ethinylestradiol [Ligand Id: 7071] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL691 (17alpha-ethinylestradiol, 17-ethinylestradiol, Enovid, Enovid-E, Estinyl, Ethinylestradiol, Ethinyl estradiol, Ethinyl Estradiol, Ethinylestradiolum, Ethinyloestradiol, Ethynylestradiol, Etinestryl, Feminone, Follicoral, Ginestrene, Lynoral, Norinyl, NSC-10973, Ovulen, Ovulen-21, Ovulen-28)
  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • 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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  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
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  • Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
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  • MATE2/Multidrug and toxin extrusion protein 2 in Human [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • Constitutive androstane receptor/Nuclear receptor subfamily 1 group I member 3 in Human [ChEMBL: CHEMBL5503] [GtoPdb: 607] [UniProtKB: Q14994]
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  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
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  • Testis-specific androgen-binding protein in Human [ChEMBL: CHEMBL3305] [UniProtKB: P04278]
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  • Proton-coupled Amino acid Transporter 1 in Human [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) B 4.93 pKi 11751 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) B 4.68 pIC50 20931 nM IC50 DrugMatrix in vitro pharmacology data
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 4.73 pKi 18610 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 4.48 pIC50 32925 nM IC50 DrugMatrix in vitro pharmacology data
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 5.96 pKi 1090 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 5.09 pIC50 8128.31 nM IC50 J Med Chem (2005) 48: 5666-5674 [PMID:16134935]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 5.79 pIC50 1634 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 5.25 pIC50 5678 nM IC50 DrugMatrix in vitro pharmacology data
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 6.35 pKi 444 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 6.25 pIC50 559 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 DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) B 9.89 pKi 0.13 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity to ERalpha by fluorescence polarization-based competitive binding assay B 8.1 pIC50 8.04 nM IC50 J Med Chem (2010) 53: 4290-4294 [PMID:20408532]
ChEMBL Binding affinity to ERalpha B 8.7 pIC50 2 nM IC50 J Med Chem (2006) 49: 3056-3059 [PMID:16722623]
GtoPdb - - 8.7 pIC50 2 nM IC50 J Med Chem (2006) 49: 3056-9 [PMID:16722623]
ChEMBL DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) B 9.35 pIC50 0.45 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Antagonist activity at full length human ERalpha receptor assessed as inhibition of estradiol-induced activation incubated for 22 to 24 hrs by cell based luciferase reporter gene assay B 7.3 pEC50 >50 nM EC50 Bioorg Med Chem (2020) 28: 115670-115670 [PMID:32912438]
ChEMBL Agonist activity at full length human ERalpha receptor assessed as transcriptional activity incubated for 22 to 24 hrs by cell based luciferase reporter gene assay B 9.52 pEC50 0.3 nM EC50 Bioorg Med Chem (2020) 28: 115670-115670 [PMID:32912438]
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
ChEMBL Binding affinity to ERbeta by fluorescence polarization-based competitive binding assay B 7.75 pIC50 17.78 nM IC50 J Med Chem (2010) 53: 4290-4294 [PMID:20408532]
GtoPdb - - 8.09 pIC50 8.1 nM IC50 J Med Chem (2006) 49: 3056-9 [PMID:16722623]
ChEMBL Binding affinity to ERbeta B 8.09 pIC50 8.1 nM IC50 J Med Chem (2006) 49: 3056-3059 [PMID:16722623]
ChEMBL Antagonist activity at full length human ERbeta receptor assessed as inhibition of estradiol-induced activation incubated for 22 to 24 hrs by cell based luciferase reporter gene assay B 8 pEC50 >10 nM EC50 Bioorg Med Chem (2020) 28: 115670-115670 [PMID:32912438]
ChEMBL Displacement of fluormone from GST-tagged ERbeta receptor LBD (unknown origin) measured after 60 mins by TR-FRET competitive binding assay B 9.43 pEC50 0.37 nM EC50 Bioorg Med Chem (2020) 28: 115670-115670 [PMID:32912438]
ChEMBL Agonist activity at full length human ERbeta receptor assessed as transcriptional activity incubated for 22 to 24 hrs by cell based luciferase reporter gene assay B 9.8 pEC50 0.16 nM EC50 Bioorg Med Chem (2020) 28: 115670-115670 [PMID:32912438]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 6.11 pKi 777 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 5.77 pIC50 1710 nM IC50 DrugMatrix in vitro pharmacology data
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 4.98 pKi 10358 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 4.59 pIC50 25894 nM IC50 DrugMatrix in vitro pharmacology data
Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
ChEMBL Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay B 4.68 pIC50 21100 nM IC50 J Med Chem (2013) 56: 781-795 [PMID:23241029]
MATE2/Multidrug and toxin extrusion protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8]
ChEMBL Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay B 4.69 pIC50 20200 nM IC50 J Med Chem (2013) 56: 781-795 [PMID:23241029]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 4.96 pKi 10867 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 4.57 pIC50 26769 nM IC50 DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 6.02 pKi 951 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 6.02 pIC50 959 nM IC50 DrugMatrix in vitro pharmacology data
Constitutive androstane receptor/Nuclear receptor subfamily 1 group I member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5503] [GtoPdb: 607] [UniProtKB: Q14994]
ChEMBL Inverse agonist activity at GAL4 fused-human CAR-LBD transfected HEK293 cells after 24 hrs by luciferase reporter gene assay B 5.52 pIC50 3000 nM IC50 Eur J Med Chem (2016) 108: 505-528 [PMID:26717202]
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0]
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 6.86 pKi 139 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 5.97 pIC50 1067 nM IC50 DrugMatrix in vitro pharmacology data
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808) B 5.88 pKi 1326 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808) B 5.1 pIC50 7953 nM IC50 DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 7.54 pKi 29 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 7.27 pIC50 54 nM IC50 DrugMatrix in vitro pharmacology data
Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
ChEMBL Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay B 5.66 pIC50 2200 nM IC50 J Med Chem (2013) 56: 781-795 [PMID:23241029]
Testis-specific androgen-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3305] [UniProtKB: P04278]
ChEMBL Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin B 6.81 pKd 154.88 nM Kd J Med Chem (2008) 51: 2047-2056 [PMID:18330978]
Proton-coupled Amino acid Transporter 1 in Human [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
GtoPdb - - 4.6 pIC50 - - - J Pharm Sci (2021) 110: 354-364 [PMID:32835702]

ChEMBL data shown on this page come from version 32:

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]