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 DataEC50: 2.40nMAssay Description:Agonist activity at PPARgamma LBD in human 293H DA cells after 16 hrs by TR-FRET activation reporter assayMore data for this Ligand-Target Pair
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
Affinity DataEC50: 4nMAssay Description:Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase repor...More data for this Ligand-Target Pair
Affinity DataEC50: 4nMAssay Description:Agonist activity at human PPARalpha at 100 uM by GAL4 transactivation assay relative to WY 14,643More data for this Ligand-Target Pair
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
TargetPeroxisome proliferator-activated receptor delta(Human)
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 5nMAssay Description:In vitro binding affinity for human PPAR delta in SPAMore data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:In vitro binding affinity for human PPAR alpha in SPAMore data for this Ligand-Target Pair
Affinity DataKd: 7nMAssay Description:Binding affinity to human PPARgamma (unknown origin) by competitive TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataKi: 8nMAssay Description:Binding affinity for human PPAR gamma construct expressed in bacteria with 3[H] rosiglitazoneMore data for this Ligand-Target Pair
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 DataEC50: 10nMAssay Description:Agonist activity at PPARgamma receptor expressed in human HepG2 cells by PPRE-luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataEC50: 10nMAssay Description:Transcriptional activation by human PPAR gammaMore data for this Ligand-Target Pair
Affinity DataEC50: 11nMAssay Description:Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene base...More data for this Ligand-Target Pair
Affinity DataEC50: 11nMAssay Description:Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assayMore data for this Ligand-Target Pair
Affinity DataEC50: 11nMAssay Description:Agonist activity at PPARgamma assessed as transcriptional activationMore data for this Ligand-Target Pair
Affinity DataKi: 14nMAssay Description:Binding affinity towards peroxisome proliferator activated receptor gamma (PPAR gamma)More data for this Ligand-Target Pair
Affinity DataEC50: 15nMAssay Description:Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation...More data for this Ligand-Target Pair
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
Affinity DataEC50: 20nMAssay Description:Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivatio...More data for this Ligand-Target Pair
Affinity DataEC50: 20nMAssay Description:Effective concentration against human Peroxisome proliferator activated receptor gamma in Gal4 transactivation assayMore 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
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: 20nMAssay Description:Agonist activity at human PPARgamma in U2OS cells by transactivation 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
Affinity DataEC50: 20nMAssay Description:Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by lucif...More data for this Ligand-Target Pair
Affinity DataEC50: 20nMAssay Description:Maximal intrinsic response against peroxisome proliferator activated receptor gamma transactivationMore data for this Ligand-Target Pair
Affinity DataEC50: 21nMAssay Description:Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR gamma receptorMore data for this Ligand-Target Pair
Affinity DataEC50: 22nMAssay Description:Effective agonist concentration for human PPAR gamma Gal4 construct in transactivation assayMore data for this Ligand-Target Pair
Affinity DataEC50: 30nMAssay Description:Partial agonist activity at human PPARgamma LBD assessed as activation of PBP by HTRF assayMore data for this Ligand-Target Pair
Affinity DataEC50: 30nMAssay Description:Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrsMore data for this Ligand-Target Pair
Affinity DataIC50: 30nMAssay Description:Initial binding affinity against PPAR-gamma receptorMore data for this Ligand-Target Pair
Affinity DataEC50: 30nMAssay Description:Agonist activity at human recombinant PPARgamma1 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene trans...More data for this Ligand-Target Pair
Affinity DataEC50: 33nMAssay Description:Agonist activity at human PPARgamma expressed in african green monkey CV-1 co-transfected with GAL4 by by dual-glo luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataEC50: 33nMAssay Description:Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transacti...More data for this Ligand-Target Pair
Affinity DataEC50: 35nMAssay Description:Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assayMore data for this Ligand-Target Pair
Affinity DataEC50: 35nMAssay Description:Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assayMore data for this Ligand-Target Pair
Affinity DataEC50: 39nMAssay Description:Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataEC50: 39nMAssay Description:Effective concentration against human PPARgamma expressed in HepG2 cellsMore data for this Ligand-Target Pair
Affinity DataEC50: 39nMAssay Description:Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by lucifera...More data for this Ligand-Target Pair
Affinity DataEC50: 39nMAssay Description:Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataEC50: 40nMAssay Description:Effective concentration against human peroxisome proliferator activated receptor gamma in Gal4 transactivation assayMore 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 DataIC50: 43nMAssay Description:Inhibition of PPARgammaMore 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
Affinity DataEC50: 43nMAssay Description:Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation act...More 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: 43nMAssay Description:Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataEC50: 45nMAssay Description:Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assayMore data for this Ligand-Target Pair
Affinity DataEC50: 46nMAssay Description:Partial agonist activity at human PPARgamma LBD assessed as activation of CBP1-453 by HTRF assayMore data for this Ligand-Target Pair