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Assay Detail

CHEMBL759444

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

Binding
Maximum transcriptional activation of human PPAR gamma receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.
Sznaidman ML, Haffner CD, Maloney PR, Fivush A, Chao E, Goreham D, Sierra ML, LeGrumelec C, Xu HE, Montana VG, Lambert MH, Willson TM, Oliver WR, Sternbach DD.
Bioorg Med Chem Lett (2003) 13 : 1517 -1521
PubMed 12699745 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 5.43 6.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38943 GW501516 2.0 1 6.07
CHEMBL38508 1 5.70
CHEMBL40614 1 5.57
CHEMBL39687 1 5.48
CHEMBL39894 1 5.38
CHEMBL288341 1 5.15
CHEMBL39129 1 5.10
CHEMBL416794 1 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38943 GW501516 EC50 = 850.0 nM 6.07
CHEMBL38508 EC50 = 2000.0 nM 5.70
CHEMBL40614 EC50 = 2700.0 nM 5.57
CHEMBL39687 EC50 = 3300.0 nM 5.48
CHEMBL39894 EC50 = 4200.0 nM 5.38
CHEMBL288341 EC50 = 7040.0 nM 5.15
CHEMBL39129 EC50 = 7900.0 nM 5.10
CHEMBL416794 EC50 = 9800.0 nM 5.01