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Assay Detail

CHEMBL5265688

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

Binding
Agonist activity at Gal4-fused mouse PPAR-delta ligand binding domain expressed in CHO-K1 cells assessed as receptor transactivation incubated for 24 to 48 hrs by luciferase reporter gene assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor delta (CHEMBL2458)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery and structure-activity relationship study of 2-piperazinyl-benzothiazole derivatives as potent and selective PPARδ agonists.
Kato T, Ohara T, Suzuki N, Naya N, Fukao K, Tokuyama R, Muto S, Fukasawa H, Itai A, Matsumura KI.
Bioorg Med Chem (2023) 82 : 117215 -117215
PubMed 36840990 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 7.59 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5267473 1 8.24
CHEMBL5272996 1 8.21
CHEMBL5283926 1 8.21
CHEMBL5289740 1 8.16
CHEMBL5290870 1 8.16
CHEMBL5277165 1 8.12
CHEMBL5278892 1 7.92
CHEMBL5290260 1 7.92
CHEMBL5289017 1 7.62
CHEMBL5271479 1 7.60
CHEMBL5268424 1 7.58
CHEMBL5285352 1 7.57
CHEMBL5279586 1 7.55
CHEMBL5268646 1 7.47
CHEMBL5273427 1 7.41
CHEMBL5288454 1 7.34
CHEMBL5278648 1 7.33
CHEMBL5281528 1 7.33
CHEMBL5271300 1 7.21
CHEMBL5180073 1 7.15
CHEMBL38943 GW501516 2.0 1 7.12
CHEMBL5279568 1 7.10
CHEMBL5272924 1 6.96
CHEMBL5267326 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5267473 EC50 = 5.8 nM 8.24
CHEMBL5272996 EC50 = 6.2 nM 8.21
CHEMBL5283926 EC50 = 6.1 nM 8.21
CHEMBL5289740 EC50 = 6.9 nM 8.16
CHEMBL5290870 EC50 = 6.9 nM 8.16
CHEMBL5277165 EC50 = 7.5 nM 8.12
CHEMBL5278892 EC50 = 12.0 nM 7.92
CHEMBL5290260 EC50 = 12.0 nM 7.92
CHEMBL5289017 EC50 = 24.0 nM 7.62
CHEMBL5271479 EC50 = 25.0 nM 7.60
CHEMBL5268424 EC50 = 26.0 nM 7.58
CHEMBL5285352 EC50 = 27.0 nM 7.57
CHEMBL5279586 EC50 = 28.0 nM 7.55
CHEMBL5268646 EC50 = 34.0 nM 7.47
CHEMBL5273427 EC50 = 39.0 nM 7.41
CHEMBL5288454 EC50 = 46.0 nM 7.34
CHEMBL5278648 EC50 = 47.0 nM 7.33
CHEMBL5281528 EC50 = 47.0 nM 7.33
CHEMBL5271300 EC50 = 61.0 nM 7.21
CHEMBL5180073 EC50 = 71.0 nM 7.15
CHEMBL38943 GW501516 EC50 = 76.0 nM 7.12
CHEMBL5279568 EC50 = 79.0 nM 7.10
CHEMBL5272924 EC50 = 110.0 nM 6.96
CHEMBL5267326 EC50 = 110.0 nM 6.96