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Assay Detail

CHEMBL896363

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]5-(4-(3-(5-methyl-2-phenyloxazol-4-yl)propanoyl)benzyl)thiazolidine-2,4-dione from human PPARgamma after 2 hrs by SPA assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of highly potent and selective benzyloxybenzyl-based peroxisome proliferator-activator receptor (PPAR) delta agonists.
Bratton LD, Filzen GF, Geyer A, Hoffman JK, Lu G, Pulaski J, Trivedi BK, Unangst PC, Xu X.
Bioorg Med Chem Lett (2007) 17 : 3624 -3629
PubMed 17498950 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 4.86 5.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL232395 1 5.25
CHEMBL234663 1 5.12
CHEMBL391478 1 5.04
CHEMBL234662 1 4.86
CHEMBL232396 1 4.67
CHEMBL234659 1 4.63
CHEMBL391479 1 4.48
CHEMBL267147 1 -
CHEMBL234660 1 -
CHEMBL392951 1 -
CHEMBL234665 1 -
CHEMBL232400 1 -
CHEMBL392950 1 -
CHEMBL232399 1 -
CHEMBL232398 1 -
CHEMBL234661 1 -
CHEMBL232397 1 -
CHEMBL233177 1 -
CHEMBL234666 1 -
CHEMBL392949 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL232395 IC50 = 5560.0 nM 5.25
CHEMBL234663 IC50 = 7570.0 nM 5.12
CHEMBL391478 IC50 = 9120.0 nM 5.04
CHEMBL234662 IC50 = 13800.0 nM 4.86
CHEMBL232396 IC50 = 21600.0 nM 4.67
CHEMBL234659 IC50 = 23600.0 nM 4.63
CHEMBL391479 IC50 = 33300.0 nM 4.48
CHEMBL267147 IC50 - -
CHEMBL234660 IC50 > 11000.0 nM -
CHEMBL392951 IC50 - -
CHEMBL234665 IC50 > 10000.0 nM -
CHEMBL232400 IC50 > 10000.0 nM -
CHEMBL392950 IC50 < 11100.0 nM -
CHEMBL232399 IC50 - -
CHEMBL232398 IC50 - -
CHEMBL234661 IC50 - -
CHEMBL232397 IC50 > 10000.0 nM -
CHEMBL233177 IC50 < 11100.0 nM -
CHEMBL234666 IC50 - -
CHEMBL392949 IC50 - -