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