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]
ChEMBL Agonist activity at human TLR7 in HEK-Blue hTLR7 cells assessed as activation of NFkappaB by SEAP reporter gene based spectrophotometry assay B 5.26 pEC50 5480 nM EC50 RSC Med Chem (2021) 12: 1065-1120 [PMID:34355178]
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]
ChEMBL Agonist activity at human TLR8 in HEK-Blue hTLR8 cells assessed as activation of NFkappaB by SEAP reporter gene based spectrophotometry assay B 5.88 pEC50 1320 nM EC50 RSC Med Chem (2021) 12: 1065-1120 [PMID:34355178]
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 Agonist activity in TLR8 (unknown origin) expressed in HEK293 cells assessed as induction of NF-kappa activation B 6.1 pEC50 800 nM EC50 Eur J Med Chem (2020) 193: 112238-112238 [PMID:32203790]

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]