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Assay Detail

CHEMBL4184449

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

Binding
Transactivation of GAL4-fused human PPARdelta LBD expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Peroxisome proliferator-activated receptor delta (CHEMBL3979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulator demonstrates improved safety profile compared to GW501516.
Lagu B, Kluge AF, Goddeeris MM, Tozzo E, Fredenburg RA, Chellur S, Senaiar RS, Jaleel M, Babu DRK, Tiwari NK, Takahashi T, Patane MA.
Bioorg Med Chem Lett (2018) 28 : 533 -536
PubMed 29275935 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.01 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38943 GW501516 2.0 1 8.59
CHEMBL3958704 1 7.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38943 GW501516 EC50 = 2.6 nM 8.59
CHEMBL3958704 EC50 = 37.0 nM 7.43