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Assay Detail

CHEMBL2215753

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

Binding
Transactivation of human GAL4-fused PPARgamma ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of fibrate-based analogues inside PPARs.
Giampietro L, D'Angelo A, Giancristofaro A, Ammazzalorso A, De Filippis B, Fantacuzzi M, Linciano P, Maccallini C, Amoroso R.
Bioorg Med Chem Lett (2012) 22 : 7662 -7666
PubMed 23102891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 5.15 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2204689 1 6.10
CHEMBL2204702 1 6.10
CHEMBL2204694 1 6.10
CHEMBL595 PIOGLITAZONE 4.0 1 6.10
CHEMBL2204696 1 5.85
CHEMBL2204686 1 5.27
CHEMBL2204688 1 5.24
CHEMBL2204701 1 5.23
CHEMBL2204692 1 5.22
CHEMBL2204690 1 5.16
CHEMBL2204683 1 5.10
CHEMBL2204697 1 5.00
CHEMBL2204693 1 4.90
CHEMBL2204695 1 4.68
CHEMBL2203301 1 4.52
CHEMBL2204698 1 4.50
CHEMBL2204699 1 4.41
CHEMBL2204687 1 4.26
CHEMBL2204691 1 4.12
CHEMBL2204700 1 -
CHEMBL2204684 1 -
CHEMBL2204685 1 -
CHEMBL683 CLOFIBRIC ACID 2.0 1 -
CHEMBL21241 GW7647 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2204689 EC50 = 800.0 nM 6.10
CHEMBL2204702 EC50 = 800.0 nM 6.10
CHEMBL2204694 EC50 = 800.0 nM 6.10
CHEMBL595 PIOGLITAZONE EC50 = 800.0 nM 6.10
CHEMBL2204696 EC50 = 1400.0 nM 5.85
CHEMBL2204686 EC50 = 5400.0 nM 5.27
CHEMBL2204688 EC50 = 5800.0 nM 5.24
CHEMBL2204701 EC50 = 5900.0 nM 5.23
CHEMBL2204692 EC50 = 6000.0 nM 5.22
CHEMBL2204690 EC50 = 6900.0 nM 5.16
CHEMBL2204683 EC50 = 7900.0 nM 5.10
CHEMBL2204697 EC50 = 10000.0 nM 5.00
CHEMBL2204693 EC50 = 12600.0 nM 4.90
CHEMBL2204695 EC50 = 21000.0 nM 4.68
CHEMBL2203301 EC50 = 30000.0 nM 4.52
CHEMBL2204698 EC50 = 32000.0 nM 4.50
CHEMBL2204699 EC50 = 39300.0 nM 4.41
CHEMBL2204687 EC50 = 54600.0 nM 4.26
CHEMBL2204691 EC50 = 75200.0 nM 4.12
CHEMBL2204700 EC50 - -
CHEMBL2204684 EC50 - -
CHEMBL2204685 EC50 - -
CHEMBL683 CLOFIBRIC ACID EC50 - -
CHEMBL21241 GW7647 EC50 - -