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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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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 |