Physicochemistry of Cereblon Modulating Drugs Determines Pharmacokinetics and Disposition

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

Facts, Patterns and Principles in Drug Discovery: appraising the Rule of 5 with measured physicochemical data.

(2020) Christopher P. Tinworth et al.   JOURNAL OF MEDICINAL CHEMISTRY

Evaluation of iberdomide and cytochrome p450 drug-drug interaction potential in vitro and in a phase 1 study in healthy subjects

(2020) Allison Gaudy et al.   EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY

First‐in‐Human, Single‐ and Multiple‐Ascending‐Dose Studies in Healthy Subjects to Assess Pharmacokinetics, Pharmacodynamics, and Safety/Tolerability of Iberdomide, a Novel Cereblon E3 Ligase Modulator

(2020) Ying Ye et al.   Clinical Pharmacology in Drug Development

Patterns of substrate affinity, competition and degradation kinetics underlie biological activity of thalidomide analogs

(2019) Adam S. Sperling et al.   BLOOD

4‐Aminophthalimide amino acids as small and environment‐sensitive fluorescent probes for transmembrane peptides

(2019) Samantha Wörner et al.   CHEMBIOCHEM

Development of targeted protein degradation therapeutics

(2019) Philip P. Chamberlain et al.   Nature Chemical Biology

Iberdomide (CC-220) is a potent cereblon E3 ligase modulator with antitumor and immunostimulatory activities in lenalidomide- and pomalidomide-resistant multiple myeloma cells with dysregulated CRBN

(2019) Chad C. Bjorklund et al.   LEUKEMIA

Defining the human C2H2 zinc finger degrome targeted by thalidomide analogs through CRBN

(2018) Quinlan L. Sievers et al.   SCIENCE

A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos

(2017) Mary E. Matyskiela et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Small Push–Pull Fluorophore for Turn-on Fluorescence

(2017) Andrea Marie Thooft et al.   JOURNAL OF ORGANIC CHEMISTRY

Intracellular drug bioavailability: a new predictor of system dependent drug disposition

(2017) André Mateus et al.   Scientific Reports

Clinical Pharmacokinetics and Pharmacodynamics of Lenalidomide

(2016) Nianhang Chen et al.   CLINICAL PHARMACOKINETICS

A sensitive and robust HPLC assay with fluorescence detection for the quantification of pomalidomide in human plasma for pharmacokinetic analyses

(2014) Shandiz Shahbazi et al.   JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS

Jaguar: A high-performance quantum chemistry software program with strengths in life and materials sciences

(2013) Art D. Bochevarov et al.   INTERNATIONAL JOURNAL OF QUANTUM CHEMISTRY

Rapid Measurement of Intracellular Unbound Drug Concentrations

(2013) André Mateus et al.   MOLECULAR PHARMACEUTICS

Pomalidomide Shows Significant Therapeutic Activity against CNS Lymphoma with a Major Impact on the Tumor Microenvironment in Murine Models

(2013) Zhimin Li et al.   PLoS One

Pharmacokinetics, metabolism and excretion of [14C]-lenalidomide following oral administration in healthy male subjects

(2011) Nianhang Chen et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Getting physical in drug discovery II: the impact of chromatographic hydrophobicity measurements and aromaticity

(2011) Robert J. Young et al.   DRUG DISCOVERY TODAY

On the Photophysical Properties of New Luminol Derivatives and their Synthetic Phthalimide Precursors

(2010) Raúl Pérez-Ruiz et al.   JOURNAL OF FLUORESCENCE

The effect of plasma protein binding on in vivo efficacy: misconceptions in drug discovery

(2010) Dennis A. Smith et al.   NATURE REVIEWS DRUG DISCOVERY

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE

Physicochemical Determinants of Human Renal Clearance

(2009) Manthena V. S. Varma et al.   JOURNAL OF MEDICINAL CHEMISTRY