17β-estradiol [Ligand Id: 1013] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL135 (17.beta.-estradiol, 17beta-estradiol, 17-.beta.-oestradiol, 17-beta-oestradiol, Adgyn estro, Agofollin, Alfatradiol, Alora, Aquagen, Bedol, Climara, Climara Pro, Depo-Estradiol, Dermestril 100, Dermestril 25, Dermestril 50, Dermestril septem 25, Dermestril septem 50, Dermestril septem 75, Destradiol, Dihydrotheelin, Dihydroxyestrin, Divigel, E-Cypionate, Elestrim, Elestrin, Elleste solo, Elleste solo mx 40, Elleste solo mx 80, Esclim, Estrace, Estraderm, Estraderm mx 100, Estraderm mx 25, Estraderm mx 50, Estraderm mx 75, Estraderm tts 100, Estraderm tts 25, Estraderm tts 50, Estradiol, Estradiol 17-beta, Estradiol anhydrous, Estradiol hemihydrate, Estradiol valerate metabolite e2, Estrasorb, Estring, Estrogel, Evamist, Evorel 100, Evorel 25, Evorel 50, Evorel 75, Fematrix 40, Fematrix 80, Fempatch, Femseven 100, Femseven 50, Femseven 75, Gvnodiol, Gynergon, Gynodiol, Gynoestryl, Gynogen, Imvexxy, Innofem, Menorest 37.5, Menorest 50, Menorest 75, Menoring 50, Menostar, Minivelle, NSC-20293, NSC-9895, Oestradiol, Progynova ts, Sandrena, Vagifem, Vagifem 18, Vagifem 8, Vivelle, Vivelle-dot, WC3011, WC-3011, Zumenon)
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  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
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  • Corticosteroid binding globulin in Human [ChEMBL: CHEMBL2421] [UniProtKB: P08185]
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  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
  • Estrogen receptor-α/Estrogen receptor alpha in Mouse [ChEMBL: CHEMBL3065] [GtoPdb: 620] [UniProtKB: P19785]
  • Estrogen receptor-α/Estrogen receptor alpha in Rat [ChEMBL: CHEMBL2724] [GtoPdb: 620] [UniProtKB: P06211]
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  • Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
  • Estrogen receptor-β/Estrogen receptor beta in Mouse [ChEMBL: CHEMBL2995] [GtoPdb: 621] [UniProtKB: O08537]
  • Estrogen receptor-β/Estrogen receptor beta in Rat [ChEMBL: CHEMBL3021] [GtoPdb: 621] [UniProtKB: Q62986]
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  • Estrogen-related receptor-α/Estrogen-related receptor alpha in Human [ChEMBL: CHEMBL3429] [GtoPdb: 622] [UniProtKB: P11474]
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  • Estrogen-related receptor-β/Estrogen-related receptor beta in Human [ChEMBL: CHEMBL3751] [GtoPdb: 623] [UniProtKB: O95718]
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  • GPBA receptor/G-protein coupled bile acid receptor 1 in Human [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6]
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  • GPER/G-protein coupled estrogen receptor 1 in Human [ChEMBL: CHEMBL5872] [GtoPdb: 221] [UniProtKB: Q99527]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
  • Organic cation transporter 2/Solute carrier family 22 member 2 in Rat [ChEMBL: CHEMBL1770032] [GtoPdb: 1020] [UniProtKB: Q9R0W2]
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  • Organic cation transporter 3/Solute carrier family 22 member 3 in Human [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751]
  • Organic cation transporter 3/Solute carrier family 22 member 3 in Rat [ChEMBL: CHEMBL1770033] [GtoPdb: 1021] [UniProtKB: O88446]
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  • Solute carrier organic anion transporter family member 1A1 in Rat [ChEMBL: CHEMBL1781859] [UniProtKB: P46720]
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  • Testis-specific androgen-binding protein in Human [ChEMBL: CHEMBL3305] [UniProtKB: P04278]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
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  • KCa1.1 in Human [GtoPdb: 380] [UniProtKB: Q12791]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Alpha-synuclein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6152] [UniProtKB: P37840]
ChEMBL Inhibition of alpha-synuclein aggregation (unknown origin) incubated for 8 days by thioflavin S based fluorescence assay B 4.22 pIC50 60000 nM IC50 Eur J Med Chem (2019) 167: 10-36 [PMID:30743095]
Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
ChEMBL Binding affinity at AR B 7.59 pIC50 26 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 6295-6298 [PMID:17890084]
ChEMBL Inhibitory activity against AR B 7.72 pIC50 19.1 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 834-838 [PMID:16309907]
ChEMBL Binding affinity to androgen receptor B 7.72 pIC50 19.1 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 2944-2948 [PMID:17448656]
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 6.63 pKi 235 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) B 6.39 pIC50 407.38 nM IC50 J. Med. Chem. (2005) 48: 5666-5674 [PMID:16134935]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 6.45 pIC50 353 nM IC50 DrugMatrix in vitro pharmacology data
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
ChEMBL DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) B 4.95 pIC50 11295 nM IC50 DrugMatrix in vitro pharmacology data
Corticosteroid binding globulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2421] [UniProtKB: P08185]
ChEMBL In silico binding affinity to human corticosteriod binding globulin B 4 pKd 4 - -Log Kdiss J. Med. Chem. (1997) 40: 3161-3172 [PMID:9379435]
ChEMBL Binding affinity to human CBG receptor (corticosteroid-binding globulins) B 5 pKi 10000 nM Ki J. Med. Chem. (2004) 47: 2732-2742 [PMID:15139751]
CYP1B1/Cytochrome P450 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4878] [GtoPdb: 1320] [UniProtKB: Q16678]
ChEMBL Inhibition of human CYP1B1 expressed in supersomes using ethoxyresorufin as substrate after 20 mins in presence of NADP by Dixon plot analysis B 5.72 pKi 1900 nM Ki Eur J Med Chem (2017) 135: 296-306 [PMID:28458135]
ChEMBL Inhibition of recombinant human CYP1B1 expressed in bacterial microsomes co-expressing P450 reductase using 7-ethyl-O-resorufin as substrate after 45 mins in presence of NADPH by fluorescence assay B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem Lett (2016) 26: 5272-5276 [PMID:27687674]
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 4.93 pKi 11847 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 4.83 pIC50 14911 nM IC50 DrugMatrix in vitro pharmacology data
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
ChEMBL Binding affinity to purified human ERalpha LBD assessed as dissociation constant incubated for 2 hrs by fluorescence tracer based competitive fluorometric binding assay B 8.46 pKd 3.49 nM Kd Eur J Med Chem (2019) 172: 48-61 [PMID:30939353]
ChEMBL Displacement of fluorescein-labeled ES2 from human recombinant ERalpha receptor after 2 hrs by fluorescence polarization assay B 8.52 pKd 3 nM Kd Bioorg. Med. Chem. (2014) 22: 303-310 [PMID:24315190]
ChEMBL Binding affinity to full-length human estrogen receptor alpha B 9.7 pKd 0.2 nM Kd Bioorg. Med. Chem. (2009) 17: 3479-3488 [PMID:19359182]
ChEMBL Binding affinity to full-length human estrogen receptor alpha B 9.7 pKd 0.2 nM Kd Bioorg. Med. Chem. (2009) 17: 3528-3535 [PMID:19394231]
ChEMBL Binding affinity for human estrogen receptor alpha B 9.7 pKd 0.2 nM Kd J. Med. Chem. (2003) 46: 4032-4042 [PMID:12954056]
ChEMBL Binding affinity to human full-length ERalpha receptor B 9.7 pKd 0.2 nM Kd Eur. J. Med. Chem. (2011) 46: 2453-2462 [PMID:21481497]
ChEMBL Binding affinity to human full length estrogen receptor alpha by Scatchard plot analysis B 9.7 pKd 0.2 nM Kd J. Med. Chem. (2013) 56: 3346-3366 [PMID:23586645]
ChEMBL Binding affinity to human full length ERalpha receptor B 9.7 pKd 0.2 nM Kd Eur. J. Med. Chem. (2009) 44: 3412-3424 [PMID:19286283]
ChEMBL Displacement of [3H]estradiol from human ERalpha B 9.7 pKd 0.2 nM Kd J. Med. Chem. (2006) 49: 5001-5012 [PMID:16884312]
ChEMBL Binding affinity for human estrogen receptor alpha by displacement of [3H]estradiol B 7 pKi 100 nM Ki J. Med. Chem. (2003) 46: 4032-4042 [PMID:12954056]
ChEMBL Binding affinity to ERalpha B 7.92 pKi 12 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 3212-3216 [PMID:17379515]
ChEMBL Ability to displace [3H]17-beta-estradiol from Estrogen receptor alpha by scintillation proximity assay. B 8.66 pKi 2.2 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1939-1942 [PMID:11459665]
ChEMBL Displacement of [3H]estradiol from full length biotinylated human ERalpha by scintillation proximity assay B 8.7 pKi 2 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 5075-5077 [PMID:18722117]
ChEMBL Binding affinity for human estrogen receptor alpha B 8.7 pKi 2 nM Ki J. Med. Chem. (2005) 48: 2243-2247 [PMID:15771467]
ChEMBL DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) B 9.34 pKi 0.46 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of E2-Alexa633 from GFP-tagged ERalpha expressed in COS7 cells by FACS B 9.52 pKi 0.3 nM Ki Nat. Chem. Biol. (2006) 2: 207-212 [PMID:16520733]
ChEMBL Binding Assay: The method employed was adapted from the scientific literature and described in detail by Osbourn et al. (1993, Biochemistry, 32, 6229-6236). Recombinant human ERalpha and ERR proteins were purified from transfected Sf9-cells. The in vitro assays involved the use of either ERalpha or ERbeta proteins and [3H]E2, at a fixed concentration of 0.5 nM, as the labeled ligand. Recombinant human ERalpha or ERbeta proteins were dissolved in binding buffer (10 mM Tris-HCL, pH 7.5, 10% glycerol, 1 mM DTT, 1 mg/ml BSA) and duplicate aliquots were then incubated with [3H]E2 at a final concentration of 0.5 nM, together with a vehicle control (0.4% DMSO), or the same amount of vehicle containing increasing concentrations of unlabeled steroid ligands as competitors. After incubation for 2 h at 25 C., the unbound ligands were removed and the amounts of [3H]E2 bound to either ERalpha or ERbeta proteins were measured. B 9.68 pKi 0.21 nM Ki US-9034854-B2. Pharmaceutical composition comprising estetrol derivatives for use in cancer therapy (2015)
ChEMBL Inhibition Assay: The method employed was adapted from the scientific literature and described in detail by Osboum et al. (1993, Biochemistry, 32, 6229-6236). Recombinant human ERalpha and ERbeta proteins were purified from transfected Sf9-cells. The in vitro assays involved the use of either ERalpha or ERbeta proteins and [3H]E2, at a fixed concentration of 0.5 nM, as the labeled ligand. Recombinant human ERalpha or ERbeta proteins were dissolved in binding buffer (10 mM Tris-HCL, pH 7.5, 10% glycerol, 1 mM DTT, 1 mg/ml BSA) and duplicate aliquots were then incubated with [3H]E2 at a final concentration of 0.5 nM, together with a vehicle control (0.4% DMSO), or the same amount of vehicle containing increasing concentrations of unlabeled steroid ligands as competitors. After incubation for 2 h at 25 C., the unbound ligands were removed and the amounts of [3H]E2 bound to either ERalpha or ERbeta proteins were measured. B 9.68 pKi 0.21 nM Ki US-9040509-B2. Method of treating human skin and a skin care composition for use in such a method (2015)
ChEMBL Displacement of [2,4,6,7-3H]estradiol from human ERalpha expressed in HeLa cells after 18 hrs by liquid scintillation counting B 9.8 pKi 0.16 nM Ki Bioorg. Med. Chem. (2010) 18: 5593-5601 [PMID:20621492]
GtoPdb - - 9.82 pKi - - - Endocrinology (1997) 138: 863-70 [PMID:9048584]
ChEMBL Binding affinity to ERalpha L384M/M421G mutant B 7.34 pIC50 46 nM IC50 J. Med. Chem. (2006) 49: 5404-5407 [PMID:16942012]
ChEMBL Inhibition of human estrogen receptor beta B 7.34 pIC50 46 nM IC50 Bioorg. Med. Chem. (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL Inhibition of [3H]estradiol binding to human estrogen receptor alpha expressed in HeLa cells B 7.55 pIC50 28 nM IC50 J. Med. Chem. (2005) 48: 364-379 [PMID:15658851]
ChEMBL Inhibitory concentration against estrogen receptor alpha using radioligand binding assay. B 7.55 pIC50 28 nM IC50 J. Med. Chem. (2003) 46: 2945-2957 [PMID:12825935]
ChEMBL Antagonist activity at ERalpha-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay F 7.68 pIC50 21.04 nM IC50 J. Med. Chem. (2010) 53: 6947-6953 [PMID:20812681]
ChEMBL Inhibition of fluorescence-labeled 17beta-estradiol binding to ERalpha receptor after 2 hrs by fluorometric analysis B 7.74 pIC50 18 nM IC50 J. Nat. Prod. (2011) 74: 937-942 [PMID:21510635]
ChEMBL Displacement of [3H]17beta-estradiol from human ERalpha expressed in SF9 cells B 7.9 pIC50 12.5 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 6740-6744 [PMID:19836949]
ChEMBL Binding affinity towards estrogen receptor alpha by [3H]17-beta-estradiol displacement. B 7.96 pIC50 11 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 2327-2330 [PMID:15081034]
ChEMBL Binding affinity to ERalpha by fluorescence polarization-based competitive binding assay B 7.99 pIC50 10.12 nM IC50 J. Med. Chem. (2010) 53: 4290-4294 [PMID:20408532]
ChEMBL Displacement of [3H]estrone from ER alpha B 8 pIC50 10 nM IC50 J. Med. Chem. (2006) 49: 2440-2455 [PMID:16610787]
ChEMBL Displacement of [3H]17-beta-estradiol from human estrogen receptor alpha B 8.23 pIC50 5.9 nM IC50 J. Med. Chem. (1999) 42: 3126-3133 [PMID:10447957]
ChEMBL Displacement of Fluormone ES2 Green from full-length estrogen receptor alpha (unknown origin) after 2 hrs by fluorescence polarization assay B 8.24 pIC50 5.7 nM IC50 J Med Chem (2018) 61: 514-534 [PMID:28426931]
ChEMBL Displacement of fluorescein-labeled estrogen from human recombinant ERalpha by fluorescence polarization based competitive binding affinity assay B 8.24 pIC50 5.7 nM IC50 J. Med. Chem. (2014) 57: 9370-9382 [PMID:25369367]
ChEMBL Inhibition of fluoromone binding to recombinant human full length untagged ERalpha expressed in insect cells after 2 hrs by fluorescence polarization assay B 8.32 pIC50 4.8 nM IC50 J Nat Prod (2018) 81: 1343-1356 [PMID:29869503]
ChEMBL Binding affinity to human ERalpha B 8.33 pIC50 4.7 nM IC50 J. Med. Chem. (2007) 50: 4471-4481 [PMID:17696335]
ChEMBL Displacement of Fluormone ES2 Green from human recombinant full length ERalpha expressed in insect cells measured up to 4 hrs by fluorescence polarization assay B 8.36 pIC50 4.4 nM IC50 Bioorg Med Chem (2016) 24: 5495-5504 [PMID:27647375]
ChEMBL Binding affinity to human recombinant ERalpha receptor by liquid scintillation counter B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5050-5053 [PMID:18760603]
ChEMBL Inhibition of human LBD of of ERalpha B 8.44 pIC50 3.6 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 118-122 [PMID:17049855]
ChEMBL Displacement of radioligand from Estrogen receptor alpha B 8.47 pIC50 3.4 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 1283-1285 [PMID:11965371]
ChEMBL Inhibitory concentration against human ER alpha expressed in Escherichia coli was determined using [3H]17-beta-estradiol as radio ligand B 8.49 pIC50 3.2 nM IC50 J. Med. Chem. (2004) 47: 5021-5040 [PMID:15456246]
ChEMBL Binding affinity towards human estrogen receptor alpha(ERalpha) B 8.49 pIC50 3.2 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2399-2403 [PMID:12824043]
ChEMBL Binding affinity for human Estrogen receptor alpha B 8.49 pIC50 3.2 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 4925-4929 [PMID:15341953]
ChEMBL Inhibition of human ERalpha by radioligand binding assay B 8.49 pIC50 3.2 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 902-906 [PMID:17188490]
ChEMBL Inhibition of human estrogen receptor alpha B 8.49 pIC50 3.2 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 3137-3142 [PMID:15876535]
ChEMBL Inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alpha expressed in Escherichia coli B 8.49 pIC50 3.2 nM IC50 J. Med. Chem. (2005) 48: 3953-3979 [PMID:15943471]
ChEMBL Binding affinity for human Estrogen receptor alpha B 8.49 pIC50 3.2 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 4520-4525 [PMID:16098741]
ChEMBL Displacement of fluorescent estrogen ES2 from human recombinant ERalpha by fluorescence polarization assay B 8.49 pIC50 3.2 nM IC50 J. Nat. Prod. (2009) 72: 1603-1607 [PMID:19705860]
ChEMBL Displacement of [3H]17-beta-estradiol from human Estrogen receptor alpha B 8.52 pIC50 3 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 147-151 [PMID:10673099]
ChEMBL Agonist activity at human GST-tagged estrogen receptor alpha ligand binding domain assessed as coactivator peptide PGC1a recruitment by TR-FRET assay B 8.59 pIC50 2.58 nM IC50 J Med Chem (2018) 61: 4720-4738 [PMID:29741891]
ChEMBL In vitro binding affinity for estrogen receptor alpha B 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1919-1922 [PMID:12749898]
ChEMBL Luciferase Assay: Estrogen receptor-negative CV-1 kidney cells are maintained in Dulbecco's modified Eagle's medium with 4.5 g/L glucose supplemented with 10% fetal bovine serum and 100 units/ml penicillin-streptomycin at 37° C. in a humidified 5% CO2 atmosphere. The cells are then plated in 6-well dishes at a density of 2×10^5 cells per well in phenol-red free Dulbecco's modified Eagle's medium containing 10% charcoal-dextran-stripped fetal bovine serum. CV-1 cells are transfected using LipofectAMINE reagent according to the manufacturer's protocol. Transfections containing 1.5 μg of reporter plasmid (containing ERE-tk-luciferase containing a single ERE cloned upstream of the thymidine kinase promoter and luciferase gene) and 0.5 μg of either ERα or ERβ expression vector (containing CMV-ERα or CMV-ERβ full length coding sequence respectively). The next day, cells receive no treatment (controls) or are treated with estradiol alone (1 nM) or estradiol plus a compound of the invention (at varying concentrations). After 16-24 hours, cells are harvested and assayed for luciferase activity. At the outset, cell monolayers are washed twice with ice-cold phosphate-buffered saline and incubated for 15 minutes in 250 μl of 1× cell culture lysis reagent (Promega, Madison, Wis.). Cell extracts are transferred to a fresh tube and assayed using the luciferase assay system (Promega). For each assay, 10 μl of extract is diluted with 90 μl of 1× cell culture lysis reagent. Luminescence is read using an AutoLumat LB953 luminometer. B 8.72 pIC50 1.9 nM IC50 US-9422324-B2. 6-substituted demethyl-estradiol derivatives as selective ER-β agonists (2016)
ChEMBL Inhibition of ER-alpha (unknown origin) by Lanthascreen-FRET assay B 8.77 pIC50 1.7 nM IC50 Bioorg. Med. Chem. (2016) 24: 4075-4099 [PMID:27407030]
ChEMBL DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) B 8.79 pIC50 1.61 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity to human ER alpha B 8.8 pIC50 1.6 nM IC50 J. Med. Chem. (2006) 49: 5404-5407 [PMID:16942012]
ChEMBL Binding affinity to human ERalpha B 8.85 pIC50 1.4 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 834-838 [PMID:16309907]
ChEMBL Binding affinity to human recombinant ERalpha by scintillation proximity assay B 8.85 pIC50 1.4 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 2944-2948 [PMID:17448656]
ChEMBL Binding affinity at human recombinant ERalpha B 8.85 pIC50 1.4 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 6295-6298 [PMID:17890084]
ChEMBL Binding affinity to ERalpha B 8.87 pIC50 1.35 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 1468-1472 [PMID:16412638]
ChEMBL Binding affinity to human recombinant ERalpha by scintillation proximity assay B 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 4652-4656 [PMID:16777408]
ChEMBL Binding affinity to human ERalpha B 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 3896-3901 [PMID:16730987]
ChEMBL Binding affinity to ERalpha by scintillation proximity assay B 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 3489-3494 [PMID:16632357]
ChEMBL Binding affinity against human estrogen receptor alpha in competitive binding assay B 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 1417-1421 [PMID:15006374]
ChEMBL Inhibition of bindign to recombinant human estrogen receptor alpha B 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 107-113 [PMID:15582421]
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]
ChEMBL Binding affinity for human estrogen receptor alpha B 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 3753-3755 [PMID:15203156]
ChEMBL Inhibition of estrogen receptor alpha B 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 1675-1681 [PMID:15745820]
ChEMBL Binding affinity towards human recombinant Estrogen receptor alpha was determined B 8.89 pIC50 1.3 nM IC50 J. Med. Chem. (2004) 47: 2171-2175 [PMID:15084115]
ChEMBL Binding affinity for human estrogen receptor alpha B 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 3747-3751 [PMID:15203155]
ChEMBL Binding potency for human ER alpha B 8.89 pIC50 1.3