foscarnet [Ligand Id: 5497] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL666 (Dihydroxyphosphinecarboxylic Acid Oxide, Foscarnet, J05AD01)
  • DNA polymerase in Varicella-zoster virus (strain Dumas) (HHV-3) (Human herpesvirus 3) [ChEMBL: CHEMBL4859] [UniProtKB: P09252]
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  • DNA polymerase alpha subunit in Human [ChEMBL: CHEMBL1828] [UniProtKB: P09884]
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  • DNA polymerase delta subunit 1 in Human [ChEMBL: CHEMBL2735] [UniProtKB: P28340]
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  • Human herpesvirus 5 DNA polymerase in Human cytomegalovirus (strain AD169) (HHV-5) (Human herpesvirus 5) [ChEMBL: CHEMBL3414] [UniProtKB: P08546]
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  • Human immunodeficiency virus type 1 reverse transcriptase in Human immunodeficiency virus 1 [ChEMBL: CHEMBL247] [UniProtKB: Q72547]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 33:

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]