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Approval Year

Substance Class Protein
Created
by admin
on Sat Dec 16 12:14:09 UTC 2023
Edited
by admin
on Sat Dec 16 12:14:09 UTC 2023
Protein Sub Type
Sequence Type COMPLETE
Record UNII
EJC4C3UYXH
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ANDROGEN RECEPTOR
Common Name English
AR
Common Name English
DHTR
Common Name English
NR3C4
Common Name English
NUCLEAR RECEPTOR SUBFAMILY 3 GROUP C MEMBER 4
Common Name English
DIHYDROTESTOSTERONE RECEPTOR
Common Name English
Classification Tree Code System Code
DRUG TARGET ONTOLOGY DTO_00117516
Created by admin on Sat Dec 16 12:14:12 UTC 2023 , Edited by admin on Sat Dec 16 12:14:12 UTC 2023
Code System Code Type Description
UNIPROT
P10275
Created by admin on Sat Dec 16 12:14:12 UTC 2023 , Edited by admin on Sat Dec 16 12:14:12 UTC 2023
PRIMARY
FDA UNII
EJC4C3UYXH
Created by admin on Sat Dec 16 12:14:12 UTC 2023 , Edited by admin on Sat Dec 16 12:14:12 UTC 2023
PRIMARY
Related Record Type Details
INHIBITOR -> TARGET
BINDING
Ki
AGONIST -> TARGET
Fluoxymesterone is an Androgen. The mechanism of action of fluoxymesterone is as an Androgen Receptor Agonist
ANTAGONIST
IC50
INHIBITOR -> TARGET
BINDING
IC50
AGONIST -> TARGET
INHIBITOR -> TARGET
ANTAGONIST
AGONIST -> TARGET
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.
ANTAGONIST
IC50
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
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
ANTAGONIST
IC50
INHIBITOR -> TARGET
INHIBITOR -> TARGET
an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.
ANTAGONIST
IC50
AGONIST -> TARGET
Andarine is a selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, tissue-selective for anabolic organs. Phase 3
ANTAGONIST
IC50
AGONIST -> TARGET
MODULATOR->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
DEGRADER, SELECTIVE->TARGET
ARD-69 is a potent proteolysis-targeting chimera (PROTAC) degrader of the androgen receptor (AR) that was designed as a proof-of-concept lead to evaluate the potential of PROTAC technology as a novel treatment mechanism for AR-positive, castration-resistant prostate cancer [2]. It contains an AR antagonist (reported in [1]) that binds the AR, joined by a small linker molecule to a second ligand (in this case a VHL ligand) that engages the E3 ubiquitin ligase system via Cullin-2. This chimeric molecular structure targets AR protein for ubiquitination-dependent proteolysis.
DEGRADER, SELECTIVE->TARGET
In VCaP cells
DC50
AGONIST -> TARGET
BINDING
IC50
AGONIST -> TARGET
INHIBITOR -> TARGET
ANTAGONIST
PARTIAL ANTAGONIST->TARGET
BINDING
IC50
AGONIST -> TARGET
AGONIST -> TARGET
RADIOLIGAND->TARGET
Kd
INHIBITOR -> TARGET
INHIBITOR -> TARGET
Bicalutamide Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line
ANTAGONIST
IC50
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
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
ANTAGONIST
IC50
AGONIST -> TARGET
INHIBITOR -> TARGET
Ki
INHIBITOR -> TARGET
INHIBITOR -> TARGET
BINDING
Ki
AGONIST -> TARGET
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.
ANTAGONIST
IC50
AGONIST -> TARGET
BINDING
IC50
INHIBITOR -> TARGET
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
ANTAGONIST
IC50
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist
ANTAGONIST
IC50
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
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.
ANTAGONIST
IC50
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR OF EXPRESSION->TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
IN-VIVO
INHIBITOR -> TARGET
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT CHEMICAL
Molecular Formula CHEMICAL