4ZYI: Discovery Of Nvp-cgm097 - A Highly Potent And Selective Mdm2 Inhibitor Undergoing Phase 1 Clinical Trials In P53wt Tumors: Hdm2 (mdm2) Complexed With Cpd2

As a result of our efforts to discover novel p53:MDM2 protein-protein interaction inhibitors useful for treating cancer, the potent and selective MDM2 inhibitor NVP-CGM097 (1) with an excellent in vivo profile was selected as a clinical candidate and is currently in phase 1 clinical development. This article provides an overview of the discovery of this new clinical p53:MDM2 inhibitor. The following aspects are addressed: mechanism of action, scientific rationale, binding mode, medicinal chemistry, pharmacokinetic and pharmacodynamic properties, and in vivo pharmacology/toxicology in preclinical species.
PDB ID: 4ZYIDownload
MMDB ID: 131323
PDB Deposition Date: 2015/5/21
Updated in MMDB: 2015/09
Experimental Method:
x-ray diffraction
Resolution: 1.67  Å
Similar Structures:
Biological Unit for 4ZYI: monomeric; determined by author and by software (PISA)
Molecular Components in 4ZYI
Label Count Molecule
Protein (1 molecule)
E3 Ubiquitin-protein Ligase Mdm2(Gene symbol: MDM2)
Molecule annotation
Chemicals (2 molecules)
* Click molecule labels to explore molecular sequence information.

Citing MMDB