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Assay Detail

CHEMBL2411348

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

Binding
Antagonist activity at estrogen receptor alpha (unknown origin) by NH Pro assay
4
Total Activities
4
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 receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.
Yang C, Shen HC, Wu Z, Chu HD, Cox JM, Balsells J, Crespo A, Brown P, Zamlynny B, Wiltsie J, Clemas J, Gibson J, Contino L, Lisnock J, Zhou G, Garcia-Calvo M, Bateman T, Xu L, Tong X, Crook M, Sinclair P.
Bioorg Med Chem Lett (2013) 23 : 4388 -4392
PubMed 23777778 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.96 5.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2407651 1 5.14
CHEMBL2407647 1 4.77
CHEMBL1095097 EPLERENONE 4.0 1 -
CHEMBL1393 SPIRONOLACTONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2407651 IC50 = 7300.0 nM 5.14
CHEMBL2407647 IC50 = 17000.0 nM 4.77
CHEMBL1095097 EPLERENONE IC50 > 20000.0 nM -
CHEMBL1393 SPIRONOLACTONE IC50 > 20000.0 nM -