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Assay Detail

CHEMBL1679580

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

Functional
Antagonist activity at ERRalpha LBD expressed in HEK293 cells assessed as Gal4-SRC2 interaction by two hybrid luciferase reporter gene assay
25
Total Activities
25
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HEK293
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 24 5.67 7.05
EC50 1 6.00 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1671982 1 7.05
CHEMBL189753 1 6.43
CHEMBL1671971 1 6.22
CHEMBL1671972 1 6.16
CHEMBL1671990 1 6.00
CHEMBL1671969 1 5.82
CHEMBL1671981 1 5.64
CHEMBL1671965 1 5.64
CHEMBL1671967 1 5.57
CHEMBL1671966 1 5.47
CHEMBL1671955 1 5.44
CHEMBL1671963 1 5.35
CHEMBL1671959 1 5.30
CHEMBL1671964 1 5.23
CHEMBL1671968 1 5.20
CHEMBL1671978 1 5.16
CHEMBL1671973 1 5.03
CHEMBL1671970 1 -
CHEMBL1671869 1 -
CHEMBL1671958 1 -
CHEMBL1671974 1 -
CHEMBL1671975 1 -
CHEMBL1671976 1 -
CHEMBL1671957 1 -
CHEMBL1671956 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1671982 IC50 = 90.0 nM 7.05
CHEMBL189753 IC50 = 370.0 nM 6.43
CHEMBL1671971 IC50 = 600.0 nM 6.22
CHEMBL1671972 IC50 = 700.0 nM 6.16
CHEMBL1671990 EC50 = 1000.0 nM 6.00
CHEMBL1671969 IC50 = 1500.0 nM 5.82
CHEMBL1671981 IC50 = 2300.0 nM 5.64
CHEMBL1671965 IC50 = 2300.0 nM 5.64
CHEMBL1671967 IC50 = 2700.0 nM 5.57
CHEMBL1671966 IC50 = 3400.0 nM 5.47
CHEMBL1671955 IC50 = 3600.0 nM 5.44
CHEMBL1671963 IC50 = 4500.0 nM 5.35
CHEMBL1671959 IC50 = 5000.0 nM 5.30
CHEMBL1671964 IC50 = 5900.0 nM 5.23
CHEMBL1671968 IC50 = 6300.0 nM 5.20
CHEMBL1671978 IC50 = 6900.0 nM 5.16
CHEMBL1671973 IC50 = 9300.0 nM 5.03
CHEMBL1671970 IC50 > 10000.0 nM -
CHEMBL1671869 IC50 > 10000.0 nM -
CHEMBL1671958 IC50 > 10000.0 nM -
CHEMBL1671974 IC50 > 10000.0 nM -
CHEMBL1671975 IC50 > 10000.0 nM -
CHEMBL1671976 IC50 > 10000.0 nM -
CHEMBL1671957 IC50 > 10000.0 nM -
CHEMBL1671956 IC50 > 10000.0 nM -