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Assay Detail

CHEMBL4413810

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

Binding
Inverse agonist activity at CMX-gal4-fused ERRgamma (unknown origin) transfected in human AD293 cells co-expressing CMV-beta galactosidase assessed as effect on beta-galactosidase activity after 24 hrs by luciferase reporter gene assay
10
Total Activities
10
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

Estrogen-related receptor gamma (CHEMBL4245)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Potent, Selective, and Orally Bioavailable Estrogen-Related Receptor-γ Inverse Agonists To Restore the Sodium Iodide Symporter Function in Anaplastic Thyroid Cancer.
Kim J, Song J, Ji HD, Yoo EK, Lee JE, Lee SB, Oh JM, Lee S, Hwang JS, Yoon H, Kim DS, Lee SJ, Jeong M, Lee S, Kim KH, Choi HS, Lee SW, Park KG, Lee IK, Kim SH, Hwang H, Jeon YH, Chin J, Cho SJ.
J Med Chem (2019) 62 : 1837 -1858
PubMed 30657313 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.54 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4436391 1 8.22
CHEMBL4437929 1 7.75
CHEMBL4580171 1 7.75
CHEMBL4579002 1 7.75
CHEMBL4451327 1 7.70
CHEMBL4443694 1 7.19
CHEMBL4541589 1 7.19
CHEMBL4472718 1 7.16
CHEMBL3932162 1 7.11
CHEMBL4585424 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4436391 IC50 = 6.0 nM 8.22
CHEMBL4437929 IC50 = 18.0 nM 7.75
CHEMBL4580171 IC50 = 18.0 nM 7.75
CHEMBL4579002 IC50 = 18.0 nM 7.75
CHEMBL4451327 IC50 = 20.0 nM 7.70
CHEMBL4443694 IC50 = 65.0 nM 7.19
CHEMBL4541589 IC50 = 64.0 nM 7.19
CHEMBL4472718 IC50 = 69.0 nM 7.16
CHEMBL3932162 IC50 = 77.0 nM 7.11
CHEMBL4585424 IC50 - -