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Assay Detail

CHEMBL4189170

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

Binding
Agonist activity at alphaHis-SUMO-tagged ERRbeta-LBD (unknown origin) assessed as decrease in RIP140 peptide recruitment by TR-FRET assay
6
Total Activities
6
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

Steroid hormone receptor ERR2 (CHEMBL3751)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and evaluation of simple phenol amides as ERRγ agonists.
Lin H, Doebelin C, Patouret R, Garcia-Ordonez RD, Chang MR, Dharmarajan V, Bayona CR, Cameron MD, Griffin PR, Kamenecka TM.
Bioorg Med Chem Lett (2018) 28 : 1313 -1319
PubMed 29548571 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.90 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4206963 1 7.70
CHEMBL4217033 1 7.51
CHEMBL4211016 1 7.35
CHEMBL4204689 1 7.05
CHEMBL4205664 1 6.20
CHEMBL4211789 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4206963 EC50 = 20.0 nM 7.70
CHEMBL4217033 EC50 = 31.0 nM 7.51
CHEMBL4211016 EC50 = 45.0 nM 7.35
CHEMBL4204689 EC50 = 90.0 nM 7.05
CHEMBL4205664 EC50 = 630.0 nM 6.20
CHEMBL4211789 EC50 = 2700.0 nM 5.57