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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 |
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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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]