ChEMBL ligand: CHEMBL46740 (Bazedoxifene)
Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] There should be some charts here, you may need to enable JavaScript!
Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] There should be some charts here, you may need to enable JavaScript!

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	Displacement of Fluormone-tagged ES2 from human recombinant ERalpha after 2 hrs by fluorescence polarization assay	B	4.5	pIC50	31710	nM	IC50	Bioorg Med Chem (2018) 26: 266-277 [PMID:29198894]
ChEMBL	Binding Assay: The competition assay was performed in a 96-well plate (polystyrene*) which binds <2.0% of the total input [3H]-17beta-estradiol and each data point was gathered in triplicate. 100 uG/100 uL of the receptor preparation was aliquoted per well. A saturating dose of 2.5 nM [3H]17beta-estradiol+competitor (or buffer) in a 50 uL volume was added in the preliminary competition when 100x and 500x competitor were evaluated, only 0.8 nM [3H]17beta-estradiol was used. The plate was incubated at room temperature for 2.5 h. At the end of this incubation period 150 uL of ice-cold dextran coated charcoal (5% activated charcoal coated with 0.05% 69K dextran) was added to each well and the plate was immediately centrifuged at 99 g for 5 minutes at 4 C. 200 uL of the supernatant solution was then removed for scintillation counting. Samples were counted to 2% or 10 minutes, whichever occurs first.	B	7.3	pIC50	50	nM	IC50	US-8815934-B2. 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole and estrogen formulations (2014)
ChEMBL	In vitro inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alpha	B	7.64	pIC50	23	nM	IC50	J Med Chem (2001) 44: 1654-1657 [PMID:11356100]
GtoPdb	-	-	7.64	pIC50	23	nM	IC50	J Med Chem (2001) 44: 1654-7 [PMID:11356100]
ChEMBL	In vitro antagonist effect on estrogen receptor alpha transcriptional activation in MCF-7 cells against 10 pM 17-beta-estradiol	F	8.43	pIC50	3.7	nM	IC50	J Med Chem (2001) 44: 1654-1657 [PMID:11356100]
ChEMBL	Inhibition of binding to recombinant human ERalpha by scintillation proximity assay	B	9.22	pIC50	0.6	nM	IC50	Bioorg Med Chem Lett (2005) 15: 5124-5128 [PMID:16203138]
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
GtoPdb	-	-	7.07	pIC50	85	nM	IC50	J Med Chem (2001) 44: 1654-7 [PMID:11356100]
ChEMBL	In vitro inhibitory concentration against [3H]17-beta-estradiol binding to human estrogen receptor 2	B	7.07	pIC50	85	nM	IC50	J Med Chem (2001) 44: 1654-1657 [PMID:11356100]
ChEMBL	Inhibition of binding to recombinant human ERbeta by scintillation proximity assay	B	8.42	pIC50	3.8	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]