Target family: 3C. 3-Ketosteroid receptors (type: nhr)
Target: Mineralocorticoid receptor

Ligand: aldosterone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Specific hydroxylations determine selective corticosteroid recognition by human glucocorticoid and mineralocorticoid receptors.
Published in: FEBS Lett

Ligand: aldosterone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Pharmacological and functional characterization of human mineralocorticoid and glucocorticoid receptor ligands.
Published in: Eur J Pharmacol

Ligand: apararenone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7 pKi
Reference (Journal): Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist.
Published in: J Med Chem

Ligand: AZD9567 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.420000076293945 pIC50
Reference (Journal): Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
Published in: J Med Chem

Ligand: AZD9977 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi
Reference (Journal): Identification of Mineralocorticoid Receptor Modulators with Low Impact on Electrolyte Homeostasis but Maintained Organ Protection.
Published in: J Med Chem

Ligand: benzodrocortisone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF 4-PREGENEN-11ß-17-21-TRIOL-3,20-DIONE DERIVATIVES

Ligand: budesonide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1997), EMA (2018)
Primary target: no
Median affinity: 7.849999904632568 pEC50
Reference (Journal): Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Published in: J Med Chem

Ligand: corticosterone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: cortisol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1953, prior history unavailable), EMA (2011)
Primary target: no
Median affinity:  pIC50
Reference (Journal): Pharmacological and functional characterization of human mineralocorticoid and glucocorticoid receptor ligands.
Published in: Eur J Pharmacol

Ligand: cortisol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1953, prior history unavailable), EMA (2011)
Primary target: no
Median affinity:  pIC50
Reference (Journal): Specific hydroxylations determine selective corticosteroid recognition by human glucocorticoid and mineralocorticoid receptors.
Published in: FEBS Lett

Ligand: deoxycorticosterone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 11 pIC50
Reference (Journal): Pharmacological and functional characterization of human mineralocorticoid and glucocorticoid receptor ligands.
Published in: Eur J Pharmacol

Ligand: dexamethasone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1958), EMA (2010)
Median affinity: 9 pIC50
Reference (Journal): Pharmacological and functional characterization of human mineralocorticoid and glucocorticoid receptor ligands.
Published in: Eur J Pharmacol

Ligand: dexamethasone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1958), EMA (2010)
Median affinity: 9 pIC50
Reference (Journal): Specific hydroxylations determine selective corticosteroid recognition by human glucocorticoid and mineralocorticoid receptors.
Published in: FEBS Lett

Ligand: drospirenone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  -
Reference (Journal): Dihydrospirorenone (ZK30595): a novel synthetic progestagen--characterization of binding to different receptor proteins.
Published in: Contraception

Ligand: eplerenone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2002)
Primary target: yes
Median affinity: 6.909999847412109 pKi
Reference (Journal): (S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.
Published in: J Med Chem

Ligand: esaxerenone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: Japan (2019)
Primary target: no
Median affinity: 8.619999885559082 pIC50
Reference (Journal): Single- and multiple-dose escalation study to assess pharmacokinetics, pharmacodynamics and safety of oral esaxerenone in healthy Japanese subjects.
Published in: Br J Clin Pharmacol

Ligand: esaxerenone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: Japan (2019)
Primary target: no
Median affinity: 8.619999885559082 pIC50
Reference (Journal): Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy.
Published in: J Med Chem

Ligand: finerenone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2021), EMA (2022)
Primary target: no
Median affinity: 7.739999771118164 pIC50
Reference (Journal): Discovery of BAY 94-8862: a nonsteroidal antagonist of the mineralocorticoid receptor for the treatment of cardiorenal diseases.
Published in: ChemMedChem

Ligand: fludrocortisone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1955), UK (2015)
Primary target: yes
Median affinity: 9.920000076293945 pIC50
Reference (Journal): Pharmacological and functional characterization of human mineralocorticoid and glucocorticoid receptor ligands.
Published in: Eur J Pharmacol

Ligand: fluticasone propionate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: no
Median affinity: 6.829999923706055 pEC50
Reference (Journal): Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Published in: J Med Chem

Ligand: nimodipine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1988)
Primary target: yes
Median affinity: 6.800000190734863 pIC50
Reference (Journal): A number of marketed dihydropyridine calcium channel blockers have mineralocorticoid receptor antagonist activity.
Published in: Hypertension

Ligand: ocedurenone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.569999694824219 pIC50
Reference (Journal): Pharmacological Profile of KBP-5074, a Novel NonSteroidal Mineralocorticoid Receptor Antagonist for the Treatment of Cardiorenal Diseases
Published in: ournal of Drug Research and Development

Ligand: onapristone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.329999923706055 pIC50
Reference (Journal): Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
Published in: Bioorg Med Chem Lett

Ligand: PF-03882845 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.039999961853027 pIC50
Reference (Journal): Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist.
Published in: J Med Chem

Ligand: prednisolone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1955)
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
Published in: J Med Chem

Ligand: prednisolone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1955)
Primary target: no
Median affinity: 7.429999828338623 pKi
Reference (Journal): Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.
Published in: J Med Chem

Ligand: progesterone (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1959)
Primary target: no
Median affinity: 11 pIC50
Reference (Journal): Pharmacological and functional characterization of human mineralocorticoid and glucocorticoid receptor ligands.
Published in: Eur J Pharmacol

Ligand: RU28318 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  -

Ligand: spironolactone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1960)
Primary target: yes
Median affinity: 8.630000114440918 pKi
Reference (Journal): (S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.
Published in: J Med Chem

Ligand: [3H]aldosterone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Extravascular CBG-like sites in rat kidney and mineralocorticoid receptor specificity.
Published in: Am J Physiol

Ligand: [3H]aldosterone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Stimulation of testosterone production in rat Leydig cells by aldosterone is mineralocorticoid receptor mediated.
Published in: Mol Cell Endocrinol

Ligand: ZK112993 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  -