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Assay Detail

CHEMBL4189167

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

Binding
Partial agonist activity at human N-terminal alphaHis-SUMO-tagged ERRgamma-LBD (229 to 458 residues) expressed in Escherichia coli BL21 gold (DE3) cells assessed as decrease in RIP140 peptide recruitment after 2 hrs by TR-FRET assay
9
Total Activities
9
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

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 9 5.75 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4204610 1 6.68
CHEMBL4211016 1 6.52
CHEMBL4204153 1 6.09
CHEMBL4209143 1 5.77
CHEMBL4217256 1 5.67
CHEMBL4216886 1 5.51
CHEMBL4211906 1 5.22
CHEMBL4206319 1 5.21
CHEMBL4206727 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4204610 EC50 = 210.0 nM 6.68
CHEMBL4211016 EC50 = 300.0 nM 6.52
CHEMBL4204153 EC50 = 810.0 nM 6.09
CHEMBL4209143 EC50 = 1710.0 nM 5.77
CHEMBL4217256 EC50 = 2150.0 nM 5.67
CHEMBL4216886 EC50 = 3100.0 nM 5.51
CHEMBL4211906 EC50 = 6000.0 nM 5.22
CHEMBL4206319 EC50 = 6200.0 nM 5.21
CHEMBL4206727 EC50 = 7900.0 nM 5.10