Compound Detail
CHEMBL2181927
FINERENONE 💊 Approved Drug
Enter ChEMBL ID:
Free Research Context
This compound will appear in recent viewed items on the research home for this browser.
Research home
View demo workspace
💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL2181927 |
| Name | FINERENONE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | BTBHLEZXCOBLCY-QGZVFWFLSA-N |
| Therapeutic | ✓ Yes |
1
Targets
4
Activities
1
Assay Types
3
PK Parameters
11
Publications
6
Known Names
6
Indications
1
Mechanisms
Molecular Properties
378.4
MW (Da)
2.99
ALogP
6
HBA
2
HBD
110.3
PSA (Ų)
0.83
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2021 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Mineralocorticoid receptor antagonist | ANTAGONIST | Mineralocorticoid receptor | ✓ | ✓ |
Indications
Cardiovascular Diseases Diabetes Mellitus, Type 2 Renal Insufficiency, Chronic Diabetes Mellitus Diabetic Nephropathies Heart Failure
ATC Classification
C03DA05
finerenone
Level 1: CARDIOVASCULAR SYSTEM
Level 2: DIURETICS
Activity Summary
IC50 4 meas. best 7.8
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Mineralocorticoid receptor CHEMBL1994 | IC50 | 7.8 | 7.635 | 16.0 | 4 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 4.68 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 26.92 | uL.min-1.(10^6cells)-1 | Rattus norvegicus |
| CL | 97.72 | mL.min-1.g-1 | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Mineralocorticoid receptor | IC50 | = | 16.0 | nM | 7.8 | Antagonist activity against human mineralocorticoid receptor expressed in CHOK1 ... | 22866979 |
| Mineralocorticoid receptor | IC50 | = | 18.0 | nM | 7.75 | Antagonist activity at mineralocorticoid receptor (unknown origin) | 23279862 |
| Mineralocorticoid receptor | IC50 | = | 18.0 | nM | 7.75 | Antagonist activity at Gal4-fused human MR LBD (734 to 985 residues) expressed i... | 28051871 |
| Mineralocorticoid receptor | IC50 | = | 58.0 | nM | 7.24 | Antagonist activity at Gal4-fused human MR LBD expressed in HEK293T cells assess... | 28051871 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.6019/CHEMBL3301361 | ADMET | 6 |
| - | 10.6019/CHEMBL3301361 | No relevant target | 2 |
| 28051871 | 10.1021/acs.jmedchem.6b01065 | Mineralocorticoid receptor | 2 |
| 28051871 | 10.1021/acs.jmedchem.6b01065 | Unchecked | 2 |
| 22866979 | 10.1021/jm300806c | Unchecked | 1 |
| 22866979 | 10.1021/jm300806c | Mineralocorticoid receptor | 1 |
| 23279862 | 10.1016/j.ejmech.2012.11.037 | Mineralocorticoid receptor | 1 |
| 28051871 | 10.1021/acs.jmedchem.6b01065 | Glucocorticoid receptor | 1 |
| 28051871 | 10.1021/acs.jmedchem.6b01065 | Androgen receptor | 1 |
| 28051871 | 10.1021/acs.jmedchem.6b01065 | Progesterone receptor | 1 |
| 28051871 | 10.1021/acs.jmedchem.6b01065 | Homo sapiens | 1 |
Data from ChEMBL 36 via Core Engine