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Assay Detail

CHEMBL2411354

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Binding
Antagonist activity at human mineralocorticoid receptor assessed as inhibition of binding to coactivator peptide by NH Pro assay
ChEMBL ↗
77
Total Activities
77
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

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 77 6.25 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1393 SPIRONOLACTONE 4.0 1 7.96
CHEMBL2407646 — — 1 7.85
CHEMBL2407647 — — 1 7.48
CHEMBL2407644 — — 1 7.43
CHEMBL2407668 — — 1 7.27
CHEMBL2407645 — — 1 7.26
CHEMBL2407684 — — 1 7.00
CHEMBL2407682 — — 1 7.00
CHEMBL2407648 — — 1 6.77
CHEMBL2407679 — — 1 6.75
CHEMBL2407651 — — 1 6.75
CHEMBL2407854 — — 1 6.72
CHEMBL2407669 — — 1 6.70
CHEMBL2407873 — — 1 6.70
CHEMBL1095097 EPLERENONE 4.0 1 6.62
CHEMBL2407855 — — 1 6.60
CHEMBL2407678 — — 1 6.57
CHEMBL2407670 — — 1 6.55
CHEMBL2407874 — — 1 6.55
CHEMBL2407683 — — 1 6.52
CHEMBL2407664 — — 1 6.52
CHEMBL2407865 — — 1 6.52
CHEMBL2407875 — — 1 6.52
CHEMBL2407659 — — 1 6.47
CHEMBL2407649 — — 1 6.40
CHEMBL2407671 — — 1 6.40
CHEMBL2407638 — — 1 6.35
CHEMBL2407674 — — 1 6.30
CHEMBL2407666 — — 1 6.30
CHEMBL2407643 — — 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1393 SPIRONOLACTONE IC50 = 11.0 nM 7.96
CHEMBL2407646 — IC50 = 14.0 nM 7.85
CHEMBL2407647 — IC50 = 33.0 nM 7.48
CHEMBL2407644 — IC50 = 37.0 nM 7.43
CHEMBL2407668 — IC50 = 54.0 nM 7.27
CHEMBL2407645 — IC50 = 55.0 nM 7.26
CHEMBL2407684 — IC50 = 100.0 nM 7.00
CHEMBL2407682 — IC50 = 100.0 nM 7.00
CHEMBL2407648 — IC50 = 170.0 nM 6.77
CHEMBL2407679 — IC50 = 180.0 nM 6.75
CHEMBL2407651 — IC50 = 180.0 nM 6.75
CHEMBL2407854 — IC50 = 190.0 nM 6.72
CHEMBL2407873 — IC50 = 200.0 nM 6.70
CHEMBL2407669 — IC50 = 200.0 nM 6.70
CHEMBL1095097 EPLERENONE IC50 = 240.0 nM 6.62
CHEMBL2407855 — IC50 = 250.0 nM 6.60
CHEMBL2407678 — IC50 = 270.0 nM 6.57
CHEMBL2407670 — IC50 = 280.0 nM 6.55
CHEMBL2407874 — IC50 = 280.0 nM 6.55
CHEMBL2407683 — IC50 = 300.0 nM 6.52
CHEMBL2407664 — IC50 = 300.0 nM 6.52
CHEMBL2407865 — IC50 = 300.0 nM 6.52
CHEMBL2407875 — IC50 = 300.0 nM 6.52
CHEMBL2407659 — IC50 = 340.0 nM 6.47
CHEMBL2407671 — IC50 = 400.0 nM 6.40
CHEMBL2407649 — IC50 = 400.0 nM 6.40
CHEMBL2407638 — IC50 = 450.0 nM 6.35
CHEMBL2407674 — IC50 = 500.0 nM 6.30
CHEMBL2407666 — IC50 = 500.0 nM 6.30
CHEMBL2407643 — IC50 = 500.0 nM 6.30
CHEMBL2407642 — IC50 = 500.0 nM 6.30
CHEMBL2407673 — IC50 = 570.0 nM 6.24
CHEMBL2407677 — IC50 = 600.0 nM 6.22
CHEMBL2407853 — IC50 = 650.0 nM 6.19
CHEMBL2407637 — IC50 = 750.0 nM 6.12
CHEMBL2407665 — IC50 = 1000.0 nM 6.00
CHEMBL2407660 — IC50 = 990.0 nM 6.00
CHEMBL2407663 — IC50 = 1000.0 nM 6.00
CHEMBL2407681 — IC50 = 1000.0 nM 6.00
CHEMBL2407851 — IC50 = 1200.0 nM 5.92
CHEMBL2407863 — IC50 = 1500.0 nM 5.82
CHEMBL2407680 — IC50 = 2000.0 nM 5.70
CHEMBL2407852 — IC50 = 2000.0 nM 5.70
CHEMBL2407862 — IC50 = 2500.0 nM 5.60
CHEMBL2407672 — IC50 = 2600.0 nM 5.58
CHEMBL2407650 — IC50 = 2900.0 nM 5.54
CHEMBL2407676 — IC50 = 3000.0 nM 5.52
CHEMBL2407667 — IC50 = 3000.0 nM 5.52
CHEMBL2407864 — IC50 = 3000.0 nM 5.52
CHEMBL2407856 — IC50 = 3000.0 nM 5.52