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Assay Detail

CHEMBL896468

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
27
Total Activities
27
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

Synthesis and SAR of selective benzothiophene, benzofuran, and indole-based peroxisome proliferator-activated receptor delta agonists.
Filzen GF, Bratton L, Cheng XM, Erasga N, Geyer A, Lee C, Lu G, Pulaski J, Sorenson RJ, Unangst PC, Trivedi BK, Xu X.
Bioorg Med Chem Lett (2007) 17 : 3630 -3635
PubMed 17512197 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.22 5.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL234589 1 5.43
CHEMBL234799 1 5.27
CHEMBL234588 1 5.24
CHEMBL391084 1 5.20
CHEMBL234587 1 5.12
CHEMBL391085 1 5.06
CHEMBL234381 1 -
CHEMBL234170 1 -
CHEMBL265868 1 -
CHEMBL391457 1 -
CHEMBL233978 1 -
CHEMBL231690 1 -
CHEMBL393373 1 -
CHEMBL231689 1 -
CHEMBL231688 1 -
CHEMBL393767 1 -
CHEMBL234801 1 -
CHEMBL234800 1 -
CHEMBL393766 1 -
CHEMBL234383 1 -
CHEMBL234382 1 -
CHEMBL234169 1 -
CHEMBL234168 1 -
CHEMBL391068 1 -
CHEMBL233976 1 -
CHEMBL393765 1 -
CHEMBL38943 GW501516 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL234589 IC50 = 3730.0 nM 5.43
CHEMBL234799 IC50 = 5400.0 nM 5.27
CHEMBL234588 IC50 = 5790.0 nM 5.24
CHEMBL391084 IC50 = 6260.0 nM 5.20
CHEMBL234587 IC50 = 7580.0 nM 5.12
CHEMBL391085 IC50 = 8660.0 nM 5.06
CHEMBL234381 IC50 - -
CHEMBL234170 IC50 - -
CHEMBL265868 IC50 - -
CHEMBL391457 IC50 - -
CHEMBL233978 IC50 > 10000.0 nM -
CHEMBL231690 IC50 > 10000.0 nM -
CHEMBL393373 IC50 > 10000.0 nM -
CHEMBL231689 IC50 > 10000.0 nM -
CHEMBL231688 IC50 > 10000.0 nM -
CHEMBL393767 IC50 > 10000.0 nM -
CHEMBL234801 IC50 > 10000.0 nM -
CHEMBL234800 IC50 > 10000.0 nM -
CHEMBL393766 IC50 > 10000.0 nM -
CHEMBL234383 IC50 > 10000.0 nM -
CHEMBL234382 IC50 > 10000.0 nM -
CHEMBL234169 IC50 > 10000.0 nM -
CHEMBL234168 IC50 > 10000.0 nM -
CHEMBL391068 IC50 > 10000.0 nM -
CHEMBL233976 IC50 > 10000.0 nM -
CHEMBL393765 IC50 - -
CHEMBL38943 GW501516 IC50 - -