1818885-54-9

1818885-54-9 structure

Name: 2-chloro-4-[trans-3-amino-2,2,4,4-tetramethylcyclobutoxy]benzonitrile
Chemical Name: AR antagonist 1
CAS Number: 1818885-54-9
Molecular Formula: C₁₅H₁₉ClN₂O
Molecular Weight: 278.78
Catalog: Signaling Pathways PROTAC Ligand for E3 Ligase
Create Date: 2020-06-01 15:27:14
Modify Date: 2024-01-13 20:23:49
AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).

Name	AR antagonist 1
Synonyms	MFCD30803693

Description	AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
Related Catalog	Research Areas >> Cancer Signaling Pathways >> PROTAC >> Ligand for E3 Ligase
Target	IC50: androgen receptor[1]
In Vitro	AR antagonist 1 (compound 29) is the ligand for target ligase of ARD-266. ARD-266 is a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. AR antagonist 1 exhibits micromolar binding affinity to its E3 ligase complex, it can be successfully employed for the design of highly potent and efficient PROTAC degraders. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
References	[1]. Han X, et al. Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands. J Med Chem. 2019 Dec 26;62(24):11218-11231.