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Testosterone (CID 6013) - Compound BioActivity Data
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BioActivity Outcomes:
Active(66)
 
 
Inactive(922)
 
 
Inconclusive(59)
 
 
Unspecified(392)
 
 
Top Targets:
p450(44)
 
 
 
 
7TM GPCR Srx(43)
 
 
 
7TM GPCR Srsx(38)
 
 
 
NR LBD AR(34)
 
 
 
 
 
NR LBD ER(23)
 
 
 
 
 
BioAssay Types:
Screening(473)
 
 
 
Confirmatory(408)
 
 
 
 
 
Literature(357)
 
 
 
 
 
Summary(24)
 
 
 
 
BioActivity Types:
Potency(375)
 
 
 
 
 
IC50(147)
 
 
 
 
Ki(10)
 
 
 
EC50(3)
 
 
Kd(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1028    Data Row: 1439   Total Pages: 29   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID104234228]
Kd 0.000631Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin [AID318680, Type: Literature]Sex hormone-binding globulin [gi:134907]
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2
[SID104234228]
Ki 0.0014Inhibitory constant against rat prostate cytosol androgen receptor using [3H]mibolerone [AID39296, Type: Literature]Androgen receptor [gi:113832]
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3
[SID144207887]
Ratio Potency (uM) 0.0014244qHTS assay to identify small molecule agonists of the androgen receptor (AR) signaling pathway: Summary [AID743053, Type: summary]AR protein [Homo sapiens] [gi:124375976]
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4
[SID17389513]
Potency 0.0016qHTS assay for small molecule agonists of androgen receptor signaling [AID588515, Type: confirmatory]AR protein [Homo sapiens] [gi:124375976]
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5
[SID144207887]
Potency-Replicate_1 0.0017qHTS assay to identify small molecule agonists of the androgen receptor (AR) signaling pathway using the MDA cell line [AID743040, Type: confirmatory]AR protein [Homo sapiens] [gi:124375976]
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6
[SID104234228]
EC50 0.002Agonist activity at androgen receptor in mouse NIH3T3 cells transiently transfected with beta-galactosidase reporter gene assessed as cellular transformation by R-SAT assay [AID445833, Type: Literature]Androgen receptor [gi:113831]
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7
[SID104234228]
IC50 0.0027Binding affinity to androgen receptor [AID307522, Type: Literature]
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8
[SID104234228]
IC50 0.0027Inhibitory activity against AR [AID260157, Type: Literature]Androgen receptor [gi:113830]
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9
[SID104234228]
IC50 0.0027Binding affinity at AR [AID310114, Type: Literature]
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10
[SID104234228]
EC50 0.00316Agonist activity at androgen receptor in human MDA-KB2 cells transfected with MMTV linked luciferase assessed as transcriptional activation by luciferase reporter gene assay [AID445841, Type: Literature]Androgen receptor [gi:113830]
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11
[SID104234228]
IC50 0.0032In vitro antagonist activity against rat prostatic androgen receptor (AR) [AID39178, Type: Literature]
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12
[SID104234228]
IC50 0.0039Inhibition of human androgen receptor expressed in Escherichia coli [AID242138, Type: Literature]Androgen receptor [gi:113830]
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13
[SID104234228]
IC50 0.00457Displacement of [3H]R1881 from wild type human androgen receptor expressed in COS-1 cells co-transfected with pSG5 after 15 mins by scintillation assay [AID694143, Type: Literature]Androgen receptor [gi:113830]
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14
[SID104234228]
Ki 0.0049Inhibition of rat prostate cytosolic androgen receptor [AID238931, Type: Literature]
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15
[SID104234228]
Ki 0.0049Binding affinity against rat prostate cytosolic Androgen receptor using [3H]mibolerone as radioligand [AID39293, Type: Literature]
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16
[SID104234228]
IC50 0.00617DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) [AID625228, Type: other]Androgen receptor [gi:113832]
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17
[SID144207887]
Potency-Replicate_1 0.0069qHTS assay to identify small molecule agonists of the androgen receptor (AR) signaling pathway [AID743036, Type: confirmatory]AR protein [Homo sapiens] [gi:124375976]
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18
[SID104234228]
IC50 0.014Displacement of [3H]DHT from human SHBG [AID274506, Type: Literature]Sex hormone-binding globulin [gi:134907]
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19
[SID144207887]
Potency-Replicate_1 0.0215qHTS 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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20
[SID104234228]
Ki 0.029Displacement of fluorescent-tagged R1881 from androgen receptor after 4 hrs by fluorometric assay [AID569786, Type: other]
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21
[SID104234228]
IC50 0.03Binding affinity to androgen receptor by fluorescence binding assay [AID539789, Type: Literature]
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22
[SID104234228]
Km 0.13Competitive inhibition constant (Km) for human placental Cytochrome P450 19A1 [AID53900, Type: Literature]Aromatase [gi:117293]
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23
[SID104234228]
Km 0.21Km for Cytochrome P450 19A1 [AID53901, Type: Literature]
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24
[SID104234228]
Ki 0.6Inhibition of human placental aromatase Cytochrome P450 19A1 [AID53880, Type: Literature]Aromatase [gi:117293]
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25
[SID104234228]
Ki 1.2Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand [AID239347, Type: Literature]
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26
[SID104234228]
IC50 1.9In vitro inhibitory activity against rat prostatic steroid 5-alpha-reductase [AID207301, Type: Literature]
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27
[SID104234228]
IC50 1.935DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) [AID625172, Type: other]Progesterone receptor [gi:75071465]
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28
[SID104234228]
IC50 3.0903Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) [AID255211, Type: Literature]
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29
[SID104234228]
IC50 3.206DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) [AID625263, Type: other]Glucocorticoid receptor [gi:121069]
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30
[SID144207887]
Potency-Replicate_1 6.8701qHTS 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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31
[SID17389513]
Potency 7.0795qHTS assay for small molecule antagonists of glucocorticoid receptor signaling [AID588533, Type: confirmatory]glucocorticoid receptor [Homo sapiens] [gi:311348376]
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32
[SID104234228]
Ki 7.76Affinity for ERG2 of Sacchromyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand [AID239296, Type: Literature]
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33
[SID17389513]
Potency 8.0875S16 Schwann cell PMP22 intronic element firefly luciferase assay [AID624032, Type: confirmatory]peripheral myelin protein 22 [Rattus norvegicus] [gi:8393992]
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34
[SID104234228]
IC50 10Binding affinity for Cytochrome P450 3A4; Range = 1-10 uM [AID54753, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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35
[SID144207887]
Ratio Potency (uM) 10.4746qHTS 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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36
[SID17389513]
Potency 12.5893qHTS assay for small molecule agonists of estrogen receptor alpha signaling [AID588514, Type: confirmatory]estrogen nuclear receptor alpha [Homo sapiens] [gi:348019627]
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37
[SID17389513]
Potency 12.5893qHTS assay for small molecule agonists of retinoid X receptor alpha signaling [AID588544, Type: confirmatory]retinoid X nuclear receptor alpha [Homo sapiens] [gi:325495497]
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38
[SID104234228]
EC50 18.3Agonist activity at human TGR5 expressed in CHO cells by luciferase assay [AID324923, Type: Literature]G-protein coupled bile acid receptor 1 [gi:74762624]
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39
[SID104234228]
Km 20.5Activity of human recombinant CYP3A4 co-expressed in Escherichia coli with human p450 NADPH reductase assessed as conversion of deoxypodophyllotoxin to epipodophyllotoxin [AID363824, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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40
[SID144207887]
Ratio Potency (uM) 21.5356qHTS assay for small molecule agonists of the antioxidant response element (ARE) signaling pathway: Summary [AID743219, Type: summary]nuclear factor erythroid 2-related factor 2 isoform 1 [Homo sapiens] [gi:20149576]
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41
[SID17389513]
Potency 26.6032qHTS assay for small molecule antagonists of the retinoid-related orphan receptor gamma (ROR-gamma) signaling pathway [AID651802, Type: confirmatory]Nuclear receptor ROR-gamma [gi:49066040]
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42
[SID104234228]
IC50 30Inhibitory concentration against mammalian m-constitutive androstane receptor (mCAR) activity [AID50905, Type: Literature]
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43
[SID144207887]
Potency-Replicate_1 30.4199qHTS assay to identify small molecule antagonists of the thyroid receptor (TR) signaling pathway [AID743065, Type: confirmatory]thyroid hormone receptor beta isoform 2 [Rattus norvegicus] [gi:399498506]
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44
[SID144207887]
Potency-Replicate_1 30.4199qHTS assay for identifying genotoxic compounds that show differential cytotoxicity against isogenic chicken DT40 cell lines with known DNA damage response pathways - Rev3 mutant cell line [AID743014, Type: confirmatory]
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45
[SID144207887]
TR Potency (uM) 38.2964qHTS 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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46
[SID144207887]
Potency-Replicate_1 54.0951qHTS 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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47
[SID144207887]
Potency-Replicate_1 54.0951qHTS assay for identifying genotoxic compounds that show differential cytotoxicity against isogenic chicken DT40 cell lines with known DNA damage response pathways - wild type cell line [AID743012, Type: confirmatory]
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48
[SID104234228]
Effective dose required to inhibit testosterone propionate-stimulated prostate weight gain by 50% using [3H]- R1881 as the radioligand; Androgenic [AID39175, Type: Literature]
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49
[SID17389513]
Cell Viability - NIH 3T3 [AID541, Type: confirmatory]
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50
[SID56462804]
Wnt/Beta-catenin HTS Measured in Cell-Based System Using Plate Reader - 2161-01_Activator_SinglePoint_HTS_Activity [AID743398, Type: screening]
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