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Assay Detail

CHEMBL1679770

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Functional
Agonist activity at 6his-tagged ERRalpha LBD assessed as recruitment of GST-labeled coactivator Scr2 by TR-FRET assay
2
Total Activities
2
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
EC50 2 7.14 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 8.23
CHEMBL1671971 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL EC50 = 5.9 nM 8.23
CHEMBL1671971 EC50 = 900.0 nM 6.05