Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4413809

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

Binding
Binding affinity to ERalpha (unknown origin) using fluorescein-conjugated coactivator PGC-1alpha incubated for 1 hr by TR-FRET assay
16
Total Activities
16
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 receptor (CHEMBL206)
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 16 5.76 5.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4563806 1 5.94
CHEMBL4436391 1 5.91
CHEMBL4441903 1 5.78
CHEMBL4438589 1 5.77
CHEMBL4451327 1 5.71
CHEMBL3932162 1 5.70
CHEMBL4586542 1 5.67
CHEMBL4513294 1 5.60
CHEMBL4585424 1 -
CHEMBL4443694 1 -
CHEMBL4462077 1 -
CHEMBL4472718 1 -
CHEMBL4541589 1 -
CHEMBL4437929 1 -
CHEMBL4580171 1 -
CHEMBL4579002 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4563806 IC50 = 1142.0 nM 5.94
CHEMBL4436391 IC50 = 1240.0 nM 5.91
CHEMBL4441903 IC50 = 1658.0 nM 5.78
CHEMBL4438589 IC50 = 1700.0 nM 5.77
CHEMBL4451327 IC50 = 1943.0 nM 5.71
CHEMBL3932162 IC50 = 2000.0 nM 5.70
CHEMBL4586542 IC50 = 2116.0 nM 5.67
CHEMBL4513294 IC50 = 2500.0 nM 5.60
CHEMBL4585424 IC50 > 10000.0 nM -
CHEMBL4443694 IC50 > 10000.0 nM -
CHEMBL4462077 IC50 > 10000.0 nM -
CHEMBL4472718 IC50 > 10000.0 nM -
CHEMBL4541589 IC50 > 10000.0 nM -
CHEMBL4437929 IC50 > 10000.0 nM -
CHEMBL4580171 IC50 > 10000.0 nM -
CHEMBL4579002 IC50 > 10000.0 nM -