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

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ChEMBL ligand: CHEMBL691 (Ethinyl estradiol component of estrostep fe, Ethinyl estradiol component of femlyv, Ethinyl estradiol component of xulane, Ethinyl estradiol component of twirla, Lynoral, Ethinylestradiolum, Ethinyl estradiol component of sprintec, 17alpha-ethinylestradiol, Ethinyl estradiol component of viorele, Etinilestradiol, Ethinyl estradiol component of lo minastrin fe, Ethinyl estradiol component of yasmin, Ethinyl estradiol component of isibloom, Ethinyl estradiol component of aranelle, Ethinyl estradiol component of volnea, Ethinyl estradiol component of femhrt, Ethinyl estradiol component of yaz, Ethinyl estradiol component of cyclessa, Ethinyl estradiol component of ortho-cept, NSC-10973, Ethinyl estradiol component of ovral, Ethinyl estradiol component of nuvaring, Ethinyl estradiol component of bekyree, Ethinyl estradiol component of loseasonique, Ethinyl estradiol component of pimtrea, Ovulen, Ethinyl estradiol component of preven, Ethinyl estradiol component of elifemme, Ethinyl estradiol component of zovia, Ethinyl estradiol component of mircette, Ethinyl estradiol component of brevicon, Ethinyl estradiol component of vienva, Ethinyl estradiol component of triphasil, Ethinyl estradiol component of orsythia, 17-ethinylestradiol, Ethinyl estradiol component of tri lo sprintec, Ethynylestradiol, Ethinyl estradiol component of seasonique, Ethinyl estradiol component of enskyce, Ethinyl estradiol component of seasonale, Ethinyl estradiol component of lo loestrin fe, Follicoral, Ethinyl estradiol component of tri-sprintec, Ethinyl estradiol component of aviane, Ethinyl estradiol component of nordette, Ethinyl estradiol component of previfem, Ethinyl estradiol component of lybrel, Ethinyl estradiol component of enpresse, Feminone, Ethinyl estradiol component of kariva, Enovid-e, Ethinyl estradiol component of altavera, Ethinyl estradiol component of beyaz, Ethinyl estradiol component of desogen, Ginestrene, Ethinyl estradiol component of taytulla, Ethinyl estradiol component of safyral, Ethinyl estradiol component of minastrin 24 fe, Ovulen-21, Ethinylestradiol, Ethinyl estradiol component of trivora, Ethinyl estradiol component of marlissa, Estinyl, Enovid, Ethinyl estradiol component of portia, Ethinyl estradiol component of kurvelo, Ethinyl estradiol component of alesse, Ethinyl estradiol component of levlite, Ethinyl estradiol component of kelnor, Ethinyl estradiol component of ortho tri-cyclen, Ethinyl estradiol component of norquest fe, Ethinyl estradiol component of levora, Ethinyl estradiol component of cryselle, Ethinyl estradiol component of tri-previfem, Ethinyl estradiol component of quartette, Ethinyl estradiol component of balcoltra, Ovulen-28, Ethinyl estradiol component of vyfemla, Ethinyl estradiol component of norinyl, Ethinyl estradiol component of annovera, Ethinyl estradiol, Ethinyl estradiol component of velivet, Ethinyl estradiol component of lessina, Etinestryl, Ethinyl estradiol component of quasense, Ethinyl estradiol component of tyblume, Ethinyl estradiol component of femcon fe, Ethinyl estradiol component of setlakin, Ethinyl estradiol component of tri-legest fe, Ethinyl estradiol component of levonest, Ethinyl estradiol component of introvale)
  • 5-hydroxytryptamine receptor 4 in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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  • A2A receptor/Adenosine receptor A2a in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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  • A3 receptor/Adenosine receptor A3 in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • aldehyde oxidase 1/Aldehyde oxidase in Human [ChEMBL: CHEMBL3257] [GtoPdb: 3186] [UniProtKB: Q06278]
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  • Estrogen receptor-α/Estrogen receptor 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-type 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-type opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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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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  • Polyunsaturated fatty acid lipoxygenase ALOX15 in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
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  • Sex hormone-binding globulin in Human [ChEMBL: CHEMBL3305] [UniProtKB: P04278]
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  • DAT/Sodium-dependent dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
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  • NET/Sodium-dependent noradrenaline transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • SERT/Sodium-dependent 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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  • 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
5-hydroxytryptamine receptor 4 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
A2A receptor/Adenosine receptor A2a 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 receptor A3 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
aldehyde oxidase 1/Aldehyde oxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3257] [GtoPdb: 3186] [UniProtKB: Q06278]
ChEMBL Inhibition of human liver AOX using phthalazine as substrate incubated for 2.5 mins by HPLC-MS analysis B 8.3 pIC50 5 nM IC50 Eur J Med Chem (2020) 187: 111948-111948 [PMID:31877540]
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
Estrogen receptor-α/Estrogen receptor 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-type 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-type 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
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]
Polyunsaturated fatty acid lipoxygenase ALOX15 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
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
Sex hormone-binding globulin 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]
DAT/Sodium-dependent 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
NET/Sodium-dependent noradrenaline 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
SERT/Sodium-dependent 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]
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 36:

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]