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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]