GIREDESTRANT

GIREDESTRANT : Antagoinist, Degrader of ESR1

Structure

Information

  • ESR1
  • Antagoinist, Degrader
  • up to 100 nM

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): GDC-9545 was highly selective against a panel of 220 kinases and 23 human nuclear receptors. Also, it showed minimal activity (<20% inhibition at 10 μM) against hNav1.5 and hCav1.2 ion channels. Tested against a secondary pharmacology panel consisting of 42 receptors, ion channels, transporters, and enzymes showed 2 hits for GDC-9545.
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SERP ratings and comments


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