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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL225157 (Cli-095, Resatorvid, Tak-242, TAK-242)
There should be some charts here, you may need to enable JavaScript!
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 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]