Drug intelligence / Profile preview

Amgen SMARCA2 compound 1

Development stage
Unknown
Lead developer
Amgen
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules
01

Overview

Amgen SMARCA2 compound 1: sourced facts only. name: "Treatment of a cancer cell line with compound 1 resulted in 50% of SMARCA2 being degraded in under 30 minutes, and greater than 90% degradation in 2 hours." [DOI:10.1158/1538-7445.am2024-6567]; target: "Treatment of a cancer cell line with compound 1 resulted in 50% of SMARCA2 being degraded in under 30 minutes, and greater than 90% degradation in 2 hours." [DOI:10.1158/1538-7445.am2024-6567]; developer: "2Amgen, Therapeutic Discovery, Thousand Oaks, CA." [DOI:10.1158/1538-7445.am2024-6567]; modality: "The hetero-bifunctional degraders that resulted from our work trade conventional linkers for chemical spacers that orient SMARCA2 and VHL to promote fortuitous protein-protein contacts in the ternary complex." [DOI:10.1158/1538-7445.am2024-6567]

02

Targets

SMARCA2 (SWI/SNF related, matrix associated, actin dependent regulator of chromatin subfamily A member 2)

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