diethylstilbestrol [Ligand Id: 2801] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL411 (Apstil, Cyren a, Diethylstilbestrol, Dietilestilbestrol, Distilbene, Estrobene, Estrogenine, Estromenin, Fonatol, New-estranol 1, NSC-3070, Palestrol, Stilbestro, Stilbestroform, Stilbestrol, Stilbetin, Stilboesterol, Stilboestrol, Synestrin, Synthestrin, Tampovagan)
  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
There should be some charts here, you may need to enable JavaScript!
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
There should be some charts here, you may need to enable JavaScript!
  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
There should be some charts here, you may need to enable JavaScript!
  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
There should be some charts here, you may need to enable JavaScript!
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
There should be some charts here, you may need to enable JavaScript!
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
There should be some charts here, you may need to enable JavaScript!
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
There should be some charts here, you may need to enable JavaScript!
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
There should be some charts here, you may need to enable JavaScript!
  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
There should be some charts here, you may need to enable JavaScript!
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
There should be some charts here, you may need to enable JavaScript!
  • Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
There should be some charts here, you may need to enable JavaScript!
  • ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
There should be some charts here, you may need to enable JavaScript!
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
There should be some charts here, you may need to enable JavaScript!
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
There should be some charts here, you may need to enable JavaScript!
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
There should be some charts here, you may need to enable JavaScript!
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
There should be some charts here, you may need to enable JavaScript!
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
There should be some charts here, you may need to enable JavaScript!
  • Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
There should be some charts here, you may need to enable JavaScript!
  • Estrogen-related receptor-γ/Estrogen-related receptor gamma in Human [ChEMBL: CHEMBL4245] [GtoPdb: 624] [UniProtKB: P62508]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
There should be some charts here, you may need to enable JavaScript!
  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
There should be some charts here, you may need to enable JavaScript!
  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
There should be some charts here, you may need to enable JavaScript!
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
There should be some charts here, you may need to enable JavaScript!
  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
There should be some charts here, you may need to enable JavaScript!
  • NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
There should be some charts here, you may need to enable JavaScript!
  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit [ChEMBL: CHEMBL4693] [UniProtKB: P04191]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
There should be some charts here, you may need to enable JavaScript!
  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • V1A receptor/Vasopressin V1a receptor in Human [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288]
There should be some charts here, you may need to enable JavaScript!
  • Estrogen-related receptor-α in Mouse [GtoPdb: 622] [UniProtKB: O08580]
There should be some charts here, you may need to enable JavaScript!
  • Estrogen-related receptor-β in Human [GtoPdb: 623] [UniProtKB: O95718]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine) B 4.59 pIC50 25550 nM IC50 DrugMatrix in vitro pharmacology data
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) B 5.78 pKi 1666 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) B 5.54 pIC50 2856 nM IC50 DrugMatrix in vitro pharmacology data
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 5.3 pKi 5060 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) B 5.05 pIC50 9013 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 5.9 pKi 1248 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 5.66 pIC50 2208 nM IC50 DrugMatrix in vitro pharmacology data
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 5.1 pKi 7888 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 4.71 pIC50 19487 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 5.27 pKi 5321 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 4.97 pIC50 10826 nM IC50 DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 5.28 pKi 5297 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 4.85 pIC50 14127 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.27 pKi 5340 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 4.93 pIC50 11698 nM IC50 DrugMatrix in vitro pharmacology data
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 5.66 pKi 2201 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 4.82 pIC50 15151 nM IC50 DrugMatrix in vitro pharmacology data
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) B 4.85 pIC50 14125.38 nM IC50 J Med Chem (2005) 48: 5666-5674 [PMID:16134935]
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
ChEMBL DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) B 5.53 pIC50 2963 nM IC50 DrugMatrix in vitro pharmacology data
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
ChEMBL TP_TRANSPORTER: drug resistance(Mitoxantrone) in BCRP-expressing K562 cells F 6.3 pIC50 500 nM IC50 Mol Cancer Ther (2003) 2: 105-112 [PMID:12533678]
ChEMBL TP_TRANSPORTER: drug resistance(SN-38) in BCRP-expressing K562 cells F 6.3 pIC50 >500 nM IC50 Mol Cancer Ther (2003) 2: 105-112 [PMID:12533678]
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 4.89 pKi 12755 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 4.66 pIC50 22088 nM IC50 DrugMatrix in vitro pharmacology data
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 5.25 pIC50 5600 nM IC50 DrugMatrix in vitro pharmacology data
CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
ChEMBL DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) B 5.05 pKi 8872 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) B 4.75 pIC50 17745 nM IC50 DrugMatrix in vitro pharmacology data
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 6.02 pKi 958 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 5.57 pIC50 2718 nM IC50 DrugMatrix in vitro pharmacology data
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 5.41 pKi 3882 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 5.11 pIC50 7763 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 5.35 pKi 4440 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 4.88 pIC50 13321 nM IC50 DrugMatrix in vitro pharmacology data
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 5.52 pKi 2987 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 5.06 pIC50 8796 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 6.07 pKi 851 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.97 pIC50 1071 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 In vitro displacement of 0.5 nM [3H]17-beta-estradiol from human Estrogen receptor alpha B 9.31 pKi 0.49 nM Ki J Med Chem (2003) 46: 1408-1418 [PMID:12672240]
ChEMBL DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) B 9.58 pKi 0.26 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]Estradiol from human recombinant estrogen receptor alpha expressed in Sf9 cells after 2 hrs B 9.66 pKi 0.22 nM Ki Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [3H]estradiol from human ER-alpha expressed in Sf21 cells incubated for 120 mins by scintillation counting analysis B 9.7 pKi 0.2 nM Ki Bioorg Med Chem (2024) 101: 117645-117645 [PMID:38401456]
GtoPdb - - 10.4 pKi - - - Endocrinology (1997) 138: 863-70 [PMID:9048584]
ChEMBL Displacement of [3H]-estradiol from human recombinant ERalpha expressed in Sf21 cells after 2 hrs B 6.11 pIC50 770 nM IC50 Bioorg Med Chem Lett (2012) 22: 4307-4309 [PMID:22652053]
ChEMBL In vitro inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alpha B 8.52 pIC50 3 nM IC50 J Med Chem (2001) 44: 1654-1657 [PMID:11356100]
ChEMBL DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) B 9.04 pIC50 0.92 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]Estradiol from human recombinant estrogen receptor alpha expressed in Sf9 cells after 2 hrs B 9.11 pIC50 0.77 nM IC50 Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [3H]estradiol from human ER-alpha expressed in Sf21 cells incubated for 120 mins by scintillation counting analysis B 9.15 pIC50 0.7 nM IC50 Bioorg Med Chem (2024) 101: 117645-117645 [PMID:38401456]
ChEMBL Displacement of radioligand from Estrogen receptor alpha B 9.48 pIC50 0.33 nM IC50 Bioorg Med Chem Lett (2002) 12: 1283-1285 [PMID:11965371]
ChEMBL Inhibition of [3H]17-beta-estradiol binding to human recombinant Estrogen receptor alpha. B 7.92 pEC50 12 nM EC50 J Med Chem (2002) 45: 1399-1401 [PMID:11906280]
ChEMBL Agonist activity at ER-alpha (unknown origin) by ER-alpha coactivator assay B 8.6 pEC50 2.5 nM EC50 Bioorg Med Chem (2024) 101: 117645-117645 [PMID:38401456]
ChEMBL Agonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ER-alpha-mediated transcriptional activity by luciferase reporter gene assay B 9.7 pEC50 0.2 nM EC50 Bioorg Med Chem (2019) 27: 1952-1961 [PMID:30940565]
ChEMBL Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation by luciferase reporter gene assay B 9.96 pEC50 0.11 nM EC50 Bioorg Med Chem (2019) 27: 1952-1961 [PMID:30940565]
ChEMBL Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor alpha. B 10.22 pEC50 0.06 nM EC50 J Med Chem (2002) 45: 1399-1401 [PMID:11906280]
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
ChEMBL In vitro displacement of 0.5 nM [3H]17-beta-estradiol from human Estrogen receptor beta B 9.2 pKi 0.63 nM Ki J Med Chem (2003) 46: 1408-1418 [PMID:12672240]
GtoPdb - - 9.8 pKi - - - Endocrinology (1997) 138: 863-70 [PMID:9048584]
ChEMBL Displacement of [3H]-estradiol from human recombinant ERbeta expressed in Sf21 cells after 2 hrs B 6.21 pIC50 610 nM IC50 Bioorg Med Chem Lett (2012) 22: 4307-4309 [PMID:22652053]
ChEMBL In vitro inhibitory concentration against [3H]17-beta-estradiol binding to human estrogen receptor 2 B 8.4 pIC50 4 nM IC50 J Med Chem (2001) 44: 1654-1657 [PMID:11356100]
ChEMBL Inhibition of [3H]17-beta-estradiol binding to human recombinant Estrogen receptor beta. B 8.05 pEC50 9 nM EC50 J Med Chem (2002) 45: 1399-1401 [PMID:11906280]
ChEMBL Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor beta. B 10.7 pEC50 0.02 nM EC50 J Med Chem (2002) 45: 1399-1401 [PMID:11906280]
Estrogen-related receptor-γ/Estrogen-related receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4245] [GtoPdb: 624] [UniProtKB: P62508]
GtoPdb - - 5.3 pIC50 - - - Genes Dev (2001) 15: 833-8 [PMID:11297507];
Proc Natl Acad Sci USA (2001) 98: 8880-4 [PMID:11447273]
ChEMBL Estrogen-Related Receptor gamma activity in FRET assay F 6.2 pEC50 630 nM EC50 J Med Chem (2005) 48: 3107-3109 [PMID:15857113]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 5.32 pKi 4818 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 4.97 pIC50 10600 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 5.74 pKi 1825 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.34 pIC50 4563 nM IC50 DrugMatrix in vitro pharmacology data
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL DRUGMATRIX: Protein Serine/Threonine Kinase, p38alpha enzyme inhibition (substrate: Myelin Basic Protein) B 4.48 pIC50 32903 nM IC50 DrugMatrix in vitro pharmacology data
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 5.63 pKi 2345 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.24 pIC50 5778 nM IC50 DrugMatrix in vitro pharmacology data
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.44 pKi 3654 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 4.82 pIC50 15171 nM IC50 DrugMatrix in vitro pharmacology data
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.41 pKi 3907 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 4.73 pIC50 18432 nM IC50 DrugMatrix in vitro pharmacology data
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 5.5 pKi 3184 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 5.02 pIC50 9553 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 5.44 pKi 3640 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.44 pIC50 3670 nM IC50 DrugMatrix in vitro pharmacology data
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469]
ChEMBL Antagonist activity at full length human PXR transfected in human HepG2 cells assessed as reduction in rifaximin-induced receptor transactivation after 18 hrs by luciferase reporter assay B 4.84 pIC50 14600 nM IC50 Eur J Med Chem (2015) 103: 551-562 [PMID:26408814]
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0]
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 6.21 pKi 611 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 5.33 pIC50 4682 nM IC50 DrugMatrix in vitro pharmacology data
Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4693] [UniProtKB: P04191]
ChEMBL Inhibition of rabbit microsomes SERCA1a by enzyme-coupled method B 4.85 pIC50 14000 nM IC50 J Med Chem (2020) 63: 1937-1963 [PMID:32030976]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 5.86 pKi 1369 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 5.32 pIC50 4790 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.7 pKi 1998 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.5 pIC50 3140 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 4.57 pKi 26619 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 4.29 pIC50 50819 nM IC50 DrugMatrix in vitro pharmacology data
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.22 pKi 5986 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 4.89 pIC50 12892 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 5.18 pKi 6637 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 4.9 pIC50 12492 nM IC50 DrugMatrix in vitro pharmacology data
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557]
ChEMBL DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) B 5.36 pIC50 4359 nM IC50 DrugMatrix in vitro pharmacology data
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr)) B 4.85 pIC50 14233 nM IC50 DrugMatrix in vitro pharmacology data
UDP-glucose 4-epimerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5843] [UniProtKB: Q14376]
ChEMBL Inhibition of human GalE by HPAEC assay B 4.12 pIC50 75000 nM IC50 Bioorg Med Chem Lett (2006) 16: 5744-5747 [PMID:16962325]
V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288]
ChEMBL DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr) B 4.98 pKi 10401 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr) B 4.59 pIC50 25925 nM IC50 DrugMatrix in vitro pharmacology data
Estrogen-related receptor-α in Mouse [GtoPdb: 622] [UniProtKB: O08580]
GtoPdb - - 5.3 pIC50 - - - Genes Dev (2001) 15: 833-8 [PMID:11297507]
Estrogen-related receptor-β in Human [GtoPdb: 623] [UniProtKB: O95718]
GtoPdb - - 5.3 pIC50 - - - Genes Dev (2001) 15: 833-8 [PMID:11297507]

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]