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

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ChEMBL ligand: CHEMBL465158
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  • TAS2R14 in Human [GtoPdb: 668] [UniProtKB: Q9NYV8]
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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]
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]

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]