resatorvid [Ligand Id: 9036] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL225157 (Cli-095, Resatorvid, Tak-242, TAK-242)
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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 Inhibition of human TLR4 signaling expressed in HEK-Blue cells co-expressing MD2/CD14 assessed as reduction in LPS-induced NF-kappaB activation-mediated SEAP production preincubated for 2 hrs followed by LPS stimulation for 20 hrs by colorimetric assay B 6.17 pIC50 680 nM IC50 Bioorg Med Chem (2018) 26: 1653-1664 [PMID:29472126]
TLR4/Toll-like receptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795167] [GtoPdb: 1754] [UniProtKB: Q9QUK6]
ChEMBL Inhibition of TLR4 in LPS/INFgamma stimulated mouse peritoneal macrophages assessed as inhibition of IL1-beta after 20 hrs by ELISA analysis B 8.24 pIC50 5.7 nM IC50 J Med Chem (2016) 59: 1691-1710 [PMID:26422006]

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]