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ChEMBL ligand: CHEMBL3989866 (Bictegravir, GS-9883, GS-9883-01) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Human immunodeficiency virus type 1 integrase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3471] [UniProtKB: Q7ZJM1] | ||||||||
ChEMBL | Inhibition of HIV integrase strand transfer activity | B | 8.12 | pIC50 | 7.5 | nM | IC50 | Bioorg Med Chem (2019) 27: 3836-3845 [PMID:31324562] |
ChEMBL | Inhibition of HIV-1 integrase DTG-resistant G118R mutant | B | 8.3 | pEC50 | <=5 | nM | EC50 | Eur J Med Chem (2021) 225: 113787-113787 [PMID:34425310] |
ChEMBL | Inhibition of HIV-1 integrase DTG-resistant R263K mutant | B | 8.3 | pEC50 | <=5 | nM | EC50 | Eur J Med Chem (2021) 225: 113787-113787 [PMID:34425310] |
ChEMBL | Inhibition of HIV-1 integrase DTG-resistant H51Y/R263K double mutant | B | 8.3 | pEC50 | <=5 | nM | EC50 | Eur J Med Chem (2021) 225: 113787-113787 [PMID:34425310] |
Integrase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296304] [UniProtKB: T1QYY3] | ||||||||
ChEMBL | Inhibition of HIV-1 integrase RAL-resistant G140S/Q148H double mutant | B | 8.3 | pEC50 | <=5 | nM | EC50 | Eur J Med Chem (2021) 225: 113787-113787 [PMID:34425310] |
ChEMBL | Inhibition of HIV-1 integrase G140S/Q148K double mutant | B | 8.51 | pEC50 | 3.1 | nM | EC50 | Eur J Med Chem (2021) 225: 113787-113787 [PMID:34425310] |
ChEMBL data shown on this page come from version 34:
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]