BDBM28681 5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)methyl]-1,3-thiazolidine-2,4-dione::Avandia::BRL 49653::Brl-49653::CHEMBL121::ROSIGLITAZONE MALEATE::[3H]rosiglitazone::cid_5281055::rosiglitazone

SMILES CN(CCOc1ccc(Cc2sc(=O)[nH]c2O)cc1)c1ccccn1

InChI Key InChIKey=FLDPBMANMDLQTH-UHFFFAOYSA-N

Data  21 KI  59 IC50  4 Kd  140 EC50

PDB links: 5 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 144 hits for monomerid = 28681   

TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKi:  8nMAssay Description:Binding affinity for human PPAR gamma construct expressed in bacteria with 3[H] rosiglitazoneMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKi:  8nMAssay Description:Displacement of [3H]Rosiglitazone from human PPARgammaMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKi:  10nMAssay Description:Displacement of [3H]-rosiglitazone from GST-tagged PPARgammaLBD (unknown origin) after 1 hr by scintillation proximity assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKi:  14nMAssay Description:Binding affinity towards human peroxisome proliferator activated receptor gamma (PPAR gamma) was determined by HTRF assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKi:  47nMAssay Description:In vitro binding to peroxisome proliferator activated receptor gamma (PPAR gamma) using [3H]-BRL 49653 as radioligand in scintillation proximity assa...Checked by AuthorMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKi:  49nMAssay Description:Binding affinity was determined by displacement of 20 nM [3H]- thiazolidinedione from 4 nM biotinylated human peroxisome proliferator-activated recep...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKi:  50nMAssay Description:Binding affinity for human peroxisome proliferator activated receptor gammaMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKi:  74nMAssay Description:Displacement of [3H]rosiglitazone from N-terminal His-tagged human PPARgamma ligand binding domain expressed in Escherichia coli BL21 DE3 cells by sc...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKi:  74nM ΔG°:  -9.62kcal/molepH: 7.5 T: 2°CAssay Description:The scintillation proximity assay was performed in 96-well plates containing polylysine-coated yttrium silicate beads, His-PPARgamma-LBD, and [3H]ros...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKi:  120nMAssay Description:Binding affinity to human Peroxisome proliferator activated receptor gamma using scintillation proximity assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKi:  136nMAssay Description:In vitro binding affinity towards human peroxisome proliferator activated receptor gamma (PPAR gamma)More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKi:  136nMAssay Description:Binding affinity towards peroxisome proliferator activated receptor gamma (PPAR gamma)More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKi:  440nMAssay Description:Displacement of radiolabeled darglitazone from human PPAR gamma by SPA binding assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKi:  440nMAssay Description:Displacement of radiolabeled darglitazone from human PPAR gamma by SPA assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  40nMAssay Description:The HepG2 cells were co-transfected with DNA construct containing PPAR-Gal4 chimeric receptor and Gal4-luciferase reporter. The luciferase activity w...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataKd:  14.8nM EC50:  3.80nMpH: 7.5 T: 2°CAssay Description:Kd values were obtained by incubating His-PPARgamma-LBD with biotinylated peptide, europium-labeled anti-histidine antibody, and allophycocyanin-labe...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  82nMAssay Description:The HepG2 cells were co-transfected with DNA construct containing PPAR-Gal4 chimeric receptor and Gal4-luciferase reporter. EC50 is the concentration...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataIC50:  274nM EC50:  223nMpH: 7.4 T: 2°CAssay Description:Human 6His-PPAR ligand-binding domain was added to the mixture containing radioligand and test compound, followed by yttrium silicate polylysine SPA ...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataIC50:  30nMAssay Description:Initial binding affinity against PPAR-gamma receptorMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  21nMAssay Description:In vitro binding affinity towards human peroxisome proliferator activated receptor alpha (PPAR alpha)More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  43nMAssay Description:Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by funct...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  20nMAssay Description:In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cellsMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  89nMAssay Description:Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection as...Checked by AuthorMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Mus musculus)
Glaxo Wellcome Research And Development

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  60nMAssay Description:In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cellsMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Mus musculus)
Glaxo Wellcome Research And Development

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  76nMAssay Description:Agonist activity for murine PPAR gamma receptor in transcriptional activation assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  43nMAssay Description:Agonist activity for Human PPAR gamma receptor in transcriptional activation assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  20nMAssay Description:Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  657nMAssay Description:Binding affinity at human PPAR gammaMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataIC50:  48nMAssay Description:Binding affinity at human peroxidase proliferator activated receptor gamma (hPPARgamma)More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  160nMAssay Description:In vitro transactivation using receptor transactivation assay against hPPAR gammaMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  160nMAssay Description:In vitro activation of human peroxisome proliferator activated receptor gamma (PPAR gamma)More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  20nMAssay Description:In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cellsMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataIC50:  440nMAssay Description:Receptor binding affinity of the compound to human Peroxisome proliferator activated receptor gamma against [3H]-ragalitazar radioligandMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataIC50:  210nMAssay Description:In vitro binding affinity for human PPAR gamma in SPAMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  120nMAssay Description:Agonistic activity against PPAR (peroxisome proliferator activated receptor gamma) in Suarus chinesisMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  160nMAssay Description:In vitro transactivation of human Peroxisome proliferator activated receptor gammaMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  10nMAssay Description:Transcriptional activation by human PPAR deltaMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataIC50:  200nMAssay Description:In vitro binding affinity for human PPAR gamma receptor using scintillation proximity assay (SPA)More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  20nMAssay Description:In vitro potency of PPAR gene activation against human PPAR gamma receptor using chimeric Gal4-hPPAR transactivation assay (TA)More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  2.88E+3nMAssay Description:In vitro transcription activation on human peroxisome proliferator activated receptor-gamma (PPAR gamma)More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  40nMAssay Description:Effective concentration against human peroxisome proliferator activated receptor gamma in Gal4 transactivation assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataIC50:  70nMAssay Description:Mean inhibitory concentration against human peroxisome proliferator-activated receptor gammaMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  268nMAssay Description:Mean effective concentration against human peroxisome proliferator-activated receptor gammaMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  20nMAssay Description:Effective concentration against human Peroxisome proliferator activated receptor gamma in Gal4 transactivation assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataIC50:  250nMAssay Description:Inhibition of human Peroxisome proliferator activated receptor gamma bindingMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  140nMAssay Description:Effective concentration against human Peroxisome proliferator activated receptor gammaMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataIC50:  250nMAssay Description:Inhibition of human Peroxisome proliferator activated receptor gammaMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  20nMAssay Description:Maximal intrinsic response against peroxisome proliferator activated receptor gamma transactivationMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataIC50:  250nMAssay Description:Inhibition of human peroxisome proliferator activated receptor gamma bindingMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Cnrs Umr 6052

Curated by ChEMBL
LigandPNGBDBM28681(5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)...)
Affinity DataEC50:  4nMAssay Description:In vitro effective concentration against human peroxisome proliferator activated receptor gamma/Gal4 in cell-based transactivation assayMore data for this Ligand-Target Pair