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Assay Detail

CHEMBL4189162

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

Binding
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
78
Total Activities
78
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 78 5.69 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4204173 1 7.08
CHEMBL4205664 1 6.41
CHEMBL193836 1 6.22
CHEMBL4204689 1 6.16
CHEMBL4206963 1 6.12
CHEMBL4207558 1 6.09
CHEMBL4211789 1 6.02
CHEMBL4217033 1 6.02
CHEMBL4209406 1 5.94
CHEMBL4210295 1 5.89
CHEMBL4208749 1 5.70
CHEMBL4203030 1 5.64
CHEMBL4216299 1 5.52
CHEMBL4205820 1 5.50
CHEMBL4208949 1 5.46
CHEMBL4217743 1 5.37
CHEMBL4218028 1 5.36
CHEMBL4202808 1 5.28
CHEMBL4212795 1 5.23
CHEMBL4211333 1 5.21
CHEMBL4206438 1 5.16
CHEMBL4213990 1 5.12
CHEMBL4207869 1 5.05
CHEMBL4212497 1 5.04
CHEMBL4210685 1 -
CHEMBL4216915 1 -
CHEMBL4209589 1 -
CHEMBL396869 1 -
CHEMBL396870 1 -
CHEMBL3302645 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4204173 EC50 = 84.0 nM 7.08
CHEMBL4205664 EC50 = 390.0 nM 6.41
CHEMBL193836 EC50 = 600.0 nM 6.22
CHEMBL4204689 EC50 = 700.0 nM 6.16
CHEMBL4206963 EC50 = 760.0 nM 6.12
CHEMBL4207558 EC50 = 820.0 nM 6.09
CHEMBL4211789 EC50 = 950.0 nM 6.02
CHEMBL4217033 EC50 = 950.0 nM 6.02
CHEMBL4209406 EC50 = 1140.0 nM 5.94
CHEMBL4210295 EC50 = 1300.0 nM 5.89
CHEMBL4208749 EC50 = 2000.0 nM 5.70
CHEMBL4203030 EC50 = 2300.0 nM 5.64
CHEMBL4216299 EC50 = 3000.0 nM 5.52
CHEMBL4205820 EC50 = 3200.0 nM 5.50
CHEMBL4208949 EC50 = 3500.0 nM 5.46
CHEMBL4217743 EC50 = 4300.0 nM 5.37
CHEMBL4218028 EC50 = 4400.0 nM 5.36
CHEMBL4202808 EC50 = 5300.0 nM 5.28
CHEMBL4212795 EC50 = 5900.0 nM 5.23
CHEMBL4211333 EC50 = 6200.0 nM 5.21
CHEMBL4206438 EC50 = 7000.0 nM 5.16
CHEMBL4213990 EC50 = 7600.0 nM 5.12
CHEMBL4207869 EC50 = 8900.0 nM 5.05
CHEMBL4212497 EC50 = 9100.0 nM 5.04
CHEMBL4216312 EC50 - -
CHEMBL4205207 EC50 - -
CHEMBL4206568 EC50 - -
CHEMBL4212179 EC50 - -
CHEMBL4217160 EC50 - -
CHEMBL4203591 EC50 - -
CHEMBL4203210 EC50 - -
CHEMBL4218741 EC50 - -
CHEMBL4208494 EC50 - -
CHEMBL4204076 EC50 - -
CHEMBL4216278 EC50 - -
CHEMBL4213794 EC50 - -
CHEMBL4212467 EC50 - -
CHEMBL4203460 EC50 - -
CHEMBL4212018 EC50 - -
CHEMBL4215061 EC50 - -
CHEMBL4213472 EC50 - -
CHEMBL4211327 EC50 - -
CHEMBL4211525 EC50 - -
CHEMBL4203867 EC50 - -
CHEMBL3302645 EC50 - -
CHEMBL396870 EC50 - -
CHEMBL396869 EC50 - -
CHEMBL4209589 EC50 - -
CHEMBL4216915 EC50 - -
CHEMBL4210685 EC50 - -