Discovery of RG7388, a Potent and Selective p53–MDM2 Inhibitor in Clinical Development

Qingjie Ding, Zhuming Zhang, Jinjun Liu, +14

Journal of Medicinal Chemistry

Drug TargetChemical BiologyCancer BiologyPharmaceutical ChemistryP53 Activity +17

Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

Binh Thanh Vu, Peter M. Wovkulich, Giacomo Pizzolato, +11

ACS Medicinal Chemistry Letters

Drug TargetCell DeathSmall-molecule Mdm2 InhibitorTumor BiologyP53 Activity +15

Preclinical Profile of a Potent γ-Secretase Inhibitor Targeting Notch Signaling with <i>In vivo</i> Efficacy and Pharmacodynamic Properties

Leopoldo Luistro, Wei He, Melissa Smith, +14

Cancer Research

Ro4929097 Ic50Cancer BiologyTumor BiologyMolecular PharmacologyPharmacodynamic Properties +15

Positive allosteric modulation of GABAA receptors by a novel antiepileptic drug cenobamate

Ramesh Sharma, Michiko Nakamura, Chiranjivi Neupane, +6

European Journal of Pharmacology

Molecular PharmacologyPositive Allosteric ModulationNeuromodulation (Medicine)Functional SelectivityMedicine +4

Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development

Zhuming Zhang, Xin‐Jie Chu, Jinjun Liu, +13

ACS Medicinal Chemistry Letters

Medicinal ChemistryPharmaceutical ChemistryChemoprevention StrategyPotential Clinical DevelopmentMedicine +12

Activation of p53 by the MDM2 inhibitor RG7112 impairs thrombopoiesis

Camelia Iancu‐Rubin, Goar Mosoyan, Kelli Glenn, +2

Experimental Hematology

InflammationThrombosisThrombopoiesisBlood PlateletMedicine +5

Preclinical Optimization of MDM2 Antagonist Scheduling for Cancer Treatment by Using a Model-Based Approach

Brian Higgins, Kelli Glenn, Antje‐Christine Walz, +13

Clinical Cancer Research

Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy

Zhuming Zhang, Qingjie Ding, Jinjun Liu, +13

Bioorganic & Medicinal Chemistry

Cancer TherapyMedicinal ChemistryOncologyMedicineRational Drug Design +7

Pyrido[2,3-d]pyrimidines: Discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors

K. Anderson, Yi Chen, Zhi Chen, +15

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryDrug TargetNovel SeriesBiochemistryPreliminary Sar +9

Effect of cenobamate on the single‐dose pharmacokinetics of multiple cytochrome P450 probes using a cocktail approach in healthy subjects

Stephen A. Greene, Charles Kwak, Marc Kamin, +4

Clinical and Translational Science