lasofoxifene [Ligand Id: 7542] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL328190 (Lasofoxifene) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
| ChEMBL | Inhibition of [3H]estradiol binding to human estrogen receptor alpha expressed in HeLa cells | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2005) 48: 364-379 [PMID:15658851] |
| ChEMBL | Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor alpha; ERE assay | B | 8.51 | pIC50 | 3.1 | nM | IC50 | J Med Chem (2005) 48: 364-379 [PMID:15658851] |
| GtoPdb | - | - | 8.51 | pIC50 | 3.1 | nM | IC50 | J Med Chem (2005) 48: 364-79 [PMID:15658851] |
| ChEMBL | Inhibition of binding to recombinant human ERalpha by scintillation proximity assay | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 5124-5128 [PMID:16203138] |
| ChEMBL | Binding affinity for human estrogen receptor alpha | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 715-718 [PMID:15664843] |
| Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] | ||||||||
| ChEMBL | Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor beta; ERE assay | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2005) 48: 364-379 [PMID:15658851] |
| ChEMBL | Inhibition of [3H]estradiol binding to human estrogen receptor beta expressed in HeLa cells | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2005) 48: 364-379 [PMID:15658851] |
| GtoPdb | - | - | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2005) 48: 364-79 [PMID:15658851] |
| ChEMBL | Binding affinity for human estrogen receptor beta | B | 8.74 | pIC50 | 1.8 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 715-718 [PMID:15664843] |
| ChEMBL | Inhibition of binding to recombinant human ERbeta by scintillation proximity assay | B | 8.74 | pIC50 | 1.8 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 5124-5128 [PMID:16203138] |
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]
