. NBD-14270 binds to HIV-1 gp120 and shows potent antiviral activity. NBD-14270 shows low cytotoxicity (CC50>100 μM).

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).

BMS-707035 is a potent, specific, and reversible HIV-I integrase (IN) inhibitor that blocks HIV IN strand transfer activity.

Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties.

Claficapavir (A1752) is a specific nucleocapsid protein (NC) inhibitor with an IC50 around 1 μM. Claficapavir strongly binds the HIV-1 NC (Kd=20 nM) thereby inhibiting the chaperone properties of NC and leading to good antiviral activity against the HIV-1.

Amphotericin B methyl ester hydrochloride is the methyl ester derivative of the polyene antibiotic Amphotericin B (A634250). Amphotericin B methyl ester hydrochloride is the cholesterol-binding compound possesses significant antifungal activity. Amphotericin B methyl ester hydrochloride disrupts HIV-1 particle production and potently inhibits HIV-1 replication.

Decanoyl-RVKR-CMK (DecRVKRcmk) TFA inhibits over-expressed gp160 processing and HIV-1 replication.

HIV-1 inhibitor-10 is a nanomolar HIV-1 maturation inhibitor.

Dolutegravir (DTG, GSK1349572) is an integrase inhibitor(IC50= 2.7 nM), modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.

Dolutegravir is a HIV integrase inhibitor with IC50 of 2.7 nM.

A new-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of HIV-1 infections, the prodrug of the active compound VM-1500A..

β-Rubromycin is a potent and selective inhibitor of human immunodeficiency virus-1 (HIV-1) RNA-directed DNA polymeras (reverse transcriptase). β-Rubromycin is a class of quinone antibacterials.

Bictegravir (GS-9883) Sodium is a novel and potent inhibitor of HIV-1 integrase, specifically targets IN strand transfer activity with an IC50 of 7.5 nM.

Tenofovir-C3-O-C15-CF3 (ammonium) exhibits substantially longer t1/2 values than tenofovir in human liver microsomes, potent anti-HIV activity in vitro, and enhances pharmacokinetic properties in vivo.