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

Ligand: APR19 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.239999771118164 pIC50
Reference (Journal): A new strategy for selective targeting of progesterone receptor with passive antagonists.
Published in: Mol Endocrinol

Ligand: asoprisnil (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Discovery of a novel mechanism of steroid receptor antagonism: WAY-255348 modulates progesterone receptor cellular localization and promoter interactions.
Published in: Biochem Pharmacol

Ligand: AZD9567 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.28000020980835 pIC50
Reference (Journal): Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
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: no
Median affinity: 7.150000095367432 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: no
Median affinity: 7.550000190734863 pEC50
Reference (Journal): Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Published in: J Med Chem

Ligand: dydrogesterone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA-no information available-discontinued
Primary target: yes
Median affinity: 6.900000095367432 pKi
Reference (Journal): Selectivity and potency of the retroprogesterone dydrogesterone in vitro.
Published in: Steroids

Ligand: dydrogesterone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA-no information available-discontinued
Primary target: yes
Median affinity: 6.900000095367432 pKi
Reference (Journal): Classification and pharmacology of progestins.
Published in: Maturitas

Ligand: fluticasone propionate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: no
Median affinity: 7.679999828338623 pEC50
Reference (Journal): Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Published in: J Med Chem

Ligand: levonorgestrel (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1990)
Primary target: yes
Median affinity:  -
Reference (Journal): Binding of progestagens to receptor proteins in MCF-7 cells.
Published in: J Steroid Biochem

Ligand: levonorgestrel (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1990)
Primary target: yes
Median affinity:  -
Reference (Journal): Classification and pharmacology of progestins.
Published in: Maturitas

Ligand: medroxyprogesterone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1959)
Primary target: yes
Median affinity: 9.470000267028809 pKi
Reference (Journal): 5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.
Published in: J Med Chem

Ligand: mifepristone (Synthetic organic)
Interaction type: Agonist
Action: Mixed
Ligand approved: yes
Approval source: FDA (2000)
Primary target: no
Median affinity: 8.960000038146973 pKi
Reference (Journal): Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.
Published in: Bioorg Med Chem Lett

Ligand: mifepristone (Synthetic organic)
Interaction type: Antagonist
Action: Mixed
Ligand approved: yes
Approval source: FDA (2000)
Primary target: yes
Median affinity: 8.960000038146973 pKi
Reference (Journal): Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.
Published in: Bioorg Med Chem Lett

Ligand: norethisterone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1973)
Primary target: yes
Median affinity: 8.65999984741211 pEC50
Reference (Journal): 5-Aryl-1,2-dihydro-5H-chromeno[3,4-f]quinolines as potent, orally active, nonsteroidal progesterone receptor agonists: the effect of D-ring substituents.
Published in: J Med Chem

Ligand: onapristone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.74 pKi
Reference (Journal): Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
Published in: J Med Chem

Ligand: ORG2058 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: PF-03882845 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.380000114440918 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: progesterone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1959)
Primary target: yes
Median affinity: 8.460000038146973 pKi
Reference (Journal): 5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.
Published in: J Med Chem

Ligand: progesterone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1959)
Primary target: yes
Median affinity: 8.819999694824219 pEC50
Reference (Journal): Preparation, resolution, and biological evaluation of 5-aryl-1, 2-dihydro-5H-chromeno[3,4-f]quinolines: potent, orally active, nonsteroidal progesterone receptor agonists.
Published in: J Med Chem

Ligand: promegestone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Classification and pharmacology of progestins.
Published in: Maturitas

Ligand: [3H]ORG2058 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -

Ligand: tanaproget (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
Published in: J Med Chem

Ligand: ulipristal acetate (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2009), FDA (2010)
Primary target: yes
Median affinity: 9.699999809265137 pIC50
Reference (Journal): 11-(pyridinylphenyl)steroids--a new class of mixed-profile progesterone agonists/antagonists.
Published in: Bioorg Med Chem

Ligand: ulipristal acetate (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2009), FDA (2010)
Primary target: yes
Median affinity: 7 pEC50
Reference (Journal): 11-(pyridinylphenyl)steroids--a new class of mixed-profile progesterone agonists/antagonists.
Published in: Bioorg Med Chem

Ligand: WAY-255348 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
Published in: J Med Chem

Ligand: WAY-255348 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Discovery of a novel mechanism of steroid receptor antagonism: WAY-255348 modulates progesterone receptor cellular localization and promoter interactions.
Published in: Biochem Pharmacol

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