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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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 26 hits for monomerid = 28661   

LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataIC50:  2.00E+3nMpH: 7.0 T: 2°CAssay 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:  1.89E+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:  1.10E+3nMAssay 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:  2.00E+3nMAssay Description:Displacement of [3H]GW 2433 from human PPARalpha by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  1.10E+3nMAssay Description:Maximum transcriptional activation of human PPAR alpha receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPeroxisome proliferator-activated receptor alpha(Mus musculus)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  2.50E+3nMAssay Description:Activity against murine PPAR alpha receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  1.23E+3nMAssay Description:Agonist activity at PPARalpha 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 PPARalpha 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:  3.90E+3nMAssay Description:Activity at human liver PPAR alpha 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:  1.00E+3nMAssay Description:Effect on PPARalpha 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 DataIC50:  463nMAssay Description:Displacement of [3H]2-(4-(2-(3-(2,4-difluorophenyl)-1-heptylureido)ethyl)phenoxy)-2-methylbutanoic acid from human PPARalpha after 30 mins by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  3.90E+3nMAssay Description:Agonist activity at human PPARalpha 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 PPARalpha 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:  1.10E+3nMAssay Description:Agonist activity at human PPARalpha 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:  990nMAssay Description:Transactivation of GAL4-fused human PPARalpha 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:  990nMAssay Description:Agonist activity at human PPARalpha-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: >1.00E+3nMAssay Description:Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 after 24 hrs by luciferase reporter gene ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  3.90E+3nMAssay Description:Agonist activity at human PPARalpha 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:  229nMAssay Description:Transactivation activity at human PPARalpha 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:  2.00E+3nMAssay Description:Agonist activity at PPARalphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  7.70E+3nMAssay Description:Transactivation of GAL4-fused human PPARalpha 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:  400nMAssay Description:Transactivation of human PPARalpha 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:  2.20E+3nMAssay Description:Transactivation of Gal4-fused human PPARalpha 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:  1.10E+3nMAssay Description:Agonist activity at human PPAR-alpha 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:  2.20E+3nMAssay Description:Agonist activity at Gal4-fused human PPAR-alpha 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 alpha(Mus musculus)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM28661(2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)ph...)
Affinity DataEC50:  6.10E+3nMAssay Description:Agonist activity at Gal4-fused mouse PPAR-alpha 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