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
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 222 hits for monomerid = 28681
Affinity DataKi: 8nMAssay Description:Binding affinity for human PPAR gamma construct expressed in bacteria with 3[H] rosiglitazoneMore data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataKi: 8nMAssay Description:Displacement of [3H]Rosiglitazone from human PPARgammaMore data for this Ligand-Target Pair
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
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
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
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
Affinity DataKi: 50nMAssay Description:Binding affinity for human peroxisome proliferator activated receptor gammaMore data for this Ligand-Target Pair
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
Affinity DataKi: 74nM ΔG°: -9.62kcal/molepH: 7.5 T: 22°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
Affinity DataKi: 120nMAssay Description:Binding affinity to human Peroxisome proliferator activated receptor gamma using scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataKi: 136nMAssay Description:In vitro binding affinity towards human peroxisome proliferator activated receptor gamma (PPAR gamma)More data for this Ligand-Target Pair
Affinity DataKi: 136nMAssay Description:Binding affinity towards peroxisome proliferator activated receptor gamma (PPAR gamma)More data for this Ligand-Target Pair
Affinity DataKi: 440nMAssay Description:Displacement of radiolabeled darglitazone from human PPAR gamma by SPA binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 440nMAssay Description:Displacement of radiolabeled darglitazone from human PPAR gamma by SPA assayMore data for this Ligand-Target Pair
Affinity DataKi: 4.20E+3nMAssay Description:Competitive inhibition of human MAOB expressed in Pichia pastorisMore data for this Ligand-Target Pair
Affinity DataKi: 5.80E+3nMAssay Description:Competitive inhibition of rat MAOB expressed in Pichia pastorisMore data for this Ligand-Target Pair
Affinity DataKi: 1.00E+4nMAssay Description:Binding affinity against Retinoic acid receptor gamma was determined in vitro by using [3H]-ATRA as radioligandMore data for this Ligand-Target Pair
Affinity DataKi: 2.76E+4nMAssay Description:Competitive inhibition of human MAOA expressed in Pichia pastorisMore data for this Ligand-Target Pair
Affinity DataKi: 3.26E+4nMAssay Description:Competitive inhibition of rat MAOA expressed in Pichia pastorisMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor alpha(Human)
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataKi: >3.33E+4nMAssay 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 delta(Human)
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataKi: >3.33E+4nMAssay Description:In vitro binding affinity towards human peroxisome proliferator activated receptor delta (PPAR delta)More data for this Ligand-Target Pair
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
Affinity DataKd: 14.8nM EC50: 3.80nMpH: 7.5 T: 37°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
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 alpha(Human)
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataEC50: >1.20E+4nMpH: 7.2 T: 15°CAssay Description:Human PPAR alpha receptor was expressed as recombinant glutathione-S-transferase (GST)-fusion proteins in Escherichia coli. The purified GST-hPPAR al...More data for this Ligand-Target Pair
Affinity DataIC50: 274nM EC50: 223nMpH: 7.4 T: 23°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
Affinity DataEC50: >7.50E+4nMAssay Description:Primary Collaborators: Kenneth Kaye,Brigham & Womens,Boston MA,kkaye@rics.bwh.harvard.edu,617-525-4256 Chantal Beauchemin,Brigham & Womens,Boston MA,...More data for this Ligand-Target Pair
TargetCorticotropin-releasing factor-binding protein(Human)
Burnham Center For Chemical Genomics
Curated by PubChem BioAssay
Burnham Center For Chemical Genomics
Curated by PubChem BioAssay
Affinity DataEC50: >5.30E+4nMAssay Description:Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, C...More data for this Ligand-Target Pair
Affinity DataIC50: 30nMAssay Description:Initial binding affinity against PPAR-gamma receptorMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor alpha(Human)
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataEC50: >3.00E+3nMAssay Description:In vitro agonist activity tested for transactivation in human PPAR alpha-Gal4 chimeric COS-1 cellsMore data for this Ligand-Target Pair
Affinity DataEC50: 21nMAssay Description:In vitro binding affinity towards human peroxisome proliferator activated receptor alpha (PPAR alpha)More data for this Ligand-Target Pair
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 delta(Human)
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataEC50: >3.00E+3nMAssay Description:In vitro transactivation of human Peroxisome proliferator activated receptor delta measured in PPAR-GAL4 chimeric COS-1 cellsMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor alpha(Human)
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataEC50: >3.00E+3nMAssay Description:In vitro transactivation of human Peroxisome proliferator activated receptor alpha measured in PPAR-GAL4 chimeric COS-1 cellMore data for this Ligand-Target Pair
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
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(Mouse)
Glaxo Wellcome Research and Development
Curated by ChEMBL
Glaxo Wellcome Research and Development
Curated by ChEMBL
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(Mouse)
Glaxo Wellcome Research and Development
Curated by ChEMBL
Glaxo Wellcome Research and Development
Curated by ChEMBL
Affinity DataEC50: 76nMAssay Description:Agonist activity for murine PPAR gamma receptor in transcriptional activation assayMore data for this Ligand-Target Pair
Affinity DataEC50: 43nMAssay Description:Agonist activity for Human PPAR gamma receptor in transcriptional activation assayMore data for this Ligand-Target Pair
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 alpha(Human)
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataEC50: >3.00E+3nMAssay Description:Agonist activity at human PPARalpha receptor expressed in african green monkey COS1 cells cotransfected with fused yeast Gal4-DBD by transactivation ...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor alpha(Human)
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Binding affinity towards human peroxidase proliferator activated receptor alpha (hPPARalpha)More data for this Ligand-Target Pair
Affinity DataEC50: 657nMAssay Description:Binding affinity at human PPAR gammaMore data for this Ligand-Target Pair
Affinity DataIC50: 48nMAssay Description:Binding affinity at human peroxidase proliferator activated receptor gamma (hPPARgamma)More data for this Ligand-Target Pair
Affinity DataEC50: 160nMAssay Description:In vitro transactivation using receptor transactivation assay against hPPAR gammaMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor alpha(Human)
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataEC50: 4.10E+3nMAssay Description:In vitro transactivation using receptor transactivation assay against hPPAR alphaMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor alpha(Human)
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataEC50: 4.10E+3nMAssay Description:In vitro activation of human peroxisome proliferator activated receptor alphaMore data for this Ligand-Target Pair
Affinity DataEC50: 160nMAssay Description:In vitro activation of human peroxisome proliferator activated receptor gamma (PPAR gamma)More data for this Ligand-Target Pair
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 delta(Human)
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataIC50: >5.00E+4nMAssay Description:In vitro binding affinity against human PPAR delta (peroxisome proliferator-activated delta receptor)More data for this Ligand-Target Pair