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ChEMBL ligand: CHEMBL1282 (Aldara, Imiquimod, NSC-369100, NSC-759651, R-837, S-26308, S26308, Tmx-101, Zyclara) |
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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 | 6.19 | pIC50 | 646 | nM | IC50 | J Med Chem (2016) 59: 2346-2361 [PMID:26878898] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) | B | 5.52 | pKi | 2987 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) | B | 5.27 | pIC50 | 5320 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.89 | pKi | 1288 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.58 | pIC50 | 2621 | nM | IC50 | DrugMatrix in vitro pharmacology data |
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
ChEMBL | DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) | B | 5.83 | pKi | 1481 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) | B | 5.82 | pIC50 | 1506 | nM | IC50 | DrugMatrix in vitro pharmacology data |
TLR7/Toll-like receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5936] [GtoPdb: 1757] [UniProtKB: Q9NYK1] | ||||||||
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 | 4.92 | pEC50 | 12100 | nM | EC50 | ACS Med Chem Lett (2012) 3: 501-504 [PMID:22837811] |
GtoPdb | - | - | 4.94 | pEC50 | 11400 | nM | EC50 | 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 | 4.94 | pEC50 | 11400 | nM | EC50 | ACS Med Chem Lett (2017) 8: 1148-1152 [PMID:29152046] |
ChEMBL | Agonist activity at human TLR-7 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay | B | 4.97 | pEC50 | 10700 | nM | EC50 | J Med Chem (2014) 57: 339-347 [PMID:24383475] |
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 | 5.17 | pEC50 | 6800 | nM | EC50 | Bioorg Med Chem Lett (2020) 30: 126788-126788 [PMID:31784317] |
ChEMBL | Agonist activity at human TLR7 in HEK293 cells cotransfected with SEAP reporter gene assessed as activity of SEAP incubated for 24 hrs by quanti-blue staining based SEAP reporter gene assay | B | 5.21 | pEC50 | 6200 | nM | EC50 | Eur J Med Chem (2019) 179: 109-122 [PMID:31247373] |
ChEMBL | Agonist activity at human TLR7 | B | 5.66 | pEC50 | 2210 | nM | EC50 | J Med Chem (2021) 64: 8010-8041 [PMID:34107682] |
ChEMBL | Agonist activity at TLR7 (unknown origin) | B | 5.67 | pEC50 | 2120 | nM | EC50 | J Med Chem (2023) 66: 6437-6462 [PMID:37163340] |
ChEMBL | Agonist activity at human TLR7 expressed in NF-kappaB-stimulated HEK293 cells assessed as induction of secreted alkaline phosphatase expression by reporter gene assay | F | 5.67 | pEC50 | 2120 | nM | EC50 | J Med Chem (2010) 53: 4450-4465 [PMID:20481492] |
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]