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Assay Detail

CHEMBL3857090

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

Binding
Inhibition of fluorescien-conjugated coactivator PGC1a binding to ERRbeta (unknown origin) after 1 hr by TR-FRET assay
8
Total Activities
8
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 ERR2 (CHEMBL3751)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of novel 4-hydroxytamoxifen analogs as estrogen-related receptor gamma inverse agonists.
Kim J, Chin J, Im CY, Yoo EK, Woo S, Hwang HJ, Cho JH, Seo KA, Song J, Hwang H, Kim KH, Kim ND, Yoon SK, Jeon JH, Yoon SY, Jeon YH, Choi HS, Lee IK, Kim SH, Cho SJ.
Eur J Med Chem (2016) 120 : 338 -352
PubMed 27236015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.65 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3961676 1 6.14
CHEMBL3978054 1 5.16
CHEMBL3957546 1 -
CHEMBL3897416 1 -
CHEMBL3968559 1 -
CHEMBL3932162 1 -
CHEMBL3973526 1 -
CHEMBL3956562 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3961676 IC50 = 722.0 nM 6.14
CHEMBL3978054 IC50 = 6950.0 nM 5.16
CHEMBL3957546 IC50 > 10000.0 nM -
CHEMBL3897416 IC50 > 10000.0 nM -
CHEMBL3968559 IC50 > 10000.0 nM -
CHEMBL3932162 IC50 > 10000.0 nM -
CHEMBL3973526 IC50 > 10000.0 nM -
CHEMBL3956562 IC50 > 10000.0 nM -