piperlongumine [Ligand Id: 13376] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL465843 (Piplartine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| proteasome 20S subunit beta 1/proteasome 20S subunit beta 8/proteasome 20S subunit beta 9/proteasome 20S subunit beta 6/proteasome 20S subunit beta 5/proteasome 20S subunit beta 2/20S proteasome in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL3831201] [GtoPdb: 2404, 2408, 2409, 2407, 2406, 2405] [UniProtKB: A5LHX3, O14818, P20618, P25786, P25787, P25788, P25789, P28062, P28065, P28066, P28070, P28072, P28074, P40306, P49720, P49721, P60900, Q8TAA3, Q99436] | ||||||||
| ChEMBL | Inhibition of human 20S proteasome | B | 4.82 | pIC50 | 15000 | nM | IC50 | Eur J Med Chem (2021) 220: 113471-113471 [PMID:33930801] |
| ChEMBL | Inhibition of recombinant human 20S constitutive proteasome | B | 4.82 | pIC50 | 15000 | nM | IC50 | J Nat Prod (2024) 87: 617-628 [PMID:38436272] |
| Forkhead box protein O3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5778] [UniProtKB: O43524] | ||||||||
| ChEMBL | Induction of nuclear translocation of FOXO3 in human U2OS cells by inverted microscopic analysis | B | 4.42 | pEC50 | 37700 | nM | EC50 | J Nat Prod (2024) 87: 617-628 [PMID:38436272] |
| signal transducer and activator of transcription 3/Signal transducer and activator of transcription 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4026] [GtoPdb: 2994] [UniProtKB: P40763] | ||||||||
| ChEMBL | Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells after 24 hrs by Western blot analysis | B | 5.15 | pIC50 | 7000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2566-2572 [PMID:29807795] |
| thioredoxin reductase 1/Thioredoxin reductase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1927] [GtoPdb: 3302] [UniProtKB: Q16881] | ||||||||
| ChEMBL | Inhibition of TrxR in human SH-SY5Y cells using DTNB as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by Ellman's method | B | 4.34 | pIC50 | 45880 | nM | IC50 | Eur J Med Chem (2019) 181: 111580-111580 [PMID:31400708] |
| ChEMBL | Inhibition of TrxR in human BEL-7402/5-FU cells by colorimetric assay | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Nat Prod (2020) 83: 3041-3049 [PMID:33026807] |
ChEMBL data shown on this page come from version 35:
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]
