Androgen Receptor

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

click to view more

Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No. Information Product Use Citations Product Validations
S2840

ARN-509

ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.

S1304

Megestrol Acetate

Megestrol acetate is a synthetic progestogen, used to treat breast cancer and loss of appetite.

S7040

AZD3514

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.

S1174

MK-2866 (GTx-024)

MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.

S1140

Andarine

Andarine is a selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, tissue-selective for anabolic organs. Phase 3.

S4677New

Fluoxymesterone

Fluoxymesterone is an Androgen. The mechanism of action of fluoxymesterone is as an Androgen Receptor Agonist.

S4593New

Chlormadinone acetate

Chlormadinone acetate is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive. Its half-life is about 34-38 hours.

S1250

Enzalutamide (MDV3100)

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.

S1190

Bicalutamide

Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line.

S7955New

EPI-001

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.

S2803

Galeterone

Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.

S1908

Flutamide

Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.

S2604

Dehydroepiandrosterone (DHEA)

Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.

S2042

Cyproterone Acetate

Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.

S4054

Spironolactone

Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.

S7559

ODM-201

ODM-201 is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.

Catalog No. Information Product Use Citations Product Validations
S2840

ARN-509

ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.

S1304

Megestrol Acetate

Megestrol acetate is a synthetic progestogen, used to treat breast cancer and loss of appetite.

S7040

AZD3514

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.

Catalog No. Information Product Use Citations Product Validations
S1250

Enzalutamide (MDV3100)

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.

2015, 10.1093/nar/gkv262

2012, 131(6):E872-83

2013, 182(2):460-73

S1190

Bicalutamide

Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line.

2014, 10.1038/onc.2014.302

2014, 10.1158/1535-7163.MCT-14-0819

2012, 131(6):E872-83

S7955New

EPI-001

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.

S2803

Galeterone

Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.

2016, 477(4):1005-10

S1908

Flutamide

Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.

2014, 10.1158/1535-7163.MCT-14-0819

2016, 104(9):2345-55

S2604

Dehydroepiandrosterone (DHEA)

Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.

S2042

Cyproterone Acetate

Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.

S4054

Spironolactone

Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.

S7559

ODM-201

ODM-201 is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.

Catalog No. Information Product Use Citations Product Validations
S1140

Andarine

Andarine is a selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, tissue-selective for anabolic organs. Phase 3.

2013, 30(9):1517-26

S4677New

Fluoxymesterone

Fluoxymesterone is an Androgen. The mechanism of action of fluoxymesterone is as an Androgen Receptor Agonist.

S4593New

Chlormadinone acetate

Chlormadinone acetate is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive. Its half-life is about 34-38 hours.

Catalog No. Information Product Use Citations Product Validations
S1174

MK-2866 (GTx-024)

MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.

2013, 84:278-84

2011, 3(5):331-6