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Assay Detail

CHEMBL3743871

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

Binding
Binding affinity to GST-PPAR-beta/delta LBP (unknown origin) after 3 hrs by TR-FRET assay
6
Total Activities
6
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

Synthesis of 5-trifluoromethyl-2-sulfonylpyridine PPARβ/δ antagonists: Effects on the affinity and selectivity towards PPARβ/δ.
Kaupang Å, Kase ET, Vo CX, Amundsen M, Vik A, Hansen TV.
Bioorg Med Chem (2016) 24 : 247 -260
PubMed 26707845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.52 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2030550 1 7.40
CHEMBL598608 1 6.63
CHEMBL3416764 1 6.55
CHEMBL3740264 1 6.50
CHEMBL3740369 1 6.22
CHEMBL3740002 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2030550 IC50 = 40.1 nM 7.40
CHEMBL598608 IC50 = 233.0 nM 6.63
CHEMBL3416764 IC50 = 284.0 nM 6.55
CHEMBL3740264 IC50 = 320.0 nM 6.50
CHEMBL3740369 IC50 = 598.0 nM 6.22
CHEMBL3740002 IC50 = 1431.0 nM 5.84