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Assay Detail

CHEMBL3241715

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

Binding
Antagonist activity at mineralocorticoid receptor (unknown origin) by PathHunter assay
22
Total Activities
22
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

Mineralocorticoid receptor (CHEMBL1994)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.
Cox JM, Chu HD, Yang C, Shen HC, Wu Z, 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 (2014) 24 : 1681 -1684
PubMed 24630411 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.41 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1393 SPIRONOLACTONE 4.0 1 7.96
CHEMBL3234858 1 7.41
CHEMBL3234850 1 7.17
CHEMBL3234863 1 7.09
CHEMBL3234861 1 6.89
CHEMBL3234856 1 6.80
CHEMBL3234847 1 6.62
CHEMBL3234848 1 6.62
CHEMBL1095097 EPLERENONE 4.0 1 6.61
CHEMBL3234849 1 6.57
CHEMBL3234859 1 6.57
CHEMBL3234855 1 6.42
CHEMBL3234862 1 6.33
CHEMBL3234852 1 6.18
CHEMBL3234854 1 6.17
CHEMBL3234846 1 5.96
CHEMBL3234853 1 5.88
CHEMBL3234851 1 5.84
CHEMBL3234860 1 5.82
CHEMBL3234845 1 5.77
CHEMBL2407661 1 5.22
CHEMBL3234857 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1393 SPIRONOLACTONE IC50 = 11.0 nM 7.96
CHEMBL3234858 IC50 = 39.0 nM 7.41
CHEMBL3234850 IC50 = 68.0 nM 7.17
CHEMBL3234863 IC50 = 82.0 nM 7.09
CHEMBL3234861 IC50 = 130.0 nM 6.89
CHEMBL3234856 IC50 = 160.0 nM 6.80
CHEMBL3234847 IC50 = 240.0 nM 6.62
CHEMBL3234848 IC50 = 240.0 nM 6.62
CHEMBL1095097 EPLERENONE IC50 = 244.0 nM 6.61
CHEMBL3234849 IC50 = 270.0 nM 6.57
CHEMBL3234859 IC50 = 270.0 nM 6.57
CHEMBL3234855 IC50 = 380.0 nM 6.42
CHEMBL3234862 IC50 = 470.0 nM 6.33
CHEMBL3234852 IC50 = 660.0 nM 6.18
CHEMBL3234854 IC50 = 670.0 nM 6.17
CHEMBL3234846 IC50 = 1110.0 nM 5.96
CHEMBL3234853 IC50 = 1320.0 nM 5.88
CHEMBL3234851 IC50 = 1440.0 nM 5.84
CHEMBL3234860 IC50 = 1530.0 nM 5.82
CHEMBL3234845 IC50 = 1700.0 nM 5.77
CHEMBL2407661 IC50 = 6000.0 nM 5.22
CHEMBL3234857 IC50 = 6740.0 nM 5.17