rosiglitazone (CID 77999) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(218)
 
 
Inactive(201)
 
 
Inconclusive(27)
 
 
Unspecified(703)
 
 
Top Targets:
NR LBD PPAR(281)
 
 
 
 
 
p450(18)
 
 
 
 
 
7TM GPCR Srx(12)
 
 
7TM GPCR Srsx(10)
 
 
NAD binding 8(6)
 
 
 
BioAssay Types:
Literature(909)
 
 
 
 
 
Confirmatory(75)
 
 
 
 
Screening(18)
 
 
 
BioActivity Types:
IC50(182)
 
 
 
 
EC50(158)
 
 
 
 
 
Potency(73)
 
 
 
 
Ki(16)
 
 
 
 
Kd(2)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1087    Data Row: 1149   Total Pages: 23   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID123083185]
EC50 0.0024Agonist activity at PPARgamma LBD in human 293H DA cells after 16 hrs by TR-FRET activation reporter assay [AID675852, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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2
[SID123083185]
EC50 0.0024Agonist activity at PPARgamma LBD in human 293H DA cells after 16 hrs by TR-FRET activation reporter assay [AID675852, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
3
[SID123083185]
EC50 0.0024Agonist activity at PPARgamma LBD in human 293H DA cells after 16 hrs by TR-FRET activation reporter assay [AID675852, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
4
[SID123083185]
EC50 0.0024Agonist activity at PPARgamma LBD in human 293H DA cells after 16 hrs by TR-FRET activation reporter assay [AID675852, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
5
[SID123083185]
EC50 0.0027Activation of wild type PPAR-gamma-mediated transcriptional activity assessed as luciferase reporter activity [AID357422, Type: Literature]
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6
[SID123083185]
EC50 0.0038Activation of human PPARgamma ligand binding domain-mediated transcriptional activity in human HepG2/C3A cells co-transfected with fused Gal4-LBD by cotransfection assay [AID357425, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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7
[SID123083185]
EC50 0.0038Activation of human PPARgamma ligand binding domain-mediated transcriptional activity in human HepG2/C3A cells co-transfected with fused Gal4-LBD by cotransfection assay [AID357425, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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8
[SID123083185]
EC50 0.0038Activation of human PPARgamma ligand binding domain-mediated transcriptional activity in human HepG2/C3A cells co-transfected with fused Gal4-LBD by cotransfection assay [AID357425, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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9
[SID123083185]
EC50 0.0038Activation of human PPARgamma ligand binding domain-mediated transcriptional activity in human HepG2/C3A cells co-transfected with fused Gal4-LBD by cotransfection assay [AID357425, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
10
[SID123083185]
EC50 0.004In vitro effective concentration against human peroxisome proliferator activated receptor gamma/Gal4 in cell-based transactivation assay [AID255669, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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11
[SID123083185]
EC50 0.004In vitro effective concentration against human peroxisome proliferator activated receptor gamma/Gal4 in cell-based transactivation assay [AID255669, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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12
[SID123083185]
EC50 0.004In vitro effective concentration against human peroxisome proliferator activated receptor gamma/Gal4 in cell-based transactivation assay [AID255669, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
13
[SID123083185]
EC50 0.004In vitro effective concentration against human peroxisome proliferator activated receptor gamma/Gal4 in cell-based transactivation assay [AID255669, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
14
[SID123083185]
EC50 0.004Agonist activity at human PPARalpha at 100 uM by GAL4 transactivation assay relative to WY 14,643 [AID314548, Type: Literature]Peroxisome proliferator-activated receptor alpha [gi:3041727]
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15
[SID123083185]
EC50 0.004Agonist activity at human PPARalpha at 100 uM by GAL4 transactivation assay relative to WY 14,643 [AID314548, Type: Literature]Peroxisome proliferator-activated receptor alpha [gi:3041727]
View
16
[SID123083185]
Ki 0.008Displacement of [3H]Rosiglitazone from human PPARgamma [AID314545, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
17
[SID123083185]
Ki 0.008Displacement of [3H]Rosiglitazone from human PPARgamma [AID314545, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
18
[SID123083185]
Ki 0.008Displacement of [3H]Rosiglitazone from human PPARgamma [AID314545, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
19
[SID123083185]
Ki 0.008Displacement of [3H]Rosiglitazone from human PPARgamma [AID314545, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
20
[SID123083185]
Ki 0.008Binding affinity for human PPAR gamma construct expressed in bacteria with 3[H] rosiglitazone [AID254528, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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21
[SID123083185]
Ki 0.008Binding affinity for human PPAR gamma construct expressed in bacteria with 3[H] rosiglitazone [AID254528, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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22
[SID123083185]
Ki 0.008Binding affinity for human PPAR gamma construct expressed in bacteria with 3[H] rosiglitazone [AID254528, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
23
[SID123083185]
Ki 0.008Binding affinity for human PPAR gamma construct expressed in bacteria with 3[H] rosiglitazone [AID254528, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
24
[SID123083185]
EC50 0.01Transcriptional activation by human PPAR gamma [AID156933, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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25
[SID123083185]
EC50 0.01Transcriptional activation by human PPAR gamma [AID156933, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
26
[SID123083185]
EC50 0.01Transcriptional activation by human PPAR gamma [AID156933, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
27
[SID123083185]
EC50 0.01Transcriptional activation by human PPAR gamma [AID156933, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
28
[SID123083185]
EC50 0.01Agonist activity at PPARgamma receptor expressed in human HepG2 cells by PPRE-luciferase reporter gene assay [AID600729, Type: Literature]
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29
[SID123083185]
EC50 0.011Agonist activity at PPARgamma assessed as transcriptional activation [AID476882, Type: Literature]
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30
[SID123083185]
EC50 0.011Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay [AID666690, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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31
[SID123083185]
EC50 0.011Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay [AID666690, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
32
[SID123083185]
EC50 0.011Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay [AID666690, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
33
[SID123083185]
EC50 0.011Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay [AID666690, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
34
[SID123083185]
EC50 0.011Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay [AID642732, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
35
[SID123083185]
EC50 0.011Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay [AID642732, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
36
[SID123083185]
EC50 0.011Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay [AID642732, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
37
[SID123083185]
EC50 0.011Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay [AID642732, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
38
[SID123083185]
Kd 0.0148Agonist activity at histidine-tagged PPARgamma ligand binding domain by cell free-coactivator recruitment assay [AID357434, Type: Literature]
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39
[SID123083185]
EC50 0.015Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay [AID417012, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
40
[SID123083185]
EC50 0.015Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay [AID417012, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
41
[SID123083185]
EC50 0.015Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay [AID417012, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
42
[SID123083185]
EC50 0.015Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay [AID417012, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
43
[SID123083185]
EC50 0.02Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay [AID421049, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
44
[SID123083185]
EC50 0.02Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay [AID421049, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
45
[SID123083185]
EC50 0.02Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay [AID421049, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
46
[SID123083185]
EC50 0.02Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay [AID421049, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
47
[SID123083185]
EC50 0.02Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay [AID372044, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
48
[SID123083185]
EC50 0.02Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay [AID372044, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
49
[SID123083185]
EC50 0.02Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay [AID372044, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
50
[SID123083185]
EC50 0.02Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay [AID372044, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View