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ChEMBL ligand: CHEMBL691 (17alpha-ethinylestradiol, 17-ethinylestradiol, Enovid, Enovid-E, Estinyl, Ethinyl estradiol, Ethinylestradiol, Ethinyl Estradiol, Ethinylestradiolum, Ethinyloestradiol, Ethynylestradiol, Etinestryl, Feminone, Follicoral, Ginestrene, Lynoral, Norinyl, NSC-10973, Ovulen, Ovulen-21, Ovulen-28) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 |
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/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 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]