Ketoconazole (CID 456201) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(390)
 
 
Inactive(1078)
 
 
Inconclusive(151)
 
 
Unspecified(2863)
 
 
Top Targets:
p450(144)
 
 
 
 
 
7TM GPCR Srx(45)
 
 
 
 
 
7TM GPCR Srsx(23)
 
 
 
 
Bcl-2 like(19)
 
 
NR LBD PPAR(17)
 
 
 
BioAssay Types:
Literature(1730)
 
 
 
 
 
Confirmatory(590)
 
 
 
 
 
Screening(558)
 
 
 
 
Summary(1)
 
 
BioActivity Types:
Potency(481)
 
 
 
 
 
IC50(381)
 
 
 
 
 
EC50(17)
 
 
 
Ki(14)
 
 
 
Kd(12)
 
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 4093    Data Row: 4482   Total Pages: 90   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103169669]
Kd 0.000221Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M [AID100102, Type: Literature]Gonadotropin-releasing hormone receptor [gi:462202]
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2
[SID103169669]
EC50 0.0003Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes expressing beta-galactosidase in mouse 3T3 fibroblast after 7 days by alamar blue assay [AID394826, Type: Literature]
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3
[SID103169669]
Kd 0.000375Dissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 M [AID102949, Type: Literature]Gonadotropin-releasing hormone receptor [gi:462202]
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4
[SID103169669]
IC50 0.00071Displacement of [131I]IMTO from CYP450c 11 in Wistar rat adrenal membrane [AID327555, Type: Literature]
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5
[SID103169669]
IC50 0.004Inhibition of human CYP3A4 [AID449589, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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6
[SID103169669]
IC50 0.004Inhibition of human CYP3A4 [AID449589, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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7
[SID103169669]
IC50 0.004Inhibition of human CYP3A4 [AID449589, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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8
[SID103169669]
IC50 0.0078Inhibition of CYP3A4 after 30 mins by fluorometric assay [AID568746, Type: Literature]
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9
[SID103169669]
IC50 0.01Antifungal activity against Candida albicans ATCC 32354 after 48 hrs by CLSI method [AID531183, Type: Literature]
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10
[SID103169669]
IC50 0.01Antifungal activity against Candida albicans ATCC 14053 after 48 hrs by CLSI method [AID531205, Type: Literature]
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11
[SID103169669]
IC50 0.01Antifungal activity against Candida albicans ATCC 60193 after 48 hrs by CLSI method [AID531206, Type: Literature]
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12
[SID103169669]
IC50 0.01Antifungal activity against Trichophyton rubrum ATCC MYA-4438 by CLSI method [AID530947, Type: Literature]
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13
[SID103169669]
IC50 0.01Antifungal activity against Fluconazole resistant Candida albicans clinical isolate 1 after 48 hrs by CLSI method [AID530970, Type: Literature]
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14
[SID103169669]
IC50 0.01Antifungal activity against Candida albicans ATCC 200955 after 48 hrs by CLSI method [AID530981, Type: Literature]
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15
[SID103169669]
IC50 0.01Antifungal activity against Candida albicans ATCC 90028 after 48 hrs by CLSI method [AID530988, Type: Literature]
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16
[SID103169669]
IC50 0.011Inhibition of human recombinant CYP3A4 [AID480595, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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17
[SID103169669]
IC50 0.011Inhibition of human recombinant CYP3A4 [AID480595, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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18
[SID103169669]
IC50 0.011Inhibition of human recombinant CYP3A4 [AID480595, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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19
[SID103169669]
IC50 0.013Inhibition of recombinant human Cytochrome P450 3A4 with BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 15 minutes [AID54780, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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20
[SID103169669]
IC50 0.013Inhibition of recombinant human Cytochrome P450 3A4 with BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 15 minutes [AID54780, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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21
[SID103169669]
IC50 0.013Inhibition of recombinant human Cytochrome P450 3A4 with BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 15 minutes [AID54780, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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22
[SID103169669]
IC50 0.016Inhibition of recombinant human Cytochrome P450 3A4 with BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 5 minutes [AID54783, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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23
[SID103169669]
IC50 0.016Inhibition of recombinant human Cytochrome P450 3A4 with BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 5 minutes [AID54783, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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24
[SID103169669]
IC50 0.016Inhibition of recombinant human Cytochrome P450 3A4 with BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 5 minutes [AID54783, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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25
[SID103169669]
IC50 0.016DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) [AID625251, Type: other]Cytochrome P450 3A4 [gi:116241312]
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26
[SID103169669]
IC50 0.016DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) [AID625251, Type: other]Cytochrome P450 3A4 [gi:116241312]
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27
[SID103169669]
IC50 0.016DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) [AID625251, Type: other]Cytochrome P450 3A4 [gi:116241312]
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28
[SID103169669]
IC50 0.017Inhibition of recombinant human Cytochrome P450 3A4 using BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 30 minutes [AID54781, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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29
[SID103169669]
IC50 0.017Inhibition of recombinant human Cytochrome P450 3A4 using BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 30 minutes [AID54781, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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30
[SID103169669]
IC50 0.017Inhibition of recombinant human Cytochrome P450 3A4 using BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 30 minutes [AID54781, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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31
[SID103169669]
IC50 0.02Inhibition of CYP3A4 in human liver microsome [AID340017, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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32
[SID103169669]
IC50 0.02Inhibition of CYP3A4 in human liver microsome [AID340017, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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33
[SID103169669]
IC50 0.02Inhibition of CYP3A4 in human liver microsome [AID340017, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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34
[SID103169669]
IC50 0.02Antifungal activity against Cryptococcus neoformans ATCC 66031 after 72 hrs by CLSI method [AID530958, Type: Literature]
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35
[SID103169669]
IC50 0.02Antifungal activity against Trichophyton rubrum ATCC 10218 by CLSI method [AID530941, Type: Literature]
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36
[SID103169669]
IC50 0.022Inhibition of recombinant human Cytochrome P450 3A4 with BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 45 minutes [AID54782, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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37
[SID103169669]
IC50 0.022Inhibition of recombinant human Cytochrome P450 3A4 with BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 45 minutes [AID54782, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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38
[SID103169669]
IC50 0.022Inhibition of recombinant human Cytochrome P450 3A4 with BFC [7-benzyloxy-4-trifluoromethylcoumarin] after 45 minutes [AID54782, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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39
[SID103169669]
Ki 0.024Inhibition of human CYP3A4 assessed as biotransformation of 7-benzyloxyquinoline [AID420064, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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40
[SID103169669]
Ki 0.024Inhibition of human CYP3A4 assessed as biotransformation of 7-benzyloxyquinoline [AID420064, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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41
[SID103169669]
Ki 0.024Inhibition of human CYP3A4 assessed as biotransformation of 7-benzyloxyquinoline [AID420064, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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42
[SID103169669]
Ki 0.0245Inhibition of lanosterol 14-alpha-demethylase in hamster hepatic microsomes [AID221159, Type: Literature]
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43
[SID103169669]
IC50 0.026Ability to inhibit the C17,20-lyase enzyme by 50% using 17-alpha-hydroxyprogesterone as substrate. [AID53248, Type: Literature]
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44
[SID103169669]
IC50 0.026Tested for inhibition of human testicular C17,20-Lyase. [AID53373, Type: Literature]
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45
[SID103169669]
IC50 0.026Inhibition of C17,20-lyase enzyme, cytochrome P450 17A1 in Human testicular microsomes [AID53376, Type: Literature]Steroid 17-alpha-hydroxylase/17,20 lyase [gi:117283]
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46
[SID103169669]
Ki 0.03Inhibition of human recombinant CYP3A4 assessed as biotransformation of 7-hydroxyquinoline to 7-benzyloxyquinoline measured every minute for 15 mins by fluorescence intensity assay [AID473745, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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47
[SID103169669]
Ki 0.03Inhibition of human recombinant CYP3A4 assessed as biotransformation of 7-hydroxyquinoline to 7-benzyloxyquinoline measured every minute for 15 mins by fluorescence intensity assay [AID473745, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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48
[SID103169669]
Ki 0.03Inhibition of human recombinant CYP3A4 assessed as biotransformation of 7-hydroxyquinoline to 7-benzyloxyquinoline measured every minute for 15 mins by fluorescence intensity assay [AID473745, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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49
[SID103169669]
Ki 0.03Inhibition of human recombinant CYP3A4 assessed as biotransformation of 7-benzyloxyquinoline to 7-hydroxyquinoline measured every 15 mins by fluorescence intensity analysis [AID437542, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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50
[SID103169669]
Ki 0.03Inhibition of human recombinant CYP3A4 assessed as biotransformation of 7-benzyloxyquinoline to 7-hydroxyquinoline measured every 15 mins by fluorescence intensity analysis [AID437542, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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