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

Ligand: flutamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: yes
Median affinity: 5.429999828338623 pKi
Reference (Journal): 4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor.
Published in: Bioorg Med Chem

Ligand: galeterone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.420000076293945 pIC50
Reference (Journal): Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.
Published in: J Med Chem

Ligand: GSK2881078 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pEC50
Reference (Journal): Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay.
Published in: J Steroid Biochem Mol Biol

Ligand: hydroxyflutamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pEC50
Reference (Journal): Androgen antagonistic effect of estramustine phosphate (EMP) metabolites on wild-type and mutated androgen receptor.
Published in: Biochem Pharmacol

Ligand: JNJ-63576253 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.429999828338623 pIC50
Reference (Journal): Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).
Published in: J Med Chem

Ligand: JNJ-63576253 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.269999980926514 pIC50
Reference (Journal): Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).
Published in: J Med Chem

Ligand: methyltestosterone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.65999984741211 pEC50
Reference (Journal): A novel selective androgen receptor modulator, NEP28, is efficacious in muscle and brain without serious side effects on prostate.
Published in: Eur J Pharmacol

Ligand: methyltrienolone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.510000228881836 pIC50
Reference (Journal): Study of 202 natural, synthetic, and environmental chemicals for binding to the androgen receptor.
Published in: Chem Res Toxicol

Ligand: methyltrienolone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Androgen antagonistic effect of estramustine phosphate (EMP) metabolites on wild-type and mutated androgen receptor.
Published in: Biochem Pharmacol

Ligand: mibolerone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.960000038146973 pIC50
Reference (Journal): Preserved male fertility despite decreased androgen sensitivity caused by a mutation in the ligand-binding domain of the androgen receptor gene.
Published in: J Clin Endocrinol Metab

Ligand: mibolerone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pIC50
Reference (Journal): Study of 202 natural, synthetic, and environmental chemicals for binding to the androgen receptor.
Published in: Chem Res Toxicol

Ligand: mifepristone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2000)
Median affinity: 9.19 pKi
Reference (Journal): Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
Published in: J Med Chem

Ligand: nandrolone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1959)
Primary target: yes
Median affinity:  -

Ligand: nilutamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Comparison of in vitro effects of the pure antiandrogens OH-flutamide, Casodex, and nilutamide on androgen-sensitive parameters.
Published in: Urology

Ligand: PF-03882845 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.050000190734863 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: PF0998425 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.
Published in: J Med Chem

Ligand: pruxelutamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.489999771118164 pIC50
Reference (Journal): Preclinical profile and phase I clinical trial of a novel androgen receptor antagonist GT0918 in castration-resistant prostate cancer.
Published in: Eur J Cancer

Ligand: stanozolol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1962)
Primary target: no
Median affinity: 7.659999847412109 pIC50
Reference (Webpage): DrugMatrix in vitro pharmacology data

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

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

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

Ligand: testosterone (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1953)
Median affinity: 7.8 pIC50
Reference (Journal): Study of 202 natural, synthetic, and environmental chemicals for binding to the androgen receptor.
Published in: Chem Res Toxicol

Ligand: testosterone propionate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: yes
Median affinity: 9.600000381469727 pKi
Reference (Journal): Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators.
Published in: Bioorg Med Chem Lett