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Assay Detail

CHEMBL760295

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

Binding
In vitro transcription activation on human peroxisome proliferator activated receptor-delta (PPAR delta)
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.
Li Z, Liao C, Ko BC, Shan S, Tong EH, Yin Z, Pan D, Wong VK, Shi L, Ning ZQ, Hu W, Zhou J, Chung SS, Lu XP.
Bioorg Med Chem Lett (2004) 14 : 3507 -3511
PubMed 15177462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 5.59 5.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL331388 1 5.98
CHEMBL325844 1 5.90
CHEMBL295416 PIRINIXIC ACID 2.0 1 5.84
CHEMBL119795 1 5.61
CHEMBL117402 1 5.58
CHEMBL118577 1 5.51
CHEMBL117796 1 5.50
CHEMBL324027 1 5.48
CHEMBL121 ROSIGLITAZONE 4.0 1 5.44
CHEMBL118816 1 5.44
CHEMBL118417 1 5.43
CHEMBL115463 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL331388 EC50 = 1050.0 nM 5.98
CHEMBL325844 EC50 = 1270.0 nM 5.90
CHEMBL295416 PIRINIXIC ACID EC50 = 1460.0 nM 5.84
CHEMBL119795 EC50 = 2450.0 nM 5.61
CHEMBL117402 EC50 = 2630.0 nM 5.58
CHEMBL118577 EC50 = 3090.0 nM 5.51
CHEMBL117796 EC50 = 3160.0 nM 5.50
CHEMBL324027 EC50 = 3310.0 nM 5.48
CHEMBL121 ROSIGLITAZONE EC50 = 3620.0 nM 5.44
CHEMBL118816 EC50 = 3620.0 nM 5.44
CHEMBL118417 EC50 = 3720.0 nM 5.43
CHEMBL115463 EC50 = 4680.0 nM 5.33