| S2005 |
Raltegravir
|
Raltegravir is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM in cell-free assays, respectively. It shows greater than 1000-fold selectivity for HIV-1 IN over several related Mg2+-dependent enzyme such as HCV polymerase, HIV reverse transcriptase, HIV RNaseH and human α-, β-, γ-polymerases.
|
-
J Clin Invest, 2025, 135(16)e187663
-
EBioMedicine, 2025, 122:106004
-
EMBO Mol Med, 2025, 10.1038/s44321-025-00255-x
|
|
| S2001 |
Elvitegravir
|
Elvitegravir is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.
|
-
Lung Cancer, 2024, 15:55-67
-
Antimicrob Agents Chemother, 2023, 67(7):e0046223
-
Sci Rep, 2023, 13(1):4594
|
|
| S2667 |
Dolutegravir (GSK1349572)
|
Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, and it shows modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.
|
-
Nucleic Acids Res, 2025, 53(10)gkaf449
-
Immunity, 2024, 57(12):2928-2944.e6
-
Lung Cancer, 2024, 15:55-67
|
|
| S7766 |
Cabotegravir (GSK1265744)
|
Cabotegravir (GSK744, GSK1265744, S/GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes. It inhibits the HIV-1 integrase catalyzed strand transfer reaction with an IC50 of 3.0 nM and is in Phase 2.
|
-
Biomed Pharmacother, 2025, 184:117925
-
Cancer Lett, 2024, 588:216813
-
Nat Commun, 2023, 14(1):708
|
|
| S5245 |
Raltegravir potassium
|
Raltegravir Potassium(MK-0518 potassium) is the orally bioavailable potassium salt of raltegravir, the first approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor.
|
-
PLoS Pathog, 2024, 20(3):e1011716
-
Cells, 2022, 11(11)1841
-
J Virol, 2022, JVI0173021
|
|
| S4642 |
Dolutegravir Sodium
|
Dolutegravir Sodium (GSK-1349572A) is a HIV integrase inhibitor with IC50 of 2.7 nM.
|
-
J Infect Dis, 2022, jiac037
-
Cells, 2022, 11(11)1841
-
J Virol, 2022, JVI0173021
|
|
| S2765 |
MK-2048
|
MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively.
|
-
Molecules, 2021, 26(17)5423
-
Mol Cell, 2020, S1097-2765(20)30723-1
-
Blood Adv, 2020, 12;4(9):1845-1858
|
|
| S5911 |
Bictegravir
|
Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.
|
-
PNAS Nexus, 2024, 3(1):pgad446
-
Cells, 2022, 11(11)1841
-
Int J Mol Sci, 2022, 23(23)15380
|
|
| S1366 |
BMS-707035
|
BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.
|
-
Blood Adv, 2020, 12;4(9):1845-1858
|
|
| E0161 |
Bictegravir Sodium
|
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.
|
-
Cells, 2022, 11(11)1841
|
|
| E0459 |
Robinetin
|
Robinetin inhibits HIV integrase cleavage and integration in a dose-dependent manne, inhibits the DNA synthesis in Proteus vulgaris, and the RNA synthesis in S. aureus, also inhibits egg yolk phosphatidylcholine (EYPC) membrane lipid peroxidation and hemoglobin A (HbA) glycosylation with high efficiency.
|
|
|
| E4468 |
Cabotegravir Sodium
|
Cabotegravir (GSK-1265744) sodium is a orally active and long-acting HIV integrase strand transfer inhibitor. It also inhibits organic anion transporter 1/3 (OAT1/OAT3) with IC50 of 0.41 μM and 0.81 μM for OAT3 and OAT1, respectively.
|
|
|
| S0235 |
Lavendustin B
|
Lavendustin B inhibits HIV-1 integrase (IN) interaction with its cognate cellular cofactor lens epithelium-derived growth factor (LEDGF/p75). This compound is an inhibitor of Tyrosine Kinase and also a competitive inhibitor of glucose transporter 1 (Glut1).
|
|
|
| S4187 |
Salicylanilide
|
Salicylanilides (WR10019,2-Hydroxybenzanilide) are a group of compounds with a wide range of biological activities including antiviral potency, antibacterial (including antimycobacterial) and antifungal activities.
|
-
Hum Mol Genet, 2020, ddaa244
|
|
| S2005 |
Raltegravir
|
Raltegravir is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM in cell-free assays, respectively. It shows greater than 1000-fold selectivity for HIV-1 IN over several related Mg2+-dependent enzyme such as HCV polymerase, HIV reverse transcriptase, HIV RNaseH and human α-, β-, γ-polymerases. |
- J Clin Invest, 2025, 135(16)e187663
- EBioMedicine, 2025, 122:106004
- EMBO Mol Med, 2025, 10.1038/s44321-025-00255-x
|
|
| S2001 |
Elvitegravir
|
Elvitegravir is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively. |
- Lung Cancer, 2024, 15:55-67
- Antimicrob Agents Chemother, 2023, 67(7):e0046223
- Sci Rep, 2023, 13(1):4594
|
|
| S2667 |
Dolutegravir (GSK1349572)
|
Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, and it shows modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. |
- Nucleic Acids Res, 2025, 53(10)gkaf449
- Immunity, 2024, 57(12):2928-2944.e6
- Lung Cancer, 2024, 15:55-67
|
|
| S7766 |
Cabotegravir (GSK1265744)
|
Cabotegravir (GSK744, GSK1265744, S/GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes. It inhibits the HIV-1 integrase catalyzed strand transfer reaction with an IC50 of 3.0 nM and is in Phase 2. |
- Biomed Pharmacother, 2025, 184:117925
- Cancer Lett, 2024, 588:216813
- Nat Commun, 2023, 14(1):708
|
|
| S5245 |
Raltegravir potassium
|
Raltegravir Potassium(MK-0518 potassium) is the orally bioavailable potassium salt of raltegravir, the first approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor. |
- PLoS Pathog, 2024, 20(3):e1011716
- Cells, 2022, 11(11)1841
- J Virol, 2022, JVI0173021
|
|
| S4642 |
Dolutegravir Sodium
|
Dolutegravir Sodium (GSK-1349572A) is a HIV integrase inhibitor with IC50 of 2.7 nM. |
- J Infect Dis, 2022, jiac037
- Cells, 2022, 11(11)1841
- J Virol, 2022, JVI0173021
|
|
| S2765 |
MK-2048
|
MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively. |
- Molecules, 2021, 26(17)5423
- Mol Cell, 2020, S1097-2765(20)30723-1
- Blood Adv, 2020, 12;4(9):1845-1858
|
|
| S5911 |
Bictegravir
|
Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase. |
- PNAS Nexus, 2024, 3(1):pgad446
- Cells, 2022, 11(11)1841
- Int J Mol Sci, 2022, 23(23)15380
|
|
| S1366 |
BMS-707035
|
BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2. |
- Blood Adv, 2020, 12;4(9):1845-1858
|
|
| E0161 |
Bictegravir Sodium
|
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.
|
- Cells, 2022, 11(11)1841
|
|
| E0459 |
Robinetin
|
Robinetin inhibits HIV integrase cleavage and integration in a dose-dependent manne, inhibits the DNA synthesis in Proteus vulgaris, and the RNA synthesis in S. aureus, also inhibits egg yolk phosphatidylcholine (EYPC) membrane lipid peroxidation and hemoglobin A (HbA) glycosylation with high efficiency. |
|
|
| E4468 |
Cabotegravir Sodium
|
Cabotegravir (GSK-1265744) sodium is a orally active and long-acting HIV integrase strand transfer inhibitor. It also inhibits organic anion transporter 1/3 (OAT1/OAT3) with IC50 of 0.41 μM and 0.81 μM for OAT3 and OAT1, respectively. |
|
|
| S0235 |
Lavendustin B
|
Lavendustin B inhibits HIV-1 integrase (IN) interaction with its cognate cellular cofactor lens epithelium-derived growth factor (LEDGF/p75). This compound is an inhibitor of Tyrosine Kinase and also a competitive inhibitor of glucose transporter 1 (Glut1). |
|
|
| S4187 |
Salicylanilide
|
Salicylanilides (WR10019,2-Hydroxybenzanilide) are a group of compounds with a wide range of biological activities including antiviral potency, antibacterial (including antimycobacterial) and antifungal activities. |
- Hum Mol Genet, 2020, ddaa244
|
|
