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ChEMBL ligand: CHEMBL2386284 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511] | ||||||||
GtoPdb | - | - | 6.35 | pKi | 442 | nM | Ki | J Med Chem (2013) 56: 4611-8 [PMID:23731360] |
ChEMBL | Inhibition of human recombinant microsomal aromatase using 7-methoxy-4-trifluoromethylcoumarin as substrate by Lineweaver-Burk plot analysis | B | 6.35 | pKi | 442 | nM | Ki | J Med Chem (2013) 56: 4611-4618 [PMID:23731360] |
ChEMBL | Inhibition of human recombinant microsomal aromatase-mediated 7-methoxy-4-trifluoromethylcoumarin conversion to 7-hydroxytrifluoromethylcoumarin preincubated for 10 mins measured after 30 mins by fluorescence assay | B | 5.99 | pIC50 | 1029 | nM | IC50 | J Med Chem (2013) 56: 4611-4618 [PMID:23731360] |
ChEMBL | Inhibition of recombinant human microsomal CYP19 using MFC as substrate measured after 30 mins by fluorometric analysis | B | 5.99 | pIC50 | 1029 | nM | IC50 | Bioorg Med Chem (2016) 24: 5400-5409 [PMID:27647367] |
ChEMBL | Inhibition of human placental microsomal aromatase using testosterone as substrate assessed as formation of estradiol after 10 mins | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2016) 59: 5131-5148 [PMID:26689671] |
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
ChEMBL | Displacement of fluorescent ES2 from human recombinant ERalpha after 2 hrs by fluorimetric analysis | B | 7.77 | pEC50 | 17 | nM | EC50 | J Med Chem (2013) 56: 4611-4618 [PMID:23731360] |
ChEMBL | Displacement of fluorescent ES2 from recombinant human ERalpha after 2 hrs in absence of light by fluorometric analysis | B | 7.77 | pEC50 | 17 | nM | EC50 | Bioorg Med Chem (2016) 24: 5400-5409 [PMID:27647367] |
GtoPdb | - | - | 7.77 | pEC50 | 17 | nM | EC50 | J Med Chem (2013) 56: 4611-8 [PMID:23731360] |
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] | ||||||||
GtoPdb | - | - | 7.56 | pEC50 | 27.5 | nM | EC50 | J Med Chem (2013) 56: 4611-8 [PMID:23731360] |
ChEMBL | Displacement of fluorescent ES2 from human recombinant ERbeta after 2 hrs by fluorimetric analysis | B | 7.56 | pEC50 | 27.5 | nM | EC50 | J Med Chem (2013) 56: 4611-4618 [PMID:23731360] |
ChEMBL | Displacement of fluorescent ES2 from recombinant human ERbeta after 2 hrs in absence of light by fluorometric analysis | B | 7.56 | pEC50 | 27.5 | nM | EC50 | Bioorg Med Chem (2016) 24: 5400-5409 [PMID:27647367] |
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]