GW0742 (CID 9934458) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(21)
 
 
Inactive(97)
 
 
Inconclusive(32)
 
 
Unspecified(5)
 
 
Top Targets:
NR LBD PPAR(17)
 
 
 
 
 
NR LBD TR(8)
 
 
 
NR LBD VDR(7)
 
 
 
 
Menin(4)
 
 
 
P53(4)
 
 
 
BioAssay Types:
Confirmatory(116)
 
 
 
 
Literature(20)
 
 
 
 
Screening(10)
 
 
 
BioActivity Types:
Potency(114)
 
 
 
 
EC50(10)
 
 
 
IC50(1)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 127    Data Row: 155   Total Pages: 4   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103215363]
EC50 0.001Maximum transcriptional activation of human PPAR delta receptor [AID156617, Type: Literature]Peroxisome proliferator-activated receptor delta [gi:417522]
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2
[SID103215363]
EC50 0.001Maximum transcriptional activation of human PPAR delta receptor [AID156617, Type: Literature]Peroxisome proliferator-activated receptor delta [gi:417522]
View
3
[SID103215363]
EC50 0.001Maximum transcriptional activation of human PPAR delta receptor [AID156617, Type: Literature]Peroxisome proliferator-activated receptor delta [gi:417522]
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4
[SID103215363]
IC50 0.001Binding affinity for human PPAR delta receptor [AID156625, Type: Literature]Peroxisome proliferator-activated receptor delta [gi:417522]
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5
[SID103215363]
IC50 0.001Binding affinity for human PPAR delta receptor [AID156625, Type: Literature]Peroxisome proliferator-activated receptor delta [gi:417522]
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6
[SID103215363]
IC50 0.001Binding affinity for human PPAR delta receptor [AID156625, Type: Literature]Peroxisome proliferator-activated receptor delta [gi:417522]
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7
[SID103215363]
EC50 0.0029Displacement of pan-PPAR fluormone from PPARdelta LBD by TR-FRET based LanthaScreen assay [AID675855, Type: Literature]
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8
[SID103215363]
EC50 0.03Activity against murine PPAR delta receptor [AID156784, Type: Literature]Peroxisome proliferator-activated receptor delta [gi:548577]
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9
[SID103215363]
EC50 0.3Agonist activity at human PPARdelta LBD by cell based luciferase reporter gene assay [AID569828, Type: Literature]Peroxisome proliferator-activated receptor delta [gi:417522]
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10
[SID103215363]
EC50 0.3Agonist activity at human PPARdelta LBD by cell based luciferase reporter gene assay [AID569828, Type: Literature]Peroxisome proliferator-activated receptor delta [gi:417522]
View
11
[SID103215363]
EC50 0.3Agonist activity at human PPARdelta LBD by cell based luciferase reporter gene assay [AID569828, Type: Literature]Peroxisome proliferator-activated receptor delta [gi:417522]
View
12
[SID103215363]
EC50 0.92Displacement of pan-PPAR fluormone from PPARalpha LBD by TR-FRET based LanthaScreen assay [AID675854, Type: Literature]
View
13
[SID103215363]
EC50 1.1Maximum transcriptional activation of human PPAR alpha receptor [AID156147, Type: Literature]Peroxisome proliferator-activated receptor alpha [gi:3041727]
View
14
[SID103215363]
EC50 1.1Maximum transcriptional activation of human PPAR alpha receptor [AID156147, Type: Literature]Peroxisome proliferator-activated receptor alpha [gi:3041727]
View
15
[SID26753244]
Potency 1.9953qHTS assay for small molecule agonists of the peroxisome proliferator-activated receptor alpha (PPARalpha) signaling pathway [AID651778, Type: confirmatory]Peroxisome proliferator-activated receptor alpha [gi:3041727]
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16
[SID26753244]
Potency 1.9953qHTS assay for small molecule agonists of the peroxisome proliferator-activated receptor alpha (PPARalpha) signaling pathway [AID651778, Type: confirmatory]Peroxisome proliferator-activated receptor alpha [gi:3041727]
View
17
[SID103215363]
EC50 2Maximum transcriptional activation of human PPAR gamma receptor [AID156945, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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18
[SID103215363]
EC50 2Maximum transcriptional activation of human PPAR gamma receptor [AID156945, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
19
[SID103215363]
EC50 2Maximum transcriptional activation of human PPAR gamma receptor [AID156945, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
20
[SID103215363]
EC50 2Maximum transcriptional activation of human PPAR gamma receptor [AID156945, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
21
[SID26753243]
Potency 7.9433qHTS Assay for Inhibitors and Substrates of Cytochrome P450 3A4 [AID884, Type: confirmatory]cytochrome P450, family 3, subfamily A, polypeptide 4 [Homo sapiens] [gi:13435386]
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22
[SID26753243]
Potency 7.9433qHTS Assay for Inhibitors and Substrates of Cytochrome P450 3A4 [AID884, Type: confirmatory]cytochrome P450, family 3, subfamily A, polypeptide 4 [Homo sapiens] [gi:13435386]
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23
[SID26753243]
Potency 7.9433qHTS Assay for Inhibitors and Substrates of Cytochrome P450 3A4 [AID884, Type: confirmatory]cytochrome P450, family 3, subfamily A, polypeptide 4 [Homo sapiens] [gi:13435386]
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24
[SID103215363]
EC50 8.8Activity against murine PPAR alpha receptor [AID156452, Type: Literature]Peroxisome proliferator-activated receptor alpha [gi:1709728]
View
25
[SID26753243]
Potency 10qHTS Assay for Inhibitors of HPGD (15-Hydroxyprostaglandin Dehydrogenase) [AID894, Type: confirmatory]15-hydroxyprostaglandin dehydrogenase [NAD+] isoform 1 [Homo sapiens] [gi:31542939]
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26
[SID26753243]
Potency 10qHTS Assay for Inhibitors of HPGD (15-Hydroxyprostaglandin Dehydrogenase) [AID894, Type: confirmatory]15-hydroxyprostaglandin dehydrogenase [NAD+] isoform 1 [Homo sapiens] [gi:31542939]
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27
[SID26753243]
Potency 10qHTS Assay for Inhibitors of HPGD (15-Hydroxyprostaglandin Dehydrogenase) [AID894, Type: confirmatory]15-hydroxyprostaglandin dehydrogenase [NAD+] isoform 1 [Homo sapiens] [gi:31542939]
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28
[SID29215130]
Potency 19.9526Inhibitors of the vitamin D receptor (VDR): qHTS [AID504847, Type: confirmatory]vitamin D3 receptor isoform VDRA [Homo sapiens] [gi:63054845]
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29
[SID29215130]
Potency 19.9526Inhibitors of the vitamin D receptor (VDR): qHTS [AID504847, Type: confirmatory]vitamin D3 receptor isoform VDRA [Homo sapiens] [gi:63054845]
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30
[SID29215130]
Potency 19.9526Inhibitors of the vitamin D receptor (VDR): qHTS [AID504847, Type: confirmatory]vitamin D3 receptor isoform VDRA [Homo sapiens] [gi:63054845]
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31
[SID29215130]
Potency 19.9526Inhibitors of the vitamin D receptor (VDR): qHTS [AID504847, Type: confirmatory]vitamin D3 receptor isoform VDRA [Homo sapiens] [gi:63054845]
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32
[SID29215130]
Potency 25.1189qHTS for Inhibitors of the vitamin D receptor (VDR): Hit Validation using a Fluorescein Assay [AID602200, Type: confirmatory]vitamin D3 receptor isoform VDRA [Homo sapiens] [gi:63054845]
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33
[SID29215130]
Potency 25.1189qHTS for Inhibitors of the vitamin D receptor (VDR): Hit Validation using a Fluorescein Assay [AID602200, Type: confirmatory]vitamin D3 receptor isoform VDRA [Homo sapiens] [gi:63054845]
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34
[SID29215130]
Potency 25.1189qHTS for Inhibitors of the vitamin D receptor (VDR): Hit Validation using a Fluorescein Assay [AID602200, Type: confirmatory]vitamin D3 receptor isoform VDRA [Homo sapiens] [gi:63054845]
View
35
[SID29215130]
Potency 25.1189qHTS for Inhibitors of the vitamin D receptor (VDR): Hit Validation using a Fluorescein Assay [AID602200, Type: confirmatory]vitamin D3 receptor isoform VDRA [Homo sapiens] [gi:63054845]
View
36
[SID29215130]
Potency 31.6228qHTS Assay for Inhibitors of GCN5L2 [AID504327, Type: confirmatory]histone acetyltransferase KAT2A [Homo sapiens] [gi:153791535]
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37
[SID29215130]
Potency 31.6228qHTS Assay for Inhibitors of GCN5L2 [AID504327, Type: confirmatory]histone acetyltransferase KAT2A [Homo sapiens] [gi:153791535]
View
38
[SID26753244]
Potency 68.5896qHTS assay for small molecule agonists of the antioxidant response element (ARE) signaling pathway [AID651741, Type: confirmatory]NFE2L2 gene product [Homo sapiens] [gi:20149576]
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39
[SID26753244]
Potency 68.5896qHTS assay for small molecule agonists of the antioxidant response element (ARE) signaling pathway [AID651741, Type: confirmatory]NFE2L2 gene product [Homo sapiens] [gi:20149576]
View
40
[SID26753244]
Potency 68.5896qHTS assay for small molecule agonists of the antioxidant response element (ARE) signaling pathway [AID651741, Type: confirmatory]NFE2L2 gene product [Homo sapiens] [gi:20149576]
View
41
[SID26753244]
Potency 68.5896qHTS assay for small molecule agonists of the antioxidant response element (ARE) signaling pathway [AID651741, Type: confirmatory]NFE2L2 gene product [Homo sapiens] [gi:20149576]
View
42
[SID103215363]
 Drug level in LDLR-deficient mouse serum at 60 mg/kg [AID547923, Type: Literature]
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43
[SID103215363]
 Antiatherogenic effect in HC/HF diet-fed apolipoprotein E-deficient C57BL/6J mouse assessed as increase in HDL-cholesterol at 2 mg/kg/day for 4 weeks [AID547907, Type: Literature]
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44
[SID103215363]
 Agonist activity at mouse PPAR-alpha expressed in african green monkey CV-1 cells after 24 hrs by luciferase reporter gene assay [AID547902, Type: Literature]Peroxisome proliferator-activated receptor alpha [gi:1709728]
View
45
[SID103215363]
 Agonist activity at mouse PPAR-gammaexpressed in african green monkey CV-1 cells after 24 hrs by luciferase reporter gene assay [AID547904, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432235]
View
46
[SID85787647]
 SMM c-myc Measured in Biochemical System Using Small Molecule MicroArray - 2081-01_Other_SinglePoint_HTS_Activity [AID624141, Type: screening]MYC gene product [Homo sapiens] [gi:71774083]
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47
[SID103215363]
EC50 0.0058Agonist activity at mouse PPAR-delta expressed in african green monkey CV-1 cells after 24 hrs by luciferase reporter gene assay [AID547903, Type: Literature]Peroxisome proliferator-activated receptor delta [gi:548577]
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48
[SID103215363]
EC50 10Activity against murine PPAR gamma receptor [AID157278, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432235]
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49
[SID103215363]
 Toxicity in LDLR-deficient mouse assessed as increase in liver weight at 60 mg/kg [AID547924, Type: Literature]
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50
[SID103215363]
 Octanol-water partition coefficient, log P of the compound [AID675856, Type: Literature]
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