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rosiglitazone (CID 77999) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(271)
 
 
Inactive(290)
 
 
Inconclusive(48)
 
 
Unspecified(749)
 
 
Top Targets:
NR LBD PPAR(313)
 
 
 
 
 
p450(20)
 
 
 
 
 
7TM GPCR Srx(17)
 
 
7TM GPCR Srsx(17)
 
 
 
NR LBD ER(9)
 
 
 
BioAssay Types:
Literature(1019)
 
 
 
 
 
Confirmatory(149)
 
 
 
 
Summary(24)
 
 
 
 
Screening(18)
 
 
 
BioActivity Types:
IC50(183)
 
 
 
 
EC50(168)
 
 
 
 
 
Potency(164)
 
 
 
 
Ki(17)
 
 
 
 
Kd(6)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1291    Data Row: 1358   Total Pages: 28   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 0.0027Activation of wild type PPAR-gamma-mediated transcriptional activity assessed as luciferase reporter activity [AID357422, Type: Literature]
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3
[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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4
[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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5
[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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6
[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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7
[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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8
[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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9
[SID123083185]
Ki 0.008Displacement of [3H]Rosiglitazone from human PPARgamma [AID314545, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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10
[SID123083185]
EC50 0.01Transcriptional activation by human PPAR gamma [AID156933, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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11
[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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12
[SID123083185]
EC50 0.011Agonist activity at PPARgamma assessed as transcriptional activation [AID476882, Type: Literature]
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13
[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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14
[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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15
[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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16
[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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17
[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]
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18
[SID144204987]
Potency-Replicate_1 0.0151qHTS assay to identify small molecule agonists of the peroxisome proliferator-activated receptor gamma (PPARg) signaling pathway [AID743094, Type: confirmatory]peroxisome proliferator activated receptor gamma [Homo sapiens] [gi:216409692]
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19
[SID123083185]
EC50 0.02Agonist activity at human PPARgamma in U2OS cells by transactivation assay [AID396054, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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20
[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]
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21
[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]
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22
[SID123083185]
EC50 0.02Maximal intrinsic response against peroxisome proliferator activated receptor gamma transactivation [AID246567, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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23
[SID123083185]
EC50 0.02Effective concentration against human Peroxisome proliferator activated receptor gamma in Gal4 transactivation assay [AID240253, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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24
[SID123083185]
EC50 0.02Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay [AID712383, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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25
[SID123083185]
EC50 0.02In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells [AID157293, Type: Literature]
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26
[SID123083185]
EC50 0.02In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells [AID156941, Type: Literature]
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27
[SID123083185]
EC50 0.02In vitro potency of PPAR gene activation against human PPAR gamma receptor using chimeric Gal4-hPPAR transactivation assay (TA) [AID156939, Type: Literature]
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28
[SID123083185]
EC50 0.021Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR gamma receptor [AID156799, Type: Literature]
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29
[SID123083185]
EC50 0.022Effective agonist concentration for human PPAR gamma Gal4 construct in transactivation assay [AID254642, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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30
[SID123083185]
EC50 0.023In vitro maximal activation of human Peroxisome proliferator activated receptor gamma in COS-1 cell transactivation assay [AID246650, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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31
[SID123083185]
EC50 0.03Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs [AID299412, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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32
[SID123083185]
EC50 0.03Agonist activity at human recombinant PPARgamma1 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay [AID465712, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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33
[SID123083185]
EC50 0.03Partial agonist activity at human PPARgamma LBD assessed as activation of PBP by HTRF assay [AID643841, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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34
[SID123083185]
EC50 0.03Effect on PPARgamma transactivation activity in U2OS cells [AID260992, Type: Literature]
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35
[SID123083185]
EC50 0.033Agonist activity at human PPARgamma expressed in african green monkey CV-1 co-transfected with GAL4 by by dual-glo luciferase reporter gene assay [AID387492, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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36
[SID123083185]
EC50 0.033Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay [AID391553, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
37
[SID123083185]
EC50 0.035Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay [AID475399, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
38
[SID123083185]
EC50 0.035Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay [AID306521, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
39
[SID123083185]
EC50 0.039Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay [AID440654, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
40
[SID123083185]
EC50 0.039Effective concentration against human PPARgamma expressed in HepG2 cells [AID240268, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
41
[SID123083185]
EC50 0.039Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay [AID722392, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
42
[SID123083185]
EC50 0.039Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay [AID344821, Type: Literature]Peroxisome proliferator-activated receptor alpha [gi:3041727]
View
43
[SID123083185]
EC50 0.04Effective concentration against human peroxisome proliferator activated receptor gamma in Gal4 transactivation assay [AID240313, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
44
[SID123083185]
EC50 0.04Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay [AID413007, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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45
[SID123083185]
EC50 0.043Agonist activity for Human PPAR gamma receptor in transcriptional activation assay [AID91246, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
46
[SID123083185]
EC50 0.043Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay [AID614594, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
View
47
[SID123083185]
EC50 0.043Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay [AID554248, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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48
[SID123083185]
IC50 0.043Inhibition of PPARgamma [AID316707, Type: Literature]
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49
[SID123083185]
EC50 0.043Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay. [AID156931, Type: Literature]
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50
[SID123083185]
EC50 0.045Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assay [AID316709, Type: Literature]
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