imiquimod [Ligand Id: 5003] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1282 (Aldara, Imiquimod, NSC-369100, NSC-759651, R-837, S26308, S-26308, Zyclara)
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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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 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 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]