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Assay Detail

CHEMBL5157824

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

Binding
Agonist activity at pBIND tagged human PPARdelta expressed in human HepG2 cells incubated for 18 hrs by dual luciferase reporter assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis, and biological evaluation of novel dual FFA1 and PPARδ agonists possessing phenoxyacetic acid scaffold.
Zhou Z, Cai Z, Zhang C, Yang B, Chen L, He Y, Zhang L, Li Z.
Bioorg Med Chem (2022) 56 : 116615 -116615
PubMed 35051813 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 5.91 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38508 1 8.00
CHEMBL5205109 1 6.77
CHEMBL5173019 1 6.57
CHEMBL5178528 1 6.44
CHEMBL5192621 1 6.41
CHEMBL5196452 1 6.35
CHEMBL5186275 1 6.32
CHEMBL5183783 1 6.27
CHEMBL5191306 1 6.06
CHEMBL5208111 1 5.79
CHEMBL5173326 1 5.75
CHEMBL5181439 1 5.71
CHEMBL5190883 1 5.67
CHEMBL5171641 1 5.54
CHEMBL5187322 1 5.53
CHEMBL5199948 1 5.51
CHEMBL5186963 1 5.49
CHEMBL5184830 1 5.49
CHEMBL5175597 1 5.44
CHEMBL5200197 1 5.42
CHEMBL5176157 1 5.37
CHEMBL5203672 1 5.35
CHEMBL5194153 1 5.33
CHEMBL5175750 1 5.32
CHEMBL5175124 1 -
CHEMBL121 ROSIGLITAZONE 4.0 1 -
CHEMBL21241 GW7647 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38508 EC50 = 10.0 nM 8.00
CHEMBL5205109 EC50 = 170.0 nM 6.77
CHEMBL5173019 EC50 = 270.0 nM 6.57
CHEMBL5178528 EC50 = 360.0 nM 6.44
CHEMBL5192621 EC50 = 390.0 nM 6.41
CHEMBL5196452 EC50 = 450.0 nM 6.35
CHEMBL5186275 EC50 = 480.0 nM 6.32
CHEMBL5183783 EC50 = 540.0 nM 6.27
CHEMBL5191306 EC50 = 880.0 nM 6.06
CHEMBL5208111 EC50 = 1610.0 nM 5.79
CHEMBL5173326 EC50 = 1760.0 nM 5.75
CHEMBL5181439 EC50 = 1950.0 nM 5.71
CHEMBL5190883 EC50 = 2160.0 nM 5.67
CHEMBL5171641 EC50 = 2920.0 nM 5.54
CHEMBL5187322 EC50 = 2980.0 nM 5.53
CHEMBL5199948 EC50 = 3120.0 nM 5.51
CHEMBL5186963 EC50 = 3250.0 nM 5.49
CHEMBL5184830 EC50 = 3240.0 nM 5.49
CHEMBL5175597 EC50 = 3630.0 nM 5.44
CHEMBL5200197 EC50 = 3850.0 nM 5.42
CHEMBL5176157 EC50 = 4230.0 nM 5.37
CHEMBL5203672 EC50 = 4510.0 nM 5.35
CHEMBL5194153 EC50 = 4710.0 nM 5.33
CHEMBL5175750 EC50 = 4750.0 nM 5.32
CHEMBL5175124 EC50 - -
CHEMBL121 ROSIGLITAZONE EC50 - -
CHEMBL21241 GW7647 EC50 - -