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ChEMBL ligand: CHEMBL666 (Dihydroxyphosphinecarboxylic Acid Oxide, Foscarnet, J05AD01) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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DNA polymerase in Varicella-zoster virus (strain Dumas) (HHV-3) (Human herpesvirus 3) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4859] [UniProtKB: P09252] | ||||||||
ChEMBL | Inhibition of Varicella-Zoster virus DNA polymerase (95 uL) activity in a solution containing 6.4 mM HEPES (pH 7.5), incubation for 12 minutes at 26 degrees C; [nd = not determined] | B | 6.55 | pIC50 | <280 | nM | IC50 | J Med Chem (2005) 48: 5794-5804 [PMID:16134946] |
DNA polymerase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1828] [UniProtKB: P09884] | ||||||||
ChEMBL | Inhibition of human alpha DNA polymerase (95 uL) activity in a solution containg 6.4 mM HEPES (pH 7.5) upon incubation for 12 minutes at 26 degrees C with the compound dissolved in DMSO | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2005) 48: 5794-5804 [PMID:16134946] |
DNA polymerase delta subunit 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2735] [UniProtKB: P28340] | ||||||||
ChEMBL | Inhibition of human delta DNA polymerase (95 uL) activity in a solution containg 6.4 mM HEPES (pH 7.5) upon incubation for 12 minutes at 26 degrees C with the compound dissolved in DMSO | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2005) 48: 5794-5804 [PMID:16134946] |
Human herpesvirus 5 DNA polymerase in Human cytomegalovirus (strain AD169) (HHV-5) (Human herpesvirus 5) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3414] [UniProtKB: P08546] | ||||||||
ChEMBL | Inhibition of human cytomegalovirus DNA polymerase (95 uL) activity in a solution containing 6.4 mM HEPES (pH 7.5), incubation for 12 minutes at 26 degrees C | B | 5.6 | pIC50 | 2500 | nM | IC50 | J Med Chem (2005) 48: 5794-5804 [PMID:16134946] |
ChEMBL | Inhibition of HCMV DNA polymerase by scintillation proximity assay | B | 5.6 | pIC50 | 2500 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3349-3353 [PMID:17434304] |
Human immunodeficiency virus type 1 reverse transcriptase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL247] [UniProtKB: Q72547] | ||||||||
ChEMBL | Binding affinity to HIV1 reverse transcriptase p66/p51-polypurine tract primer complex in absence of Mg2+ ions by band shift assay | B | 4.86 | pKd | 13900 | nM | Kd | J Biol Chem (2007) 282: 3337-3346 [PMID:17145704] |
ChEMBL | Binding affinity to HIV1 reverse transcriptase p66/p51-polypurine tract primer complex in presence of Mg2+ ions by band shift assay | B | 6.4 | pKd | 400 | nM | Kd | J Biol Chem (2007) 282: 3337-3346 [PMID:17145704] |
ChEMBL | Inhibitory concentration against wild type HIV-1/138Lys reverse transcriptase (RT) using [3H]dGTP as a radioligand | B | 4.25 | pIC50 | 56000 | nM | IC50 | J Med Chem (2004) 47: 3418-3426 [PMID:15189038] |
ChEMBL | Inhibitory concentration against wild type HIV-1 reverse transcriptase (RT) using poly rC.dG as the template or primer | B | 4.62 | pIC50 | 24000 | nM | IC50 | J Med Chem (2004) 47: 3418-3426 [PMID:15189038] |
ChEMBL | Inhibition of wild type HIV1 reverse transcriptase E89T mutant assessed as inhibition of DNA primer extension using [8-3H(N)]-dATP by scintillation proximity assay | B | 5.28 | pIC50 | 5200 | nM | IC50 | J Med Chem (2014) 57: 7435-7449 [PMID:25144111] |
ChEMBL | Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA/DNAM duplex primed substrate by scintillation proximity assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Biol Chem (2007) 282: 8005-8010 [PMID:17172472] |
ChEMBL | Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA PPT primed substrate by scintillation proximity assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Biol Chem (2007) 282: 8005-8010 [PMID:17172472] |
ChEMBL | Inhibition of wild type HIV1 reverse transcriptase K65R mutant assessed as inhibition of DNA primer extension using [8-3H(N)]-dATP by scintillation proximity assay | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2014) 57: 7435-7449 [PMID:25144111] |
ChEMBL | Inhibition of wild type HIV1 reverse transcriptase assessed as inhibition of DNA primer extension using [8-3H(N)]-dATP by scintillation proximity assay | B | 5.6 | pIC50 | 2500 | nM | IC50 | J Med Chem (2014) 57: 7435-7449 [PMID:25144111] |
ChEMBL | Inhibition of wild type HIV1 reverse transcriptase M184V mutant assessed as inhibition of DNA primer extension using [8-3H(N)]-dATP by scintillation proximity assay | B | 6.1 | pIC50 | 800 | nM | IC50 | J Med Chem (2014) 57: 7435-7449 [PMID:25144111] |
ChEMBL | Inhibition of HIV1 reverse transcriptase p66/p51 polymerase using PPT57 DNA/Cy5-labeled PPT24 as template/primer preincubated for 10 mins followed by dNTP addition measured after 5 mins by bromophenol blue staining based phosphor imaging analysis | B | 6.1 | pIC50 | 800 | nM | IC50 | Bioorg Med Chem (2018) 26: 1713-1726 [PMID:29478802] |
ChEMBL data shown on this page come from version 32:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]