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HIV Protease Inhibitor
Saquinavir is a protease inhibitor. Proteases are enzymes that cleave protein molecules into smaller fragments. Saquinavir inhibits both HIV-1 and HIV-2 proteases.- Ernawati Arifin Giri-Rachman, .et al. , ACS Synth Biol, 2024, Feb 16; 13(2): 509-520 PMID: 38316139
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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HIV-1 protease inhibitor
Nelfinavir 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.- Joanna Ireland, .et al. , Front Microbiol, 2024, Mar 20:15:1385775 PMID: 38572241
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
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HIV integrase inhibitor
S/GSK1349572 is a potent next generation HIV integrase inhibitor and demonstrates a superior resistance profile substantiated with 60 integrase mutant molecular clones.- Lea El Khoury, .et al. , PeerJ Preprints, 2019, 7:e27833v1
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HIV integrase inhibitor
Elvitegravir (GS-9137) is a potent inhibitor of the strand-transfer step of integration mediated by human immunodeficiency virus type 1 (HIV-1) integrase.- Lea El Khoury, .et al. , PeerJ Preprints, 2019, 7:e27833v1
- El Khoury L, .et al. , Biochem Biophys Res Commun, 2017, Jul 1;488(3):433-438 PMID: 28478035
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HIV-1 integrase Inhibitor
Bictegravir, also known as GS-9883, is a potent, unboosted, once-Daily HIV-1 Integrase Strand Transfer Inhibitor (INSTI) (IC50 - 1.6 nM) with improved pharmacokinetics and in vitro resistance profile.- Michal S Barski, .et al. , Nat Commun, 2021, Aug 17;12(1):4996 PMID: 34404793
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HIV-1 integrase inhibitor
Raltegravir (MK-0518) targets integrase, an HIV enzyme that integrates the viral genetic material into human chromosomes, a critical step in the pathogenesis of HIV.- Min Li, .et al. , J Infect Dis, 2025, Jul 16:jiaf373
- Joanna Ireland, .et al. , Front Microbiol, 2024, Mar 20:15:1385775 PMID: 38572241
- Michal S Barski, .et al. , Nat Commun, 2021, Aug 17;12(1):4996 PMID: 34404793
- Lea El Khoury, .et al. , PeerJ Preprints, 2019, 7:e27833v1
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HIV-1 attachment inhibitor
BMS-663068 is an HIV-1 attachment inhibitor in development for the treatment of HIV-1 infection.- Min Li, .et al. , J Infect Dis, 2025, Jul 16:jiaf373
- Min Li, .et al. , Nat Commun, 2020, 11: 4051 PMID: 32792548
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HIV-1 maturation inhibitor
Bevirimat (MPC-4326, PA-457, YK-FH312) is a first-in-class HIV-1 maturation inhibitor that demonstrates high potency in cell culture and has shown clinical efficacy in HIV-1-infected patients.- Mingzhang Wang, .et al. , Nat Commun, 2017, 8: 1779 PMID: 29176596
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HIV-1 production Inhibitor
Baicalin is a known prolyl endopeptidase inhibitor and affects the GABA receptors.- Shoichi Ozawa, .et al. , Sci Rep, 2019, 9: 15464 PMID: 31664047
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HIV Protease inhibitor
Atazanavir is an antiretroviral drug of the protease inhibitor (PI) class. Like other antiretrovirals, it is used to treat infection of human immunodeficiency virus (HIV). -
HIV Protease inhibitor
Atazanavir is an antiretroviral drug of the protease inhibitor (PI) class. Like other antiretrovirals, it is used to treat infection of human immunodeficiency virus (HIV). -
HIV-1 integrase inhibitor
BMS-707035 is an HIV-1 integrase (IN) inhibitor. HIV-1 integrase (IN) represents a therapeutically advantageous viral target to treat HIV/AIDS in the clinic.
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HIV Protease inhibitor
Ritonavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease.Ritonavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles. -
HIV reverse transcriptase inhibitor
Tenofovir is in a class of medications called nucleoside reverse transcriptase inhibitors (NRTIs). It works by decreasing the amount of HIV in the blood. -
HIV replication inhibitor
Feglymycin is a HIV replication inhibitor. Feglymycin is also an antibiotic peptide that has antibacterial activity (MIC: 32-64 μg/mL for Staphylococcus aureus). -
anti-HIV-1 fusion inhibitor
Enfuvirtide (T20; DP178) acetate is an anti-HIV-1 fusion inhibitor peptide. -
HIV Reverse Transcriptase Inhibitor
β-Rubromycin is a selective inhibitor of HIV-1 reverse transcriptase, exhibiting a Ki of 0.27 μM. Additionally, it demonstrates potent telomerase inhibition with an IC50 of 3 μM. β-Rubromycin effectively inhibits the proliferation of K-562 and HeLa cell lines, showing IC50 values of 19.5 µM and 22.7 µM, respectively, making it a valuable tool for research in HIV and telomerase-related studies. -
HIV Protease Inhibitor
Cytochalasin A is a cell-permeable fungal toxin that is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50=3 μM) and inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhydryl groups. Antibiotic and fungicidal activitives. -
HIV-1 protease/PTP1B inhibitor
Isosinensetin is a bioactive flavonoid compound with diverse pharmacological properties. It acts as a dual inhibitor of HIV-1 protease and protein tyrosine phosphatase 1B (PTP1B), with an IC₅₀ of 2.61 µM and a Kᵢ of 0.92 µM for PTP1B, indicating its potential in antiviral and metabolic disease research. Additionally, isosinensetin inhibits P-glycoprotein (P-gp) activity in MDR1-MDCKII cells, suggesting its utility in overcoming multidrug resistance. Isosinensetin exhibits multiple therapeutic effects, including anti-tumor, anti-viral, anti-inflammatory, and antioxidant activities. These properties support its application in the research of various conditions such as cancer, chronic inflammation, osteoporosis, diabetes, and infectious diseases. -
HIV-1 Entry Inhibitor
Trilobatin is a natural sweetener extracted from Lithocarpus polystachyus Rehd, functioning primarily as an HIV-1 entry inhibitor by targeting the HIV-1 Gp41 envelope protein. It demonstrates neuroprotective effects and acts as a selective SGLT1/2 inhibitor, promoting the proliferation of human hepatoblastoma cells. Trilobatin is valuable for research involving HIV-1 entry mechanisms and potential therapeutic applications in hepatoblastoma and neuroprotection studies. -
Antifungal Agent/HIV-1 Inhibitor
Amphotericin B methyl ester is a methyl ester derivative of the polyene antibiotic Amphotericin B, targeting cell membranes through cholesterol binding. Exhibiting potent antifungal activity, it effectively disrupts the structural integrity of fungal cells. Additionally, Amphotericin B methyl ester has demonstrated the ability to inhibit HIV-1 particle production and replication, making it valuable for research in both antifungal therapies and HIV-1 studies. -
Antifungal Agent/HIV-1 Inhibitor
Amphotericin B methyl ester hydrochloride is a derivative of the polyene antibiotic amphotericin B, functioning primarily as an antifungal agent. This compound exhibits potent antifungal activity by binding to cholesterol in fungal cell membranes, leading to cell death. Additionally, it disrupts HIV-1 particle production and significantly inhibits HIV-1 replication, making it valuable for research in antifungal therapies and HIV treatment studies. -
HIV Inhibitor
Ilimaquinone is a marine sponge-derived compound that functions as an HIV inhibitor. It exhibits anti-HIV activity along with anti-inflammatory, antimicrobial, and anticancer properties, primarily through the GADD153-mediated pathway. Additionally, Ilimaquinone has been shown to induce vesiculation of the Golgi apparatus, making it a valuable tool for research on viral infections and cellular mechanisms. -
HIV Inhibitor
ZL0580 is an HIV inhibitor that functions by selectively binding to the BD1 domain of BRD4, leading to epigenetic suppression of the virus. This compound effectively inhibits Tat transactivation and transcription elongation while promoting a repressive chromatin structure at the HIV promoter. ZL0580 is valuable for research applications focused on HIV therapies and the mechanisms of viral transcription regulation. -
HIV-1 Inhibitor
Formycin A is a purine nucleoside antibiotic that acts as a potent inhibitor of human immunodeficiency virus type 1 (HIV-1), exhibiting an EC50 of 10 μM. This compound demonstrates notable antiviral and antitumor activities, making it a valuable tool for research in virology and cancer biology. Its efficacy against HIV-1 makes it a relevant candidate for studies aimed at developing antiviral therapies. -
HIV Protease Inhibitor
Palinavir is a potent inhibitor of HIV-1 and HIV-2 proteases, exhibiting an IC50 range of 0.5-30 nM. It demonstrates significant antiviral activity, making it valuable for research focused on HIV treatment strategies and drug development. Palinavir's mechanism of action targets the viral protease enzyme, disrupting the replication cycle of the virus and providing insights into HIV pathogenesis and therapeutic interventions. -
HIV-1 Protease Inhibitor
Lasinavir (CGP 61755) is a selective inhibitor of HIV-1 protease, exhibiting an IC50 value of 1 nM. This compound demonstrates significant antiviral activity against HIV-1, making it a valuable tool for studying HIV-1 infection and pathogenesis. Lasinavir is applicable in research focused on antiretroviral therapies and the mechanism of protease inhibition in viral replication. -
HIV Protease Inhibitor
L-689502 is a potent HIV protease inhibitor with an IC50 of 1 nM. This compound effectively disrupts the proteolytic activity of HIV-1 protease, thereby inhibiting viral replication. L-689502 is valuable for research into antiretroviral therapies and mechanisms of HIV resistance. -
HIV-1 Capsid Inhibitor
Lenacapavir is an HIV-1 capsid inhibitor that targets the interface between capsid hexamers and CA monomers, disrupting capsid assembly and viral maturation. This compound inhibits the nuclear translocation of HIV-1 DNA and interferes with CA-mediated protein-protein interactions, resulting in reduced formation of 2-LTR circles and pre-integration proviruses. Additionally, Lenacapavir induces aberrant capsids and decreases the production of mature HIV-1. It demonstrates efficacy against various HIV-1 subtypes and clinical isolates, making it a valuable reagent for research on HIV-1 infection. -
HIV-1 RT Inhibitor
Tenofovir diphosphate disodium is a potent inhibitor of HIV-1 reverse transcriptase, with a Ki value of 1.55 μM for DNA and 0.022 μM for RNA. This compound exhibits key biological activity as an antiretroviral agent, making it a valuable tool for the study of HIV and AIDS. It is suitable for research applications focused on understanding viral replication and developing therapeutic strategies against HIV infection. -
HIV-1 Inhibitor
PYR01 is a non-nucleoside reverse transcriptase inhibitor that targets HIV-1 by activating the death of infected cells. It exhibits significant antiviral activity, demonstrating IC50 values of 27.5 nM and 39.7 nM for cytotoxic and antiviral effects, respectively. By promoting HIV-1 Gag-Pol dimerization and intracellular activation of HIV-1 protease, PYR01 induces selective cytotoxicity in HIV-1-infected cells. This compound is valuable for research focused on HIV biology and therapeutic strategies. -
HIV-1 Inhibitor
PF-3450074 is a specific inhibitor of the HIV-1 capsid protein (CA), exhibiting broad-spectrum antiviral activity against various HIV isolates with submicromolar potency (EC50=8-640 nM). This compound functions at an early stage of the HIV-1 life cycle, impeding viral replication by competing with the binding of nuclear host factors CPSF6 and NUP153. Additionally, PF-3450074 disrupts key processes such as uncoating, assembly, and reverse transcription, making it a valuable tool for HIV research. -
CD4-Targeted HIV Inhibitor
Cyclotriazadisulfonamide (CADA) is a selective inhibitor of HIV entry that targets CD4. It functions by inhibiting the co-translational translocation of human CD4 into the endoplasmic reticulum lumen in a signal peptide-dependent manner. In addition, CADA acts as a Sec61 translocon inhibitor, making it a valuable tool for studying HIV pathogenesis and potential therapeutic strategies against HIV infection. -
HIV-1 Inhibitor
Glycolithocholic acid 3-sulfate is a cholic acid derivative that serves as an effective HIV-1 inhibitor. It demonstrates the ability to inhibit the replication of HIV-1 in vitro, making it a valuable tool for studying HIV infection. Additionally, Glycolithocholic acid 3-sulfate may have relevance in research related to gallbladder disease. -
V-ATPase/HIV-1 Inhibitor
Diphyllin is a potent inhibitor of vacuolar H+-ATPase (V-ATPase) with an IC50 of 17 nM, and also acts as an HIV-1 inhibitor with an IC50 of 0.38 μM. This compound effectively disrupts the acidification of osteoclast lysosomes, leading to significant inhibition of osteoclast-mediated bone resorption while leaving osteoblastic bone formation unaffected. Diphyllin is valuable for investigating bone metabolism-related diseases and exploring therapeutic avenues for conditions characterized by excessive bone resorption. -
HIV Inhibitor
Censavudine is a nucleoside reverse transcriptase inhibitor that exhibits potent antiviral activity against HIV. With EC50 values ranging from 30 nM to 81 nM for HIV-2 and 450 nM to 890 nM for HIV-1, this compound is effective in disrupting viral replication. Additionally, Censavudine possesses a reactive alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a versatile tool for click chemistry applications in drug development and molecular biology research. -
HIV/NRTTI Inhibitor
MK-8527 is an orally active inhibitor of HIV that functions as a nucleoside reverse transcriptase translocation inhibitor (NRTTI). This compound exhibits antiviral activity by impeding reverse transcriptase, an essential enzyme for viral replication. MK-8527 is primarily utilized in research focused on the development of HIV therapeutic strategies and studying mechanisms of resistance in retroviral infections. -
HIV Inhibitor
2',3'-Dideoxyadenosine is an inhibitor of HIV replication that functions by incorporating into viral DNA, thereby terminating chain elongation. This compound exhibits significant antiretroviral activity and is utilized in research to understand mechanisms of HIV infection and the development of therapeutic strategies against the virus. Its efficacy makes it a valuable tool in antiviral studies and drug development pipelines focused on HIV. -
HIV Inhibitor
Zingibroside R1 is a dammarane-type triterpenoid saponin that targets HIV through its inhibitory effects. Isolated from the rhizomes, taproots, and lateral roots of Panax japonicus C. A. Meyer, it demonstrates anti-HIV-1 activity, in addition to notable anti-tumor and anti-angiogenic properties. Zingibroside R1 also inhibits 2-deoxy-D-glucose (2-DG) uptake in EAT cells with an IC50 of 91.3 μM, highlighting its potential for further research in cancer and viral therapies. -
HIV Inhibitor
(R)-Edelfosine, also known as (R)-ET-18-OCH3, is an ether lipid analog that primarily targets HIV through its antiviral properties. This compound exhibits significant anti-HIV activity and demonstrates potential antineoplastic effects. It is commonly utilized in research applications related to antiviral therapies and cancer treatment investigations. -
HIV-1 reverse transcriptase Inhibitor
Ulonivirine is an orally active non-nucleoside inhibitor of HIV-1 reverse transcriptase, targeting the hydrophobic binding pocket adjacent to the enzyme's polymerase active site. It effectively disrupts viral replication, making it a valuable tool for research focused on HIV-1 infection and the mechanisms of antiretroviral resistance. Ulonivirine is suitable for studies aimed at understanding HIV-1 pathogenesis and developing therapeutic interventions. -
HIV-1 Integrase Inhibitor
Bictegravir sodium is a highly potent inhibitor of HIV-1 integrase, demonstrating an IC50 of 7.5 nM. This compound exhibits robust and selective anti-HIV activity while maintaining low cytotoxicity. Bictegravir sodium is primarily utilized in research focused on HIV treatment strategies and the development of antiretroviral therapies. -
HIV-1 Integrase Inhibitor
1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide is a potent inhibitor of HIV-1 integrase, targeting both the 3'-processing and strand transfer stages of the integration process. This compound serves as a valuable tool in HIV-1 research, facilitating the study of viral replication and integration mechanisms. Its effectiveness in inhibiting key steps in the integration pathway makes it an important reagent for investigations related to HIV-1 therapeutic development. -
HIV-1 Inhibitor
BIT-225 is an HIV-1 inhibitor that specifically targets the Vpu protein by blocking its ion channel function. This mechanism effectively inhibits the release of HIV-1, particularly in monocyte-derived macrophages, with an EC50 of 2.25 μM. BIT-225 demonstrates a favorable safety profile, exhibiting minimal cytotoxicity (TC50 of 284 μM). This compound is valuable for research into therapeutic strategies for HIV-1. -
HIV Inhibitor
APOBEC3G-IN-1 is a potent inhibitor of the HIV virus that targets the APOBEC3G enzyme. This compound demonstrates significant activity in inhibiting viral replication, making it a valuable tool in HIV research. Its ability to modulate the immune response against HIV provides insights into viral pathogenesis and potential therapeutic strategies. -
HIV-1 Nucleocapsid Protein Inhibitor
Claficapavir is a potent inhibitor of the HIV-1 nucleocapsid protein, specifically designed to interfere with its chaperone functions. With an IC50 of approximately 1 μM and a strong binding affinity (Kd = 20 nM), Claficapavir exhibits significant antiviral activity against HIV-1. This compound serves as a valuable tool for research focused on HIV pathogenesis and therapeutic interventions targeting viral replication. -
HIV-1 inhibitor
HIV-1 inhibitor-6 is a diheteroarylamide-based compound that functions as a potent inhibitor of HIV-1 pre-mRNA alternative splicing. This compound effectively blocks HIV replication and exhibits activity against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. Additionally, HIV-1 inhibitor-6 demonstrates inhibitory effects against various HIV strains that are resistant to existing therapies targeting reverse transcriptase, protease, integrase, and CCR5, with EC50s ranging from 0.9 to 1.5 μM. This compound is a valuable tool for researching HIV-1 mechanisms and therapeutic strategies. -
HIV Inhibitor
Decanoyl-RVKR-CMK TFA is a potent inhibitor of HIV-1, specifically targeting the over-expression of the gp160 protein, thereby blocking its processing. This compound demonstrates significant antiviral activity against HIV-1 replication, making it a valuable tool in the study of HIV biology and therapeutic development. Its application includes research focused on the mechanisms of HIV infection and potential therapeutic interventions. -
HIV Inhibitor
Schisantherin D is a dibenzocyclooctadiene lignan that exhibits significant anti-HIV activity with an EC50 of 0.5 μg/mL. This compound selectively inhibits endothelin receptor B (ETBR) and demonstrates hepatoprotective properties. Schisantherin D is valuable for research applications focused on HIV replication and the exploration of liver protective mechanisms.

