3M-002 [Ligand Id: 9270] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL512901 (CL-075)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TLR7/Toll-like receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5936] [GtoPdb: 1757] [UniProtKB: Q9NYK1]
ChEMBL Agonist activity at TLR7 in human cryopreserved PBMC assessed as induction of IFNalpha production measured after 24 hrs B 4.74 pEC50 18000 nM EC50 J Med Chem (2020) 63: 10188-10203 [PMID:32407112]
TLR8/Toll-like receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5805] [GtoPdb: 1758] [UniProtKB: Q9NR97]
ChEMBL Agonist activity at TLR8 in human cryopreserved PBMC assessed as inhibition of IL-12p40 production measured after 24 hrs B 5.31 pEC50 4900 nM EC50 J Med Chem (2020) 63: 10188-10203 [PMID:32407112]
ChEMBL Agonist activity at human TLR8 expressed in HEK293 cells assessed as induction of NF-kappaB activity by measuring extracellular secreted alkaline phosphatase by HEK-blue reporter gene assay F 5.88 pEC50 1320 nM EC50 J Med Chem (2012) 55: 8137-8151 [PMID:22924757]
GtoPdb Assessed as ability to activate NF-κB in HEK293 cells expressing human TLR8. - 5.88 pEC50 1320 nM EC50 J Med Chem (2012) 55: 8137-51 [PMID:22924757]

ChEMBL data shown on this page come from version 33:

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]