resiquimod [Ligand Id: 5051] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL383322 (CD11301, CD-11301, R-848, Resiquimod, S-28463)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
7,8-dihydro-8-oxoguanine triphosphatase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3708265] [UniProtKB: P36639]
ChEMBL Inhibition of MTH1 (unknown origin) using 8-oxo-dGTP as substrate preincubated for 15 mins followed by substrate addition and measured after 20 mins by PPiLight detection reagent based luminescence assay B 5.69 pIC50 2056 nM IC50 J Med Chem (2016) 59: 2346-2361 [PMID:26878898]
TLR7/Toll-like receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5936] [GtoPdb: 1757] [UniProtKB: Q9NYK1]
ChEMBL Agonist activity at human TLR-7 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay B 5.82 pEC50 1500 nM EC50 J Med Chem (2014) 57: 339-347 [PMID:24383475]
ChEMBL Agonist activity at human TLR7 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay F 5.85 pEC50 1400 nM EC50 ACS Med Chem Lett (2012) 3: 501-504 [PMID:22837811]
GtoPdb - - 5.87 pEC50 1340 nM EC50 Nat Immunol (2002) 3: 196-200 [PMID:11812998];
Nat Immunol (2002) 3: 499 [PMID:12032557];
ACS Med Chem Lett (2017) 8: 1148-1152 [PMID:29152046]
ChEMBL Agonist activity at human TLR7 expressed in HEK cells after 8 to 12 hrs by NFkappaB/SEAP reporter gene assay B 5.87 pEC50 1340 nM EC50 ACS Med Chem Lett (2017) 8: 1148-1152 [PMID:29152046]
ChEMBL Agonist activity at TLR7 in human PBMC assessed as induction of IN-12 stimulation B 5.9 pEC50 1259 nM EC50 J Med Chem (2016) 59: 2346-2361 [PMID:26878898]
ChEMBL Reporter Assay: For TLR8 and TLR7 activity testing, HEK-Blue human TLR8 or TLR7 cells, respectively, (Invivogen, San Diego, Calif., USA) transfected with a SEAP reporter (secreted embryonic alkaline phosphatase) construct were used, in which the reporter expression is regulated by the NF-κB promoter upon stimulation for 24 hr. The reporter activity was determined using Quanti Blue kit (Invivogen, San Diego, Calif., USA) at a wavelength of 640 nm. B 6.12 pEC50 760 nM EC50 US-9334268-B2. 4-amino-imidazoquinoline compounds (2016)
ChEMBL Agonist activity at human TLR7 expressed in HEK293 cells assessed as induction of NFKappaB activity after 24 hrs by SEAP reporter gene assay B 6.12 pEC50 750 nM EC50 Bioorg Med Chem Lett (2020) 30: 126984-126984 [PMID:32001135]
ChEMBL Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay F 6.58 pEC50 260.1 nM EC50 J Med Chem (2010) 53: 2964-2972 [PMID:20232824]
ChEMBL Agonist activity at human TLR7 expressed in HEK-Blue cells assessed as induction of NFkappaB activation by measuring increase in SEAP level by SEAP reporter gene-based UV-vis absorbance method B 6.6 pEC50 250 nM EC50 Bioorg Med Chem Lett (2020) 30: 126788-126788 [PMID:31784317]
ChEMBL Agonist activity at human TLR7 expressed in HEK293 cells incubated for 6 to 16 hrs by SEAP reporter gene assay B 7.12 pEC50 75 nM EC50 J Med Chem (2021) 64: 7507-7532 [PMID:34048243]
TLR8/Toll-like receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5805] [GtoPdb: 1758] [UniProtKB: Q9NR97]
ChEMBL Reporter Assay: For TLR8 and TLR7 activity testing, HEK-Blue human TLR8 or TLR7 cells, respectively, (Invivogen, San Diego, Calif., USA) transfected with a SEAP reporter (secreted embryonic alkaline phosphatase) construct were used, in which the reporter expression is regulated by the NF-κB promoter upon stimulation for 24 hr. The reporter activity was determined using Quanti Blue kit (Invivogen, San Diego, Calif., USA) at a wavelength of 640 nm. B 5.02 pEC50 9600 nM EC50 US-9334268-B2. 4-amino-imidazoquinoline compounds (2016)
ChEMBL Agonist activity at human TLR8 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay F 5.19 pEC50 6400 nM EC50 ACS Med Chem Lett (2012) 3: 501-504 [PMID:22837811]
GtoPdb - - 5.21 pEC50 6130 nM EC50 Nat Immunol (2002) 3: 196-200 [PMID:11812998];
Nat Immunol (2002) 3: 499 [PMID:12032557];
ACS Med Chem Lett (2017) 8: 1148-1152 [PMID:29152046]
ChEMBL Agonist activity at human TLR8 expressed in HEK cells after 8 to 12 hrs by NFkappaB/SEAP reporter gene assay B 5.21 pEC50 6130 nM EC50 ACS Med Chem Lett (2017) 8: 1148-1152 [PMID:29152046]
ChEMBL Agonist activity at human TLR8 expressed in HEK293 cells assessed as induction of NFKappaB activity after 24 hrs by SEAP reporter gene assay B 5.23 pEC50 5870 nM EC50 Bioorg Med Chem Lett (2020) 30: 126984-126984 [PMID:32001135]
ChEMBL Agonist activity at human TLR-8 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay B 5.35 pEC50 4500 nM EC50 J Med Chem (2014) 57: 339-347 [PMID:24383475]
ChEMBL Agonist activity at human TLR8 expressed in HEK293 cells incubated for 6 hrs by luciferase reporter gene assay B 5.4 pEC50 4000 nM EC50 J Med Chem (2016) 59: 5868-5878 [PMID:27270029]
ChEMBL Agonist activity at human TLR8 expressed in HEK-Blue cells assessed as induction of NFkappaB activation by measuring increase in SEAP level by SEAP reporter gene-based UV-vis absorbance method B 5.52 pEC50 3000 nM EC50 Bioorg Med Chem Lett (2020) 30: 126788-126788 [PMID:31784317]
ChEMBL Agonist activity at human TLR8 expressed in HEK293 cells incubated for 6 to 16 hrs by SEAP reporter gene assay B 6.32 pEC50 480 nM EC50 J Med Chem (2021) 64: 7507-7532 [PMID:34048243]

ChEMBL data shown on this page come from version 32:

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]