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 109 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: 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
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))
Zhejiang Hisun Pharmaceutical Co., Ltd
US Patent
Zhejiang Hisun Pharmaceutical Co., Ltd
US Patent
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
Affinity DataEC50: 10nMAssay Description:Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
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
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
Institute of Chinese Materia Medica
Curated by ChEMBL
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
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
Affinity DataIC50: 76nMAssay 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
Affinity DataIC50: 4.00E+4nMAssay Description:Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate up...More data for this Ligand-Target Pair
Affinity DataIC50: 6.40E+3nMAssay Description:Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptakeMore data for this Ligand-Target Pair
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
Affinity DataIC50: 38nMAssay Description:Binding affinity to GST-tagged human PPAR-gamma receptor by FRET assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor alpha(Homo sapiens (Human))
Suez Canal University
Curated by ChEMBL
Suez Canal University
Curated by ChEMBL
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
Affinity DataIC50: 10nMAssay Description:Displacement of [3H]rosiglitazone from human recombinant PPARgamma receptor expressed in Escherichia coliMore data for this Ligand-Target Pair
Affinity DataEC50: 89nMAssay Description:Transcriptional activation of peroxisome proliferator activated receptor gammaMore data for this Ligand-Target Pair
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
TargetNuclear receptor coactivator 2 [740-753]()
Metabolic Solutions Development Company, LLC
US Patent
Metabolic Solutions Development Company, LLC
US Patent
Affinity DataIC50: 125nMAssay Description:PPARγ binding is measured by a TR-FRET competitive binding assay using Invitrogen LanthaScreen TR-FRET PPARγ Competitive Binding Assay (I...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 DataIC50: 731nMAssay 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 DataIC50: 292nMAssay Description:Displacement of fluormone-PPARgamma Green from recombinant human N-terminal GST-tagged PPARgamma-LBD by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Displacement of [3H]rosiglitazone from human recombinant PPAR-gamma receptor expressed in Escherichia coli measured after 120 mins by scintillation c...More data for this Ligand-Target Pair
Affinity DataKd: 1.50E+4nMAssay Description:Binding affinity to RXRalpha-LBD (unknown origin) measured up to 120 sec by surface plasma resonance methodMore data for this Ligand-Target Pair
Affinity DataIC50: 3.75E+3nMAssay Description:Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell plasma membrane vesicles assessed as reduction in ATP-dependent [3H]-...More data for this Ligand-Target Pair
Affinity DataIC50: 4.40E+3nMAssay Description:Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate t...More data for this Ligand-Target Pair
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
Affinity DataKon: 0.145M-1s-1Assay 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
Affinity DataKd: 1.20nMAssay 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
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
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
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
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
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
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
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
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
Affinity DataIC50: 6.36E+3nMAssay Description:Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-...More data for this Ligand-Target Pair
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...More data for this Ligand-Target Pair
Affinity DataIC50: 103nMAssay Description:Inhibition of fluormone PPARgamma Green binding to recombinant N-terminal GST-tagged human PPARgamma LBD by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataIC50: 2.80E+3nMAssay Description:Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...More data for this Ligand-Target Pair
Affinity DataIC50: 2.10E+4nMAssay Description:Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
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
Affinity DataIC50: 2.20E+4nMAssay Description:Transrepression activity at human PPARgamma expressed in HEK293 cells assessed as inhibition of TNFalpha induced NF-kappaB promoter activity pretreat...More data for this Ligand-Target Pair
Affinity DataEC50: 240nMAssay Description:Transactivation of recombinant human N-terminal GAL4-DBD fused PPARgamma LBD expressed in reporter cells measured after 24 hrs by luciferase reporter...More data for this Ligand-Target Pair
Affinity DataIC50: 298nMAssay Description:Displacement of fluormone-PPARgamma green from GST-tagged PPARgamma-LBD (unknown origin) by fluorescence polarization assayMore data for this Ligand-Target Pair