AMG232

AMG232 : Competitive inhibitor of MDM2-p53 interaction

Structure

Information

  • MDM2
  • Antagonist, Competitive inhibitor of MDM2-p53 interaction
  • 10-100 nM

In Vitro Validations

Uniprot ID: Q00987
Target Class: Other post-translational modification
Target SubClass: E3 ubiquitin ligase
Potency: Kd
Potency Value: 0.045 nM
Potency Assay: Surface plasmon resonance assay
PDB ID for probe-target interaction (3D structure): 4OAS
Structure-activity relationship: Yes, see J Med Chem paper
Target aliases:
E3 ubiquitin-protein ligase Mdm2, MDM2, MDM2_HUMAN ...

DOI Reference: 10.1021/jm401753e

Uniprot ID: Q00987
Target Class: Other post-translational modification
Target SubClass: E3 ubiquitin ligase
Potency: IC50
Potency Value: 0.6 nM
Potency Assay: HTRF assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
E3 ubiquitin-protein ligase Mdm2, MDM2, MDM2_HUMAN ...

DOI Reference: 10.1021/jm401753e

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

AMG232 showed minimal activity in CYP3A4-inhibition assay and PXR-induction assay.

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This is a potent, competitive inhibitor of the p53-MDM2 interaction. It has been demonstrated to interrupt p53 binding to MDM2 and induce death in SJSA-1 osteosarcoma cells in a p53-dependent manner. It induces p21 expression in SJSA-1 mouse xenograft and is orally available with favorable PK properties. 

(last updated: 24 Jul 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 28 Jul 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 11 Nov 2020 )