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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 |
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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 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]