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Compound Detail

CHEMBL237122

EPIERENONE
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COC(=O)[C@@H]1CC2=CC(=O)CC[C@]2(C)C2C1C1CC[C@@]3(CCC(=O)O3)[C@@]1(C)[C@H]1O[C@@H]21

Basic Information

ChEMBL ID CHEMBL237122
Name EPIERENONE
Phase Preclinical
Structure Type MOL
InChI Key QBIRIYASLUPKQB-CBHLJOAQSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

414.5
MW (Da)
2.98
ALogP
6
HBA
0
HBD
82.2
PSA (Ų)
0.48
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30O6
MW 414.50
Aromatic Rings 0
Heavy Atoms 30
NP-Likeness 2.32

Activity Summary

Ki 4 meas. best 6.91

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mineralocorticoid receptor
CHEMBL1994
Ki 6.91 6.91 124.0 1
Glucocorticoid receptor
CHEMBL2034
Ki 5.75 5.75 1758.0 1
Androgen receptor
CHEMBL1871
Ki 5.05 5.05 8892.0 1
Progesterone receptor
CHEMBL208
Ki 4.53 4.53 29424.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18038968 10.1021/jm701186z Mineralocorticoid receptor 2
18038968 10.1021/jm701186z Glucocorticoid receptor 1
18038968 10.1021/jm701186z Androgen receptor 1
18038968 10.1021/jm701186z Progesterone receptor 1
18038968 10.1021/jm701186z Estrogen receptor 1
18038968 10.1021/jm701186z Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine