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  7 KI  33 IC50  4 Kd  64 EC50  1 Koff

PDB links: 13 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 109 hits for monomerid = 50030474   

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
In DepthDetails Article
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
In DepthDetails ArticlePubMed
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
Affinity DataKi:  47nMAssay Description:Binding affinity against Peroxisome proliferator activated receptor gamma (PPAR gamma)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 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 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))
Zhejiang Hisun Pharmaceutical

US Patent
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 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
TargetBile salt export pump(Rattus norvegicus)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
In DepthDetails ArticlePubMed
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 gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
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 DataIC50:  10nMAssay Description:Displacement of [3H]rosiglitazone from human recombinant PPARgamma receptor expressed in Escherichia coliMore 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:  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
TargetNuclear receptor coactivator 2 [740-753]()
Metabolic Solutions Development

US Patent
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
In DepthDetails US Patent
TargetCDGSH iron-sulfur domain-containing protein 1(Homo sapiens (Human))
West Virginia University

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
In DepthDetails ArticlePubMed
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
TargetRetinoic acid receptor RXR-alpha(Homo sapiens (Human))
Xiamen University

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
TargetBile salt export pump(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
In DepthDetails ArticlePubMed
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 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
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
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
TargetBile salt export pump(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
In DepthDetails ArticlePubMed
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
TargetBile salt export pump(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
In DepthDetails ArticlePubMed
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
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
TargetPeroxisome proliferator-activated receptor gamma(Homo sapiens (Human))
Universit?? De Rennes 1

LigandPNGBDBM50030474(Avandamet | Avandaryl | Avandia | BRL-49653 | CHEB...)
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
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