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rosiglitazone (CID 77999) - Compound BioActivity Data
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BioActivity Outcomes:
Active(279)
 
 
Inactive(296)
 
 
Inconclusive(43)
 
 
Unspecified(1129)
 
 
Top Targets:
NR LBD PPAR(321)
 
 
 
 
 
7tm 4(34)
 
 
 
 
p450(20)
 
 
 
 
 
NR LBD ER(9)
 
 
 
NR LBD AR(8)
 
 
 
 
BioAssay Types:
Literature(1079)
 
 
 
 
 
Confirmatory(272)
 
 
 
 
 
Summary(24)
 
 
 
 
Screening(18)
 
 
 
BioActivity Types:
IC50(188)
 
 
 
 
EC50(172)
 
 
 
 
 
Potency(165)
 
 
 
 
Ki(18)
 
 
 
 
Kd(6)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1680    Data Row: 1747   Total Pages: 88   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID123083185]
Ki 0.00023Displacement of [125I]-SI-Ang-2 from AT1 receptor in Rattus norvegicus Sprague-Dawley (rat) liver membranes after 2 hr [AID1094657, Type: confirmatory]Type-1A angiotensin II receptor [gi:113493]
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2
[SID123083185]
EC50 0.002Agonist activity at GAL4-fused PPARgamma M463A mutant (unknown origin) expressed in human HepG2 cells by transactivation assay [AID744326, Type: Literature]
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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]
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4
[SID123083185]
EC50 0.0027Activation of wild type PPAR-gamma-mediated transcriptional activity assessed as luciferase reporter activity [AID357422, Type: Literature]
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5
[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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6
[SID123083185]
EC50 0.004Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase reporter gene assay [AID731518, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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7
[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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8
[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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9
[SID123083185]
Kd 0.007Binding affinity to human PPARgamma (unknown origin) by competitive TR-FRET assay [AID731519, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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10
[SID123083185]
Ki 0.008Displacement of [3H]Rosiglitazone from human PPARgamma [AID314545, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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11
[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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12
[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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13
[SID123083185]
EC50 0.01Transcriptional activation by human PPAR gamma [AID156933, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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14
[SID123083185]
EC50 0.01Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay [AID744324, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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15
[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]
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16
[SID123083185]
EC50 0.011Agonist activity at PPARgamma assessed as transcriptional activation [AID476882, Type: Literature]
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17
[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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18
[SID123083185]
IC50 0.011Binding affinity to human PPARgamma receptor by radioligand displacement assay [AID751861, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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19
[SID123083185]
IC50 0.012Binding affinity to human PPARgamma receptor by radioligand displacement assay [AID752224, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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20
[SID144204987]
Ratio Potency (uM) 0.0145209qHTS assay to identify small molecule agonists of the peroxisome proliferator-activated receptor gamma (PPARg) signaling pathway: Summary [AID743140, Type: summary]peroxisome proliferator activated receptor gamma [Homo sapiens] [gi:216409692]
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