BDBM28661 2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acid::CHEMBL38943::GW 501516::GW-501516::GW1516::GW501516

SMILES Cc1nc(sc1CSc1ccc(OCC(O)=O)c(C)c1)-c1ccc(cc1)C(F)(F)F

InChI Key InChIKey=YDBLKRPLXZNVNB-UHFFFAOYSA-N

Data  5 KI  13 IC50  89 EC50

PDB links: 1 PDB ID matches this monomer.

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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 25 hits for monomerid = 28661   

LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataIC50:  6.31E+3nMAssay Description:Competition-binding curves for test compounds were determined with expressed human PPAR LBD. Plots of inhibitor concentration versus cpm of radioliga...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  8.90E+3nMAssay Description:The ligand binding domain for PPAR was fused to the yeast transcription factor GAL4 DNA binding domain. CV-1 cells were transiently transfected with ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  850nMAssay Description:The HEK293 cells were co-transfected with DNA constructs containing the ligand-binding domain of PPAR and Gal4-luciferase reporter. The luciferase ac...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataIC50:  6.31E+3nMAssay Description:Displacement of [3H]GW 2433 from human PPARgamma by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPeroxisome proliferator-activated receptor gamma(Mus musculus)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  1.00E+3nMAssay Description:Activity against murine PPAR gamma receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  850nMAssay Description:Maximum transcriptional activation of human PPAR gamma receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at PPARgamma by transactivation assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  1.00E+4nMAssay Description:Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50: >1.00E+4nMAssay Description:Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  8.60E+3nMAssay Description:Effect on PPARgamma transactivation activity in HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at human PPARgamma by transactivation assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells cotransfected with Gal4-DBD assessed as transcriptional activation ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  800nMAssay Description:Agonist activity at human PPARgamma expressed in HepG2 cells cotransfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 h...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  4.10E+3nMAssay Description:Transactivation of GAL4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  4.10E+3nMAssay Description:Agonist activity at human PPARgamma-LBD expressed in CV1 cells cotransfected with Gal4 after 40 hrs by luciferase based transactivation assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  912nMAssay Description:Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometeric analy...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at human PPARgamma by transactivation assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50: >1.20E+3nMAssay Description:Transactivation activity at human PPARgamma expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataIC50:  6.31E+3nMAssay Description:Agonist activity at PPARgammaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50: >1.00E+4nMAssay Description:Transactivation of GAL4-fused human PPARgamma LBD expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50: >1.50E+3nMAssay Description:Transactivation of human PPARgamma expressed in monkey CV-1 cells coexpressing TK-PPRE-Luc after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  4.40E+3nMAssay Description:Transactivation of Gal4-fused human PPARgamma expressed in CHO cells co expressing pG5-Luc reporterMore data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  850nMAssay Description:Agonist activity at human PPAR-gamma assessed as receptor transactivation by measuring maximum induction of alkaline phosphatase activityMore data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  4.40E+3nMAssay Description:Agonist activity at Gal4-fused human PPAR-gamma ligand binding domain expressed in CHO-K1 cells assessed as receptor transactivation incubated for 24...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetPeroxisome proliferator-activated receptor gamma(Mus musculus)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  3.50E+3nMAssay Description:Agonist activity at Gal4-fused mouse PPAR-gamma ligand binding domain expressed in CHO-K1 cells assessed as receptor transactivation incubated for 24...More data for this Ligand-Target Pair
In DepthDetails PubMed