BDBM50030474 Avandamet::Avandaryl::Avandia::BRL-49653::CHEBI:50122::Rosiglitazone::US10744117, Compound Rosiglitazone::US9562012, rosiglitazone

SMILES CN(CCOc1ccc(CC2SC(=O)NC2=O)cc1)c1ccccn1

InChI Key InChIKey=YASAKCUCGLMORW-UHFFFAOYSA-N

Data  8 KI  34 IC50  5 Kd  68 EC50  1 Koff

PDB links: 13 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 68 hits for monomerid = 50030474   

TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  280nMAssay Description:Agonist activity at human PPARgamma expressed in nonhuman mammalian cells assessed as increase in receptor transcriptional activity incubated for 22 ...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  18nMAssay Description:Agonist activity at GAL4-tagged human PPAR receptorMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  260nMAssay Description:Agonist activity at N-terminal Gal4 fused human PPARgamma LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  40nMAssay Description:Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells at 100 nM to 100 uM incubated for 20 to 22 hrs by luciferase report...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  259nMAssay Description:Transactivation of human PPARgamma transfected in U2OS cells co-tranfected with human RXR measured after 24 hrs by luciferase reporter assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  18nMAssay Description:Agonist activity at GAL4-tagged human PPAR receptorMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  200nMAssay Description:Agonist activity at recombinant human PPARgamma LBD (205 to 505 residues) expressed in African green monkey COS-1 cells incubated for 18 hrs by lucif...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  76nMAssay Description:Agonist activity at GAL4-tagged PPARg-LBD (unknown origin) expressed in HEK293 cells assessed as induction of receptor transactivation incubated for ...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  481nMAssay Description:Agonist activity at PPARg-LBD (unknown origin) expressed in HEK293 cells assessed as recruitment of TIF2 incubated for 16 hrs by luciferase reporter ...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  297nMAssay Description:Agonist activity at PPARg-LBD (unknown origin) expressed in HEK293 cells assessed as recruitment of MED1 incubated for 16 hrs by luciferase reporter ...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  156nMAssay Description:Agonist activity at human PPARgamma transfected in human HEK293 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor alpha(Homo sapiens (Human))
University Of Toledo College Of Pharmacy And Pharmaceutical Sciences

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  3.39E+3nMAssay Description:Agonist activity at human PPARalpha transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactiv...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPeroxisome proliferator-activated receptor delta(Homo sapiens (Human))
University Of Toledo College Of Pharmacy And Pharmaceutical Sciences

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  8.89E+3nMAssay Description:Agonist activity at human PPARdelta transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactiv...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  144nMAssay Description:Agonist activity at human PPARgamma transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactiv...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  1.92E+5nMAssay Description:Agonist activity at human Gal4 fused PPARgamma LBD expressed in COS-7 cells incubated for 24 hrs by firefly luciferase reporter gene assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  83nMAssay Description:Agonist activity at recombinant N-terminal His6 -tagged GFP fused PPARgamma LBD (unknown origin) (203 to 477 residues) expressed in Escherichia cell ...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  169nMAssay Description:Agonist activity at PPARgamma (unknown origin)More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  100nMAssay Description:Partial agonist activity at sGSF-PPARgamma (unknown origin) assessed as CBP-1 recruitment by HT-FRET assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  26nMAssay Description:Partial agonist activity at PPARgamma LBD (unknown origin) assessed as increase in FITC-labeled PGC-1alpha coactivator peptide recruitment by HTRF as...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  4.40E+4nMAssay Description:Partial agonist activity at PPARgamma LBD (unknown origin) assessed as increase in FITC-labeled PGC-1alpha coactivator peptide recruitment in presenc...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  134nMAssay Description:Agonist activity at pBIND tagged human PPARgamma expressed in human HEK293 cells incubated for 18 hrs by dual luciferase reporter assay relative to c...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  40nMAssay Description:Agonist activity at yeast Gal4-fused human PPARgamma transfected in human HepG2 cells assessed as transactivation by measuring beta-galactosidase act...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  49nMAssay Description:Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase/beta-galactosidase reporter gene assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  120nMAssay Description:Agonist activity at human PPARgamma measured by dual luciferase reporter gene assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  27nMAssay Description:Agonist activity at Gal4-fused PPARgamma (unknown origin) expressed in human U2OS cells co-transfected with pSG5 expression vector preincubated for 4...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  300nMAssay Description:Binding affinity to PPARgamma (unknown origin)More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  9nMAssay Description:Agonist activity at human PPARgamma transfected in HEK293 cells assessed increase in luciferase activity incubated for 24 hrsMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  730nMAssay Description:Agonist activity at GAL4-fused human PPARgamma expressed in HepG2 cellsMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  14nMAssay Description:Agonist activity at PPAR-gamma in human BMMSC cells assessed as induction of adiponectin production in presence of IDX adipogenic induction medium an...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  1nMAssay Description:After 24 h treatment with the medicament, the cells were lysed with a lysis solution (Cell Culture Lysis buffer, Promega) and centrifuged, and the su...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor delta(Homo sapiens (Human))
University Of Toledo College Of Pharmacy And Pharmaceutical Sciences

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  5.25E+3nMAssay Description:After 24 h treatment with the medicament, the cells were lysed with a lysis solution (Cell Culture Lysis buffer, Promega) and centrifuged, and the su...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  10nMAssay Description:Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
TargetFree fatty acid receptor 1(Homo sapiens (Human))
Suez Canal University

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  1.15E+4nMAssay Description:Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  39nMAssay Description:Agonist activity at human GAL4-PPARgamma ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Mus musculus)
Institute Of Chinese Materia Medica

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  30nMAssay Description:Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  40nMAssay Description:Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transacti...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  87nMAssay Description:Agonist activity at human PPARgamma transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor alpha(Homo sapiens (Human))
University Of Toledo College Of Pharmacy And Pharmaceutical Sciences

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  240nMAssay Description:Transactivation of N-terminal Gal4 DNA binding domain-linked human PPARalpha ligand binding domain after 24 hrs by luciferase reporter gene assay rel...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  89nMAssay Description:Transcriptional activation of peroxisome proliferator activated receptor gammaMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  260nMAssay Description:Agonist activity at GAL4-tagged human PPARgamma ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  40nMAssay Description:Inhibition of FTase-catalyzed incorporation of [3H]- FPP radioligand into recombinant Ha-Ras by 50% at an enzyme concentration of 1 nM.More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  95nMAssay Description:Displacement of N-terminal biotin-labeled SMRT-ID1 (2339 to 2363 residues) from recombinant GST-tagged PPARgamma (unknown origin) expressed in Escher...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  52nMAssay Description:Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled LCOR (39 to ...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  117nMAssay Description:Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled NCoA3 (671 t...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  316nMAssay Description:Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled SRC1 (619 to...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  326nMAssay Description:Displacement of N-terminal biotin-labeled NCOR-ID1 (2253 to 2277 residues) from recombinant GST-tagged PPARgamma (unknown origin) expressed in Escher...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  114nMAssay Description:Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled NCoA3 (607 t...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  332nMAssay Description:Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled PGC1alpha (1...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  300nMAssay Description:Ability to displace [3H]quipazine binding to 5-hydroxytryptamine 3 receptor sites in NG 108-15.More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataEC50:  1.10E+3nMAssay Description:Transactivation activity at Gal4 fused full length human PPARgamma LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair