ChEMBL ligand: CHEMBL46740 (Bazedoxifene, Bazedoxifeno)
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	Displacement of fluorochrome-tagged estrogen from human recombinant estrogen receptor-alpha incubated for 2 hr by competitive binding based microplate reader analysis	B	6.47	pIC50	339.2	nM	IC50	RSC Med Chem (2024) 15: 1329-1347 [PMID:38665833]
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 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]