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
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 116 hits for monomerid = 50030474
Affinity DataKi: 0.230nMAssay Description:Displacement of [125I]-SI-Ang-2 from AT1 receptor in Rattus norvegicus Sprague-Dawley (rat) liver membranes after 2 hrMore data for this Ligand-Target Pair
Affinity DataKi: 8nM ΔG°: -10.3kcal/molepH: 8.2 T: 2°CAssay Description:Binding assays were performed in 96-well plate format, using a classical filtration assay with a human full length PPARγ construct (GST-PPAR LBD...More data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataKi: 17nMAssay Description:Binding affinity to GST-tagged PPARG LBD (unknown origin) by Fluormone Pan-PPAR Green tracer based TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataKi: 26nMAssay Description:Displacement of [3H]rosiglitazone from human PPAR-gamma incubated for 1 day by radioligand binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 27nMAssay Description:Agonist activity at PPARgamma ligand binding domain (unknown origin) using fluormone Pan-PPAR green tracer by TR-FRET assay based competitive ligand ...More data for this Ligand-Target Pair
TargetCDGSH iron-sulfur domain-containing protein 1(Homo sapiens (Human))
West Virginia University
Curated by ChEMBL
West Virginia University
Curated by ChEMBL
Affinity DataKi: 31nMAssay Description:Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichi...More data for this Ligand-Target Pair
Affinity DataKi: 47nMAssay Description:Binding affinity against Peroxisome proliferator activated receptor gamma (PPAR gamma)More data for this Ligand-Target Pair
Affinity DataKi: 59nMAssay Description:Displacement of fluormone PPAR green tracer ligand from recombinant GST-tagged PPARgamma ligand binding domain (unknown origin) incubated for 4 hrs b...More data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor alpha(Mus musculus)
Terns Pharmaceuticals
Curated by ChEMBL
Terns Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 80nMAssay Description:Activation of mouse liver PPARalphaMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 2.95E+4nMAssay Description:Inhibition of human ERG expressed in CHO cells by patch clamp assayMore data for this Ligand-Target Pair
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
Affinity DataIC50: 76nMAssay Description:Displacement of fluormone PPAR green tracer ligand from recombinant GST-tagged PPARgamma ligand binding domain (unknown origin) incubated for 4 hrs b...More data for this Ligand-Target Pair
Affinity DataEC50: 18nMAssay Description:Agonist activity at GAL4-tagged human PPAR receptorMore data for this Ligand-Target Pair
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
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
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
Affinity DataEC50: 18nMAssay Description:Agonist activity at GAL4-tagged human PPAR receptorMore data for this Ligand-Target Pair
TargetSodium/bile acid cotransporter(Homo sapiens (Human))
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 5.10E+3nMAssay Description:Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed ...More data for this Ligand-Target Pair
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
TargetBile salt export pump(Homo sapiens (Human))
Norman Drug Discovery Training And Consulting
Curated by ChEMBL
Norman Drug Discovery Training And Consulting
Curated by ChEMBL
Affinity DataIC50: 3.80E+3nMAssay Description:Inhibition of human BSEP expressed in HEK293 cell membrane vesicles assessed as reduction in 3H-TCA uptake incubated for 5 mins by radiodetection met...More data for this Ligand-Target Pair
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
Affinity DataKd: 48nMAssay Description:Binding affinity to PPARg (unknown origin) by SPR assayMore data for this Ligand-Target Pair
Affinity DataIC50: 88nMAssay Description:Agonist activity at PPARg-LBD (unknown origin) expressed in HEK293 cells assessed as displacement of NCoR incubated for 16 hrs by luciferase reporter...More data for this Ligand-Target Pair
Affinity DataIC50: 7.70nMAssay Description:Agonist activity at PPARg-LBD (unknown origin) expressed in HEK293 cells assessed as displacement of SMRT incubated for 16 hrs by luciferase reporter...More data for this Ligand-Target Pair
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
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
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
University Of Toledo College Of Pharmacy And Pharmaceutical Sciences
Curated by ChEMBL
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
TargetPeroxisome proliferator-activated receptor delta(Homo sapiens (Human))
University Of Toledo College Of Pharmacy And Pharmaceutical Sciences
Curated by ChEMBL
University Of Toledo College Of Pharmacy And Pharmaceutical Sciences
Curated by ChEMBL
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
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
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
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
Affinity DataEC50: 169nMAssay Description:Agonist activity at PPARgamma (unknown origin)More data for this Ligand-Target Pair
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
Affinity DataKd: 3.30E+3nMAssay Description:Binding affinity to PPARgamma LBD (unknown origin) assessed as dissociation constant followed by heating for 3 mins by Bradford assayMore data for this Ligand-Target Pair
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
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
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
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
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
TargetAmine oxidase [flavin-containing] B(Homo sapiens (Human))
Comsats University Islamabad
Curated by ChEMBL
Comsats University Islamabad
Curated by ChEMBL
Affinity DataIC50: 832nMAssay Description:Inhibition of recombinant human MAO-BMore data for this Ligand-Target Pair
Affinity DataEC50: 120nMAssay Description:Agonist activity at human PPARgamma measured by dual luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataIC50: 90nMAssay Description:Binding affinity to PPARgamma (unknown origin) by lanthascreen TR-FRET assayMore data for this Ligand-Target Pair
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
Affinity DataIC50: 4.40E+3nMAssay Description:Inhibition of PPARgamma (unknown origin) phosphorylation at pS273 residueMore data for this Ligand-Target Pair
Affinity DataKd: 650nMAssay Description:Binding affinity to human PPARgamma-LBD (206 to 477 residues)/human RXRalpha-LBD (224 to 462 residues) heterodimer assessed as dissociation constant ...More data for this Ligand-Target Pair
Affinity DataEC50: 300nMAssay Description:Binding affinity to PPARgamma (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4.00E+5nMAssay Description:Inhibition of PTP1B (unknown origin)More data for this Ligand-Target Pair
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