GSK1795091 [Ligand Id: 11150] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL507938
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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 Agonist activity at human TLR4 in human HEK-Blue hTLR4 cells assessed as NF-kappaB activation incubated for 48 hrs by SEAP reporter gene based Quanti-blue assay B 9.03 pEC50 0.93 nM EC50 J Med Chem (2023) 66: 13900-13917 [PMID:37847244]
ChEMBL Agonist activity at TLR4 in human PBMC cells assessed as induction of TNFalpha release incubated for 20 hrs by ELISA B 9.59 pEC50 0.26 nM EC50 J Med Chem (2023) 66: 13900-13917 [PMID:37847244]
GtoPdb Determined by measuring induction of TNFα production in primary human monocytes. - 9.77 pEC50 0.17 nM EC50 Bioorg Med Chem Lett (2008) 18: 5350-4 [PMID:18835160]
ChEMBL Agonist activity at TLR4 in human MONO-MAC-6 cells assessed as induction of MIP-1beta release incubated for 24 hrs by ELISA B 10.22 pEC50 0.06 nM EC50 J Med Chem (2023) 66: 13900-13917 [PMID:37847244]
ChEMBL Agonist activity at TLR4 in human PBMC cells assessed as induction of IL-1beta release incubated for 20 hrs by ELISA B 10.55 pEC50 0.03 nM EC50 J Med Chem (2023) 66: 13900-13917 [PMID:37847244]
ChEMBL Agonist activity at TLR4 in human PBMC cells assessed as induction of RANTES release incubated for 20 hrs by ELISA B 10.85 pEC50 0.01 nM EC50 J Med Chem (2023) 66: 13900-13917 [PMID:37847244]
ChEMBL Agonist activity at TLR4 in human PBMC cells assessed as induction of MIP-1beta release incubated for 20 hrs by ELISA B 11 pEC50 0.01 nM EC50 J Med Chem (2023) 66: 13900-13917 [PMID:37847244]
TLR4/Toll-like receptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795167] [GtoPdb: 1754] [UniProtKB: Q9QUK6]
ChEMBL Agonist activity at TLR4 in mouse RAW264.7 cells assessed as induction of MIP-1beta release incubated for 24 hrs by ELISA B 10.82 pEC50 0.01 nM EC50 J Med Chem (2023) 66: 13900-13917 [PMID:37847244]

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]