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Assay Detail

CHEMBL4414338

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

Binding
Activation of human Gal4-fused PPARgamma LBD transfected in HEK293T after 14 to 16 hrs by dual-glo luciferase reporter gene assay
18
Total Activities
18
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 gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.
Pollinger J, Gellrich L, Schierle S, Kilu W, Schmidt J, Kalinowsky L, Ohrndorf J, Kaiser A, Heering J, Proschak E, Merk D.
J Med Chem (2019) 62 : 2112 -2126
PubMed 30702885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 4.80 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4575123 1 5.68
CHEMBL459972 1 5.52
CHEMBL4458208 1 5.51
CHEMBL491950 1 5.26
CHEMBL4536821 1 4.92
CHEMBL454691 1 4.89
CHEMBL512563 1 4.89
CHEMBL4459701 1 4.88
CHEMBL4439891 1 4.85
CHEMBL4514313 1 4.55
CHEMBL461409 1 4.52
CHEMBL4471255 1 4.48
CHEMBL88917 1 4.44
CHEMBL459521 1 4.42
CHEMBL4443400 1 4.31
CHEMBL4533202 1 4.28
CHEMBL295416 PIRINIXIC ACID 2.0 1 4.27
CHEMBL274797 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4575123 EC50 = 2100.0 nM 5.68
CHEMBL459972 EC50 = 3000.0 nM 5.52
CHEMBL4458208 EC50 = 3100.0 nM 5.51
CHEMBL491950 EC50 = 5500.0 nM 5.26
CHEMBL4536821 EC50 = 12000.0 nM 4.92
CHEMBL454691 EC50 = 13000.0 nM 4.89
CHEMBL512563 EC50 = 13000.0 nM 4.89
CHEMBL4459701 EC50 = 13200.0 nM 4.88
CHEMBL4439891 EC50 = 14000.0 nM 4.85
CHEMBL4514313 EC50 = 28000.0 nM 4.55
CHEMBL461409 EC50 = 30000.0 nM 4.52
CHEMBL4471255 EC50 = 33000.0 nM 4.48
CHEMBL88917 EC50 = 36000.0 nM 4.44
CHEMBL459521 EC50 = 38000.0 nM 4.42
CHEMBL4443400 EC50 = 49000.0 nM 4.31
CHEMBL4533202 EC50 = 52000.0 nM 4.28
CHEMBL295416 PIRINIXIC ACID EC50 = 54000.0 nM 4.27
CHEMBL274797 EC50 - -