motolimod [Ligand Id: 9026] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3301618 (Motolimod, VTX-2337, VTX-378)
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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 4.52 pEC50 >30000 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 5.89 pEC50 1300 nM EC50 J Med Chem (2020) 63: 10188-10203 [PMID:32407112]
GtoPdb - - 7 pEC50 ~100 nM EC50 Clin Cancer Res (2012) 18: 499-509 [PMID:22128302]
ChEMBL Agonist activity at TLR8 (unknown origin) B 7 pEC50 100 nM EC50 Eur J Med Chem (2020) 193: 112238-112238 [PMID:32203790]
ChEMBL Agonist activity at TLR8 (unknown origin) B 7 pEC50 100 nM EC50 RSC Med Chem (2021) 12: 1065-1120 [PMID:34355178]
ChEMBL Agonist activity at human TLR8 expressed in HEK293 cells by reporter gene assay B 7 pEC50 100 nM EC50 Eur J Med Chem (2018) 157: 582-598 [PMID:30125720]

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]