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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

Summary for 4ZYI
Entry DOI10.2210/pdb4zyi/pdb
DescriptorE3 ubiquitin-protein ligase Mdm2, (S)-7-((R)-sec-butoxy)-1-(4-chlorophenyl)-6-methoxy-2-(4-(methyl(pyridin-4-ylmethyl)amino)phenyl)-1,2-dihydroisoquinolin-3(4H)-one, CHLORIDE ION, ... (4 entities in total)
Functional Keywordsppi with p53, inhibitor complex, cell cycle
Biological sourceHomo sapiens (Human)
Cellular locationNucleus, nucleoplasm: Q00987
Total number of polymer chains1
Total formula weight11747.60
Authors
Kallen, J. (deposition date: 2015-05-21, release date: 2015-07-29, Last modification date: 2024-01-10)
Primary citationHolzer, P.,Masuya, K.,Furet, P.,Kallen, J.,Valat-Stachyra, T.,Ferretti, S.,Berghausen, J.,Bouisset-Leonard, M.,Buschmann, N.,Pissot-Soldermann, C.,Rynn, C.,Ruetz, S.,Stutz, S.,Chene, P.,Jeay, S.,Gessier, F.
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
J.Med.Chem., 58:6348-6358, 2015
Cited by
PubMed: 26181851
DOI: 10.1021/acs.jmedchem.5b00810
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (1.67 Å)
Structure validation

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