parthenolide [Ligand Id: 12428] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL465158
Created with Highcharts 10.3.3ValuesChart context menuToll-like receptor 4pKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuUbiquitin carboxyl-terminal hydrolase 7pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • TAS2R14 in Human [GtoPdb: 668] [UniProtKB: Q9NYV8]
Created with Highcharts 10.3.3ValuesChart context menuTAS2R14pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • thioredoxin reductase 1 in Rat [GtoPdb: 3302] [UniProtKB: O89049]
Created with Highcharts 10.3.3ValuesChart context menuthioredoxin reductase 1pKd RatpKi RatpIC50 RatpEC50 Rat0123456Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TLR4/Toll-like receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5255] [GtoPdb: 1754] [UniProtKB: O00206]
ChEMBL Modulation of TLR4 in human THP1 cells assessed as reduction in LPS-induced TLR4 expression pretreated for 2 hrs followed by LPS challenge and measured after 18 hrs by flow cytometry B 5.85 pIC50 1400 nM IC50 J Med Chem (2020) 63: 13466-13513 [PMID:32845153]
Ubiquitin carboxyl-terminal hydrolase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2157850] [UniProtKB: Q93009]
ChEMBL Inhibition of recombinant full length wild type human Flag-tagged USP7 expressed in human HEK293 cells using Ub-AMC as substrate by fluorometric assay B 5.18 pIC50 6580 nM IC50 Eur J Med Chem (2021) 212: 113149-113149 [PMID:33445154]
TAS2R14 in Human [GtoPdb: 668] [UniProtKB: Q9NYV8]
GtoPdb - - 4.99 pEC50 10270 nM EC50 Biochim Biophys Acta Gen Subj (2018) 1862: 2162-2173 [PMID:30009876]
thioredoxin reductase 1 in Rat [GtoPdb: 3302] [UniProtKB: O89049]
GtoPdb - - 5.52 pIC50 ~3000 nM IC50 J Biol Chem (2016) 291: 10021-31 [PMID:27002142]

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]