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Estriol (CID 5756) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(23)
 
 
Inactive(877)
 
 
Inconclusive(33)
 
 
Unspecified(180)
 
 
Top Targets:
7TM GPCR Srx(40)
 
 
 
7TM GPCR Srsx(37)
 
 
 
NR LBD ER(22)
 
 
 
 
 
NR LBD PPAR(22)
 
 
 
p450(18)
 
 
 
 
BioAssay Types:
Screening(505)
 
 
 
 
Confirmatory(326)
 
 
 
 
 
Literature(61)
 
 
 
 
 
Summary(48)
 
 
 
 
BioActivity Types:
Potency(310)
 
 
 
 
 
IC50(156)
 
 
 
 
 
EC50(7)
 
 
Kd(2)
 
 
 
Ki(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 957    Data Row: 1113   Total Pages: 23   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID144205873]
Potency-Replicate_1 0.0007qHTS assay to identify small molecule agonists of the estrogen receptor alpha (ER-alpha) signaling pathway using the BG1 cell line [AID743079, Type: confirmatory]estrogen nuclear receptor alpha [Homo sapiens] [gi:348019627]
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2
[SID144211921]
Potency-Replicate_1 0.0015qHTS assay to identify small molecule agonists of the estrogen receptor alpha (ER-alpha) signaling pathway [AID743075, Type: confirmatory]estrogen nuclear receptor alpha [Homo sapiens] [gi:348019627]
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3
[SID103469357]
IC50 0.00169DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) [AID625258, Type: other]Estrogen receptor [gi:544257]
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4
[SID144211921]
Ratio Potency (uM) 0.00206539qHTS assay to identify small molecule agonists of the estrogen receptor alpha (ER-alpha) signaling pathway: Summary [AID743077, Type: summary]estrogen nuclear receptor alpha [Homo sapiens] [gi:348019627]
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5
[SID144205873]
Potency-Replicate_1 0.0024qHTS assay to identify small molecule agonists of the estrogen receptor alpha (ER-alpha) signaling pathway [AID743075, Type: confirmatory]estrogen nuclear receptor alpha [Homo sapiens] [gi:348019627]
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6
[SID144205873]
Ratio Potency (uM) 0.00408854qHTS assay to identify small molecule agonists of the estrogen receptor alpha (ER-alpha) signaling pathway: Summary [AID743077, Type: summary]estrogen nuclear receptor alpha [Homo sapiens] [gi:348019627]
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7
[SID103469357]
Kd 0.23442Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin [AID318680, Type: Literature]Sex hormone-binding globulin [gi:134907]
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8
[SID144211921]
Potency-Replicate_1 6.9167qHTS assay to identify small molecule antagonists of the androgen receptor (AR) signaling pathway [AID743035, Type: confirmatory]AR protein [Homo sapiens] [gi:124375976]
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9
[SID103469357]
IC50 8.635DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) [AID625146, Type: other]Arachidonate 15-lipoxygenase [gi:126397]
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10
[SID103469357]
IC50 10.336DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) [AID625222, Type: other]Sodium-dependent serotonin transporter [gi:400630]
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11
[SID144211921]
Ratio Potency (uM) 13.8006qHTS assay to identify small molecule antagonists of the androgen receptor (AR) signaling pathway: Summary [AID743063, Type: summary]AR protein [Homo sapiens] [gi:124375976]
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12
[SID144205873]
Potency-Replicate_1 18.9959qHTS assay to identify small molecule antagonists of the androgen receptor (AR) signaling pathway [AID743035, Type: confirmatory]AR protein [Homo sapiens] [gi:124375976]
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13
[SID144205873]
Ratio Potency (uM) 20.1215qHTS assay to identify small molecule antagonists of the androgen receptor (AR) signaling pathway: Summary [AID743063, Type: summary]AR protein [Homo sapiens] [gi:124375976]
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14
[SID144211921]
Potency-Replicate_1 38.8952qHTS assay to identify small molecule antagonists of the glucocorticoid receptor (GR) signaling pathway [AID720692, Type: confirmatory]glucocorticoid receptor [Homo sapiens] [gi:311348376]
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15
[SID103469357]
IC50 39.345DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) [AID625263, Type: other]Glucocorticoid receptor [gi:121069]
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16
[SID144211921]
AR Potency (uM) 54.4827qHTS assay to identify small molecule antagonists of the androgen receptor (AR) signaling pathway using the MDA cell line: Summary [AID743054, Type: summary]AR protein [Homo sapiens] [gi:124375976]
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17
[SID144211921]
TR Potency (uM) 61.1306qHTS assay to identify small molecule antagonists of the thyroid receptor (TR) signaling pathway: Summary [AID743067, Type: summary]thyroid hormone receptor beta isoform 2 [Rattus norvegicus] [gi:399498506]
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18
[SID144211921]
Potency-Replicate_1 61.1306qHTS assay for identifying genotoxic compounds that show differential cytotoxicity against isogenic chicken DT40 cell lines with known DNA damage response pathways - Rad54/Ku70 mutant cell line [AID743015, Type: confirmatory]
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19
[SID48421872]
DSSTox (NCTRER) National Center for Toxicological Research Estrogen Receptor Binding Database [AID1204, Type: screening]
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20
[SID144211921]
Potency-Replicate_1 qHTS assay to identify small molecule agonists of the estrogen receptor alpha (ER-alpha) signaling pathway using the BG1 cell line [AID743079, Type: confirmatory]estrogen nuclear receptor alpha [Homo sapiens] [gi:348019627]
View
21
[SID144205873]
qHTS assay to identify small molecule antagonists of the glucocorticoid receptor (GR) signaling pathway: Summary [AID720725, Type: summary]glucocorticoid receptor [Homo sapiens] [gi:311348376]
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22
[SID144211921]
qHTS assay to identify small molecule antagonists of the glucocorticoid receptor (GR) signaling pathway: Summary [AID720725, Type: summary]glucocorticoid receptor [Homo sapiens] [gi:311348376]
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23
[SID11532998]
Inhibitors of Cav3 T-type Calcium Channels: Primary Screen [AID449739, Type: screening]voltage-dependent T-type calcium channel subunit alpha-1H isoform a [Homo sapiens] [gi:53832009]
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24
[SID103469357]
Ki 9.8TP_TRANSPORTER: inhibition of E217betaG uptake in Oatp1-expressing HeLa cells [AID681147, Type: other]Solute carrier organic anion transporter family member 1A1 [gi:1171883]
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25
[SID103469357]
Kd 100Binding affinity to Mycobacterium tuberculosis His4-tagged recombinant CYP51 substrate binding site expressed in Escherichia coli HMS174(DE3) by UV-visible spectral titration method [AID351876, Type: Literature]Lanosterol 14-alpha demethylase [gi:61221548]
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26
[SID103469357]
IC50 436.516Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) [AID255211, Type: Literature]
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27
[SID103469357]
Permeability coefficient in human skin [AID311367, Type: Literature]
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28
[SID103469357]
IC50 DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) [AID625270, Type: other]Histamine H2 receptor [gi:123120]
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29
[SID103469357]
IC50 DRUGMATRIX: HMG-CoA Reductase enzyme inhibition (substrate: [14C]HMG-CoA) [AID625271, Type: other]3-hydroxy-3-methylglutaryl-coenzyme A reductase [gi:123343]
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30
[SID103469357]
IC50 DRUGMATRIX: Insulin radioligand binding (ligand: [125I] Insulin) [AID625273, Type: other]Insulin receptor [gi:124531]
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31
[SID103469357]
IC50 DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr)) [AID625185, Type: other]Tyrosine-protein kinase Fyn [gi:125370]
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32
[SID103469357]
IC50 DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr)) [AID625187, Type: other]Tyrosine-protein kinase Lck [gi:125474]
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33
[SID103469357]
IC50 DRUGMATRIX: CYP450, 2E1 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625250, Type: other]Cytochrome P450 2E1 [gi:117250]
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34
[SID103469357]
IC50 DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) [AID625253, Type: other]D(2) dopamine receptor [gi:118206]
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35
[SID103469357]
IC50 DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) [AID625252, Type: other]D(1A) dopamine receptor [gi:118228]
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36
[SID103469357]
DRUGMATRIX: Peptidase, ELA2 (Neutrophil Elastase 2) enzyme inhibition (substrate: N-MeOSuc-Ala-Ala-Pro-Val-pNA) [AID625176, Type: other]Neutrophil elastase [gi:119292]
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37
[SID103469357]
IC50 DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr)) [AID625186, Type: other]Receptor tyrosine-protein kinase erbB-2 [gi:119533]
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38
[SID103469357]
IC50 DRUGMATRIX: Protein Serine/Threonine Kinase, ERK2 enzyme inhibition (substrate: Myelin Basic Protein) [AID625181, Type: other]Mitogen-activated protein kinase 1 [gi:119554]
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39
[SID103469357]
Oral estrogenic activity in uterotropic assay in rats at 1000-40000 ng dose [AID197231, Type: Literature]Estrogen receptor [gi:119600]
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40
[SID103469357]
IC50 DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1) [AID625257, Type: other]Endothelin-1 receptor [gi:119606]
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41
[SID103469357]
Metabolic stability in human liver microsomes assessed as medium signal/noise ratio (S/N of 10 to 100) by measuring GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis [AID678719, Type: Literature]
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42
[SID103469357]
Binding affinity towards testosterone binding globulin is expressed as log(1/k). [AID212919, Type: Literature]
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43
[SID103469357]
Binding affinity against transport protein testosterone binding globulin. [AID212920, Type: Literature]
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44
[SID103469357]
Binding affinity towards human testosterone binding globulin. [AID212931, Type: Literature]
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45
[SID103469357]
Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system [AID237685, Type: Literature]
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46
[SID103469357]
IC50 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) [AID625191, Type: other]5-hydroxytryptamine receptor 1B [gi:112815]
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47
[SID103469357]
IC50 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) [AID625218, Type: other]5-hydroxytryptamine receptor 2C [gi:112816]
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48
[SID103469357]
IC50 DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine) [AID625193, Type: other]Acetylcholinesterase [gi:113037]
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49
[SID103469357]
IC50 DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625151, Type: other]Muscarinic acetylcholine receptor M1 [gi:113118]
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50
[SID103469357]
IC50 DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625152, Type: other]Muscarinic acetylcholine receptor M2 [gi:113122]
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