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

Ligand: ABBV-3373 (Antibody)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Discovery of ABBV-3373, an Anti-TNF Glucocorticoid Receptor Modulator Immunology Antibody Drug Conjugate.
Published in: J Med Chem

Ligand: AZD2906 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.890000343322754 pEC50
Reference (Journal): Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
Published in: J Med Chem

Ligand: AZD5423 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.3100004196167 pIC50
Reference (Journal): Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Published in: J Med Chem

Ligand: AZD9567 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.420000076293945 pIC50
Reference (Journal): Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
Published in: J Med Chem

Ligand: AZD9567 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.960000038146973 pEC50
Reference (Journal): Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
Published in: J Med Chem

Ligand: beclometasone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: yes
Median affinity: 8.430000305175781 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

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: betamethasone (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1961)
Primary target: yes
Median affinity: 8.109999656677246 pIC50
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: BI 653048 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.150000095367432 pIC50
Reference (Journal): Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.
Published in: ACS Med Chem Lett

Ligand: budesonide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1997), EMA (2018)
Primary target: yes
Median affinity: 7.420000076293945 pEC50
Reference (Journal): Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Published in: J Med Chem

Ligand: budesonide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1997), EMA (2018)
Primary target: yes
Median affinity: 7.909999847412109 pEC50
Reference (Journal): Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma.
Published in: Bioorg Med Chem Lett

Ligand: C108297 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.149999618530273 pKi
Reference (Journal): 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity.
Published in: Bioorg Med Chem Lett

Ligand: ciclesonide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2006)
Primary target: yes
Median affinity: 7.429999828338623 pKi
Reference (Journal): Preclinical profile of ciclesonide, a novel corticosteroid for the treatment of asthma.
Published in: J Pharmacol Exp Ther

Ligand: clobetasol propionate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1985)
Primary target: yes
Median affinity: 9.180000305175781 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: compound 17 [PMID: 29741897] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.119999885559082 pKi
Reference (Journal): Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
Published in: J Med Chem

Ligand: corticosterone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.199999809265137 pIC50
Reference (Journal): Specific hydroxylations determine selective corticosteroid recognition by human glucocorticoid and mineralocorticoid receptors.
Published in: FEBS Lett

Ligand: corticosterone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.199999809265137 pIC50
Reference (Journal): Functional probing of the human glucocorticoid receptor steroid-interacting surface by site-directed mutagenesis. Gln-642 plays an important role in steroid recognition and binding.
Published in: J Biol Chem

Ligand: corticosterone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.199999809265137 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: yes
Median affinity:  pIC50
Reference (Journal): Functional probing of the human glucocorticoid receptor steroid-interacting surface by site-directed mutagenesis. Gln-642 plays an important role in steroid recognition and binding.
Published in: J Biol Chem

Ligand: cortisol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1953, prior history unavailable), EMA (2011)
Primary target: yes
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: yes
Median affinity:  pIC50
Reference (Journal): Specific hydroxylations determine selective corticosteroid recognition by human glucocorticoid and mineralocorticoid receptors.
Published in: FEBS Lett

Ligand: CpdA (parent molecule) (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.1899995803833 pIC50
Reference (Journal): A fully dissociated compound of plant origin for inflammatory gene repression.
Published in: Proc Natl Acad Sci U S A

Ligand: dazucorilant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.550000190734863 pKi
Reference (Journal): Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist.
Published in: J Med Chem

Ligand: deoxycorticosterone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.2 pIC50
Reference (Journal): Pharmacological and functional characterization of human mineralocorticoid and glucocorticoid receptor ligands.
Published in: Eur J Pharmacol

Ligand: deoxycorticosterone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.2 pIC50
Reference (Journal): Functional probing of the human glucocorticoid receptor steroid-interacting surface by site-directed mutagenesis. Gln-642 plays an important role in steroid recognition and binding.
Published in: J Biol Chem

Ligand: desoximetasone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: yes
Median affinity: 8.930000305175781 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: dexamethasone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1958), EMA (2010)
Primary target: yes
Median affinity:  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)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Functional probing of the human glucocorticoid receptor steroid-interacting surface by site-directed mutagenesis. Gln-642 plays an important role in steroid recognition and binding.
Published in: J Biol Chem

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

Ligand: diflorasone diacetate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: yes
Median affinity: 8.539999961853027 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: difluprednate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2008)
Primary target: yes
Median affinity:  -
Reference (Journal): Pharmacokinetic features of difluprednate ophthalmic emulsion in rabbits as determined by glucocorticoid receptor-binding bioassay.
Published in: J Ocul Pharmacol Ther

Ligand: flunisolide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (prior to1984)
Primary target: yes
Median affinity: 8.619999885559082 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: fluocinolone acetonide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1963)
Primary target: yes
Median affinity: 8.5 pIC50
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: fluocinonide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1971)
Primary target: yes
Median affinity: 8.279999732971191 pIC50
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: fluorometholone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1972)
Primary target: yes
Median affinity: 8.800000190734863 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: fluticasone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1994), EMA (2008)
Primary target: yes
Median affinity:  -

Ligand: fluticasone propionate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity: 8.050000190734863 pEC50
Reference (Journal): Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Published in: J Med Chem

Ligand: fluticasone propionate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Selective plasma hydrolysis of glucocorticoid gamma-lactones and cyclic carbonates by the enzyme paraoxonase: an ideal plasma inactivation mechanism.
Published in: J Med Chem

Ligand: fosdagrocorat (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Patent): Tricyclic compounds, compositions, and methods

Ligand: GSK866 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.5 pIC50
Reference (Journal): The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.
Published in: Bioorg Med Chem Lett

Ligand: LEO 134310 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.849999904632568 pEC50
Reference (Journal): Characterization of a novel non-steroidal glucocorticoid receptor agonist optimized for topical treatment.
Published in: Sci Rep

Ligand: mapracorat (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Journal): Characterization of ZK 245186, a novel, selective glucocorticoid receptor agonist for the topical treatment of inflammatory skin diseases.
Published in: Br J Pharmacol

Ligand: methylprednisolone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1957)
Primary target: yes
Median affinity: 8.300000190734863 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: mifepristone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2000)
Primary target: yes
Median affinity: 9.399999618530273 pKd
Reference (Journal): Plasma concentrations and receptor binding of RU 486 and its metabolites in humans.
Published in: J Steroid Biochem

Ligand: mifepristone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2000)
Primary target: yes
Median affinity: 9.399999618530273 pKd
Reference (Journal): Pharmacological and functional characterization of human mineralocorticoid and glucocorticoid receptor ligands.
Published in: Eur J Pharmacol

Ligand: miricorilant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.100000381469727 pKi
Reference (Journal): Discovery of a novel non-steroidal GR antagonist with in vivo efficacy in the olanzapine-induced weight gain model in the rat.
Published in: Bioorg Med Chem Lett

Ligand: mometasone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: 1987 (FDA)
Primary target: yes
Median affinity:  -

Ligand: onapristone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.570000171661377 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: ORG 214007-0 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.65999984741211 pKi
Reference (Journal): Org 214007-0: a novel non-steroidal selective glucocorticoid receptor modulator with full anti-inflammatory properties and improved therapeutic index.
Published in: PLoS One

Ligand: ORG 214007-0 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.289999961853027 pEC50
Reference (Journal): Org 214007-0: a novel non-steroidal selective glucocorticoid receptor modulator with full anti-inflammatory properties and improved therapeutic index.
Published in: PLoS One

Ligand: ORIC-101 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.25 pIC50
Reference (Journal): Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
Published in: J Med Chem

Ligand: prednisolone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1955)
Primary target: yes
Median affinity: 8.619999885559082 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: prednisolone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1955)
Primary target: yes
Median affinity: 8.149999618530273 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: Full agonist
Ligand approved: yes
Approval source: FDA (1955)
Primary target: yes
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Functional probing of the human glucocorticoid receptor steroid-interacting surface by site-directed mutagenesis. Gln-642 plays an important role in steroid recognition and binding.
Published in: J Biol Chem

Ligand: prednisone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1955)
Primary target: yes
Median affinity: 6.28000020980835 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: RU26988 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: RU28362 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [3H]dexamethasone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -

Ligand: triamcinolone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1957)
Primary target: yes
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Functional probing of the human glucocorticoid receptor steroid-interacting surface by site-directed mutagenesis. Gln-642 plays an important role in steroid recognition and binding.
Published in: J Biol Chem

Ligand: triamcinolone acetonide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2017)
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Species-related differences in steroid-binding specificity of glucocorticoid receptors in lung.
Published in: Endocrinology

Ligand: triamcinolone acetonide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2017)
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Distinction between binding of [3H]triamcinolone acetonide to a ligand binding domain on the glucocorticoid receptor complex in cytosol fractions of brain and liver from the rat with intact adrenals.
Published in: Brain Res

Ligand: vamorolone (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: yes
Approval source: FDA & EMA (2023)
Primary target: yes
Median affinity:  -
Reference (Journal): VBP15, a novel anti-inflammatory and membrane-stabilizer, improves muscular dystrophy without side effects.
Published in: EMBO Mol Med

Ligand: vamorolone (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: yes
Approval source: FDA & EMA (2023)
Primary target: yes
Median affinity:  -
Reference (Journal): VBP15: preclinical characterization of a novel anti-inflammatory delta 9,11 steroid.
Published in: Bioorg Med Chem

Ligand: velsecorat (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.050000190734863 pEC50
Reference (Patent): Phenyl and benzodioxinyl substituted indazoles derivatives

Ligand: velsecorat (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.050000190734863 pEC50
Reference (Journal): Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Published in: J Med Chem

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

Ligand: ZK216348 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.690000057220459 pIC50
Reference (Journal): Dissociation of transactivation from transrepression by a selective glucocorticoid receptor agonist leads to separation of therapeutic effects from side effects.
Published in: Proc Natl Acad Sci USA