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ChEMBL ligand: CHEMBL383322 (CD-11301, CD11301, 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 |
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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 | Activation of TLR7 (unknown origin) | B | 5.82 | pEC50 | 1500 | nM | EC50 | Eur J Med Chem (2020) 193: 112238-112238 [PMID:32203790] |
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 receptor | B | 5.82 | pEC50 | 1500 | nM | EC50 | Eur J Med Chem (2021) 218: 113356-113356 [PMID:33773287] |
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-ÎşB 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-ÎşB 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 TLR8 receptor | B | 5.35 | pEC50 | 4500 | nM | EC50 | Eur J Med Chem (2021) 218: 113356-113356 [PMID:33773287] |
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 | Activation of TLR8 (unknown origin) | B | 5.35 | pEC50 | 4500 | nM | EC50 | Eur J Med Chem (2020) 193: 112238-112238 [PMID:32203790] |
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 in TLR8 (unknown origin) expressed in HEK293 cells assessed as induction of NF-kappa activation | B | 5.82 | pEC50 | 1500 | nM | EC50 | Eur J Med Chem (2020) 193: 112238-112238 [PMID:32203790] |
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 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]