cabotegravir [Ligand Id: 11386] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL2403238 (S-265744, GSK1265744A, Gsk744, Apretude, GSK1265744, GSK-1265744A, Gsk-1265744, Cabotegravir, Cabotegravir component of cabenuva, GSK744)
  • Human immunodeficiency virus type 1 integrase in Human immunodeficiency virus 1 [ChEMBL: CHEMBL3471] [UniProtKB: Q7ZJM1]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Human immunodeficiency virus type 1 integrase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3471] [UniProtKB: Q7ZJM1]
ChEMBL Inhibition of HIV-1 integrase strand transfer activity B 5.74 pIC50 1800 nM IC50 Eur J Med Chem (2024) 279: 116900-116900 [PMID:39332384]
ChEMBL Inhibition of HIV-1 integrase strand transfer activity using [3H]-DNA as substrate preincubated for 60 mins prior to substrate addition measured after 25 to 45 mins B 8.52 pIC50 3 nM IC50 J Med Chem (2013) 56: 5901-5916 [PMID:23845180]
ChEMBL Inhibition of HIV-1 NL4-3 integrase B 9.47 pIC50 0.34 nM IC50 Bioorg Med Chem (2024) 111: 117860-117860 [PMID:39094527]
ChEMBL Inhibition of HIV-1 BAL integrase strand transfer activity B 9.66 pIC50 0.22 nM IC50 Bioorg Med Chem (2024) 111: 117860-117860 [PMID:39094527]

ChEMBL data shown on this page come from version 37:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]