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Assay Detail

CHEMBL4131392

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

Binding
Antagonist activity at His6-tagged ERRalpha LBD (unknown origin) assessed as inhibition of GST-tagged SRC-2 co-activator peptide recruitment after 18 hrs by TR-FRET assay
31
Total Activities
31
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 ERR1 (CHEMBL3429)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
Patch RJ, Huang H, Patel S, Cheung W, Xu G, Zhao BP, Beauchamp DA, Rentzeperis D, Geisler JG, Askari HB, Liu J, Kasturi J, Towers M, Gaul MD, Player MR.
Eur J Med Chem (2017) 138 : 830 -853
PubMed 28735214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.68 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4170306 1 8.30
CHEMBL4169272 1 8.10
CHEMBL4161346 1 8.10
CHEMBL4166492 1 8.10
CHEMBL4159613 1 8.05
CHEMBL4163909 1 8.05
CHEMBL4166832 1 7.92
CHEMBL4165363 1 7.89
CHEMBL4172522 1 7.82
CHEMBL4172209 1 7.82
CHEMBL4163054 1 7.80
CHEMBL4163375 1 7.77
CHEMBL4173278 1 7.75
CHEMBL4173757 1 7.72
CHEMBL4177113 1 7.72
CHEMBL4164196 1 7.66
CHEMBL4169919 1 7.64
CHEMBL4164640 1 7.64
CHEMBL4175927 1 7.64
CHEMBL4174856 1 7.64
CHEMBL4161594 1 7.62
CHEMBL4161992 1 7.60
CHEMBL4168072 1 7.60
CHEMBL4171282 1 7.58
CHEMBL4167938 1 7.55
CHEMBL4171419 1 7.47
CHEMBL4174736 1 7.37
CHEMBL4160799 1 7.35
CHEMBL4170236 1 7.34
CHEMBL4159675 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4170306 IC50 = 5.0 nM 8.30
CHEMBL4169272 IC50 = 8.0 nM 8.10
CHEMBL4161346 IC50 = 8.0 nM 8.10
CHEMBL4166492 IC50 = 8.0 nM 8.10
CHEMBL4159613 IC50 = 9.0 nM 8.05
CHEMBL4163909 IC50 = 9.0 nM 8.05
CHEMBL4166832 IC50 = 12.0 nM 7.92
CHEMBL4165363 IC50 = 13.0 nM 7.89
CHEMBL4172522 IC50 = 15.0 nM 7.82
CHEMBL4172209 IC50 = 15.0 nM 7.82
CHEMBL4163054 IC50 = 16.0 nM 7.80
CHEMBL4163375 IC50 = 17.0 nM 7.77
CHEMBL4173278 IC50 = 18.0 nM 7.75
CHEMBL4173757 IC50 = 19.0 nM 7.72
CHEMBL4177113 IC50 = 19.0 nM 7.72
CHEMBL4164196 IC50 = 22.0 nM 7.66
CHEMBL4169919 IC50 = 23.0 nM 7.64
CHEMBL4164640 IC50 = 23.0 nM 7.64
CHEMBL4175927 IC50 = 23.0 nM 7.64
CHEMBL4174856 IC50 = 23.0 nM 7.64
CHEMBL4161594 IC50 = 24.0 nM 7.62
CHEMBL4161992 IC50 = 25.0 nM 7.60
CHEMBL4168072 IC50 = 25.0 nM 7.60
CHEMBL4171282 IC50 = 26.0 nM 7.58
CHEMBL4167938 IC50 = 28.0 nM 7.55
CHEMBL4171419 IC50 = 34.0 nM 7.47
CHEMBL4174736 IC50 = 43.0 nM 7.37
CHEMBL4160799 IC50 = 45.0 nM 7.35
CHEMBL4170236 IC50 = 46.0 nM 7.34
CHEMBL4159675 IC50 = 54.0 nM 7.27
CHEMBL4160018 IC50 = 580.0 nM 6.24