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Assay Detail

CHEMBL1679579

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

Functional
Antagonist activity at 6his-tagged ERRalpha LBD assessed as inhibition of recruitment of GST-labeled coactivator Scr2 by TR-FRET assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Steroid hormone receptor ERR1 (CHEMBL3429)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of diaryl ether-based ligands for estrogen-related receptor α as potential antidiabetic agents.
Patch RJ, Searle LL, Kim AJ, De D, Zhu X, Askari HB, O'Neill JC, Abad MC, Rentzeperis D, Liu J, Kemmerer M, Lin L, Kasturi J, Geisler JG, Lenhard JM, Player MR, Gaul MD.
J Med Chem (2011) 54 : 788 -808
PubMed 21218783 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 6.55 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1671982 1 7.89
CHEMBL1671969 1 7.80
CHEMBL1671970 1 7.44
CHEMBL1671971 1 7.40
CHEMBL1671964 1 7.33
CHEMBL1671974 1 7.24
CHEMBL1671981 1 7.21
CHEMBL1671972 1 7.17
CHEMBL1671973 1 7.16
CHEMBL1671966 1 7.10
CHEMBL1671967 1 6.85
CHEMBL1671965 1 6.78
CHEMBL478524 1 6.72
CHEMBL1671978 1 6.66
CHEMBL1671963 1 6.62
CHEMBL1671955 1 6.57
CHEMBL1671959 1 6.55
CHEMBL1671956 1 6.54
CHEMBL1671986 1 6.46
CHEMBL1671957 1 6.33
CHEMBL1671975 1 6.33
CHEMBL1671962 1 6.30
CHEMBL1671869 1 6.27
CHEMBL1671977 1 6.19
CHEMBL1671968 1 6.14
CHEMBL1671987 1 6.14
CHEMBL1671984 1 6.14
CHEMBL1671985 1 6.10
CHEMBL1671976 1 6.05
CHEMBL1671980 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1671982 IC50 = 13.0 nM 7.89
CHEMBL1671969 IC50 = 16.0 nM 7.80
CHEMBL1671970 IC50 = 36.0 nM 7.44
CHEMBL1671971 IC50 = 40.0 nM 7.40
CHEMBL1671964 IC50 = 47.0 nM 7.33
CHEMBL1671974 IC50 = 57.0 nM 7.24
CHEMBL1671981 IC50 = 62.0 nM 7.21
CHEMBL1671972 IC50 = 68.0 nM 7.17
CHEMBL1671973 IC50 = 70.0 nM 7.16
CHEMBL1671966 IC50 = 80.0 nM 7.10
CHEMBL1671967 IC50 = 140.0 nM 6.85
CHEMBL1671965 IC50 = 165.0 nM 6.78
CHEMBL478524 IC50 = 190.0 nM 6.72
CHEMBL1671978 IC50 = 220.0 nM 6.66
CHEMBL1671963 IC50 = 240.0 nM 6.62
CHEMBL1671955 IC50 = 270.0 nM 6.57
CHEMBL1671959 IC50 = 280.0 nM 6.55
CHEMBL1671956 IC50 = 290.0 nM 6.54
CHEMBL1671986 IC50 = 350.0 nM 6.46
CHEMBL1671975 IC50 = 470.0 nM 6.33
CHEMBL1671957 IC50 = 470.0 nM 6.33
CHEMBL1671962 IC50 = 500.0 nM 6.30
CHEMBL1671869 IC50 = 540.0 nM 6.27
CHEMBL1671977 IC50 = 640.0 nM 6.19
CHEMBL1671968 IC50 = 720.0 nM 6.14
CHEMBL1671987 IC50 = 730.0 nM 6.14
CHEMBL1671984 IC50 = 720.0 nM 6.14
CHEMBL1671985 IC50 = 800.0 nM 6.10
CHEMBL1671976 IC50 = 890.0 nM 6.05
CHEMBL1671980 IC50 = 1000.0 nM 6.00
CHEMBL1671960 IC50 = 1000.0 nM 6.00
CHEMBL1671958 IC50 = 1100.0 nM 5.96
CHEMBL1671983 IC50 = 1200.0 nM 5.92
CHEMBL1671979 IC50 = 1300.0 nM 5.89
CHEMBL1671988 IC50 = 1800.0 nM 5.75
CHEMBL1671961 IC50 = 2400.0 nM 5.62
CHEMBL1671989 IC50 = 2600.0 nM 5.58