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

Ligand: andarine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pKi
Reference (Journal): Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.
Published in: J Med Chem

Ligand: androstenedione (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.56 pIC50
Reference (Journal): Study of 202 natural, synthetic, and environmental chemicals for binding to the androgen receptor.
Published in: Chem Res Toxicol

Ligand: apalutamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2018), EMA (2019)
Primary target: yes
Median affinity: 6.909999847412109 pIC50
Reference (Journal): Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC).
Published in: J Med Chem

Ligand: apalutamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2018), EMA (2019)
Primary target: no
Median affinity: 7.03000020980835 pKi
Reference (Journal): Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies.
Published in: Sci Rep

Ligand: apalutamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2018), EMA (2019)
Primary target: yes
Median affinity: 6.699999809265137 pIC50
Reference (Journal): Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies.
Published in: Sci Rep

Ligand: ARD-266 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands.
Published in: J Med Chem

Ligand: ARD-69 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.230000019073486 pIC50
Reference (Journal): Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.
Published in: J Med Chem

Ligand: bicalutamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: yes
Median affinity: 6 pIC50
Reference (Journal): Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC).
Published in: J Med Chem

Ligand: bicalutamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: yes
Median affinity: 7.71999979019165 pKi
Reference (Journal): (+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
Published in: J Med Chem

Ligand: bisphenol A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.230000019073486 pIC50
Reference (Journal): Structure-activity relationships of bisphenol A analogs at estrogen receptors (ERs): discovery of an ERα-selective antagonist.
Published in: Bioorg Med Chem Lett

Ligand: clascoterone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2020)
Primary target: yes
Median affinity: 7.400000095367432 pKi
Reference (Journal): A full conformational characterization of antiandrogen cortexolone-17-propionate and related compounds through theoretical calculations and nuclear magnetic resonance spectroscopy
Published in: MedChemComm

Ligand: cyproterone acetate (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity: 7.849999904632568 pKi
Reference (Journal): Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.
Published in: J Med Chem

Ligand: danazol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1976)
Primary target: yes
Median affinity: 8 pKi
Reference (Journal): Danazol binding and translocation of steroid receptors.
Published in: Am J Obstet Gynecol

Ligand: darolutamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2019), EMA (2020)
Primary target: yes
Median affinity: 7.590000152587891 pIC50
Reference (Journal): Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies.
Published in: Sci Rep

Ligand: darolutamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2019), EMA (2020)
Primary target: no
Median affinity: 7.960000038146973 pKi
Reference (Journal): Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies.
Published in: Sci Rep

Ligand: dihydrotestosterone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.3 pKd
Reference (Journal): Characterization and expression of a cDNA encoding the human androgen receptor.
Published in: Proc Natl Acad Sci USA

Ligand: dihydrotestosterone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.65 pIC50
Reference (Journal): Study of 202 natural, synthetic, and environmental chemicals for binding to the androgen receptor.
Published in: Chem Res Toxicol

Ligand: dromostanolone propionate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: yes
Median affinity:  -

Ligand: enzalutamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2012), EMA (2013)
Primary target: yes
Median affinity: 7.440000057220459 pIC50
Reference (Journal): Development of a second-generation antiandrogen for treatment of advanced prostate cancer.
Published in: Science

Ligand: enzalutamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2012), EMA (2013)
Primary target: yes
Median affinity: 6.659999847412109 pIC50
Reference (Journal): Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies.
Published in: Sci Rep

Ligand: enzalutamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2012), EMA (2013)
Primary target: no
Median affinity: 7.070000171661377 pKi
Reference (Journal): Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies.
Published in: Sci Rep

Ligand: ethylestrenol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1964)
Primary target: yes
Median affinity:  -

Ligand: fluoxymesterone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1956)
Primary target: yes
Median affinity: 8.239999771118164 pKi
Reference (Journal): Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
Published in: J Med Chem