Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 16 12:14:09 GMT 2023
by
admin
on
Sat Dec 16 12:14:09 GMT 2023
|
| Protein Sub Type | |
| Sequence Type | COMPLETE |
| Record UNII |
EJC4C3UYXH
|
| Record Status |
Validated (UNII)
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| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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DRUG TARGET ONTOLOGY |
DTO_00117516
Created by
admin on Sat Dec 16 12:14:12 GMT 2023 , Edited by admin on Sat Dec 16 12:14:12 GMT 2023
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| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
P10275
Created by
admin on Sat Dec 16 12:14:12 GMT 2023 , Edited by admin on Sat Dec 16 12:14:12 GMT 2023
|
PRIMARY | |||
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EJC4C3UYXH
Created by
admin on Sat Dec 16 12:14:12 GMT 2023 , Edited by admin on Sat Dec 16 12:14:12 GMT 2023
|
PRIMARY |
| Linkage Type | Residue Index | |||
|---|---|---|---|---|
| COORDINATION COMPOUND | 1_596 | 1_602 | 1_612 | 1_615 |
| COORDINATION COMPOUND | 1_560 | 1_563 | 1_577 | 1_580 |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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INHIBITOR -> TARGET |
BINDING
Ki
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AGONIST -> TARGET |
Fluoxymesterone is an Androgen. The mechanism of action of fluoxymesterone is as an Androgen Receptor Agonist
ANTAGONIST
IC50
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INHIBITOR -> TARGET |
BINDING
IC50
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
ANTAGONIST
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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
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
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INHIBITOR -> TARGET | |||
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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
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.
ANTAGONIST
IC50
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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
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AGONIST -> TARGET |
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MODULATOR->TARGET |
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AGONIST -> TARGET |
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AGONIST -> TARGET |
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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.
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DEGRADER, SELECTIVE->TARGET |
In VCaP cells
DC50
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AGONIST -> TARGET |
BINDING
IC50
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET |
ANTAGONIST
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PARTIAL ANTAGONIST->TARGET |
BINDING
IC50
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AGONIST -> TARGET |
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AGONIST -> TARGET |
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RADIOLIGAND->TARGET |
Kd
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INHIBITOR -> TARGET | |||
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INHIBITOR -> TARGET |
Bicalutamide
Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line
ANTAGONIST
IC50
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
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AGONIST -> TARGET |
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
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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
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET |
Ki
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
BINDING
Ki
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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
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AGONIST -> TARGET |
BINDING
IC50
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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
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET |
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AGONIST -> TARGET |
Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist
ANTAGONIST
IC50
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
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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
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AGONIST -> TARGET |
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INHIBITOR -> TARGET | |||
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INHIBITOR -> TARGET |
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AGONIST -> TARGET |
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INHIBITOR -> TARGET | |||
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INHIBITOR OF EXPRESSION->TARGET | |||
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
IN-VIVO
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INHIBITOR -> TARGET |
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| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT | CHEMICAL |
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| Molecular Formula | CHEMICAL |
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