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, 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 |
|---|---|---|---|---|---|---|---|---|
| 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 33:
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]
