Kwai-Ming J. Cheung

发表

Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing

Gary Box, Ian Collins, Isaac M. Westwood, 2011, Journal of medicinal chemistry.

Aminopyrazine Inhibitors Binding to an Unusual Inactive Conformation of the Mitotic Kinase Nek2: SAR and Structural Characterization†

Caterina Barillari, Ian Collins, Samantha Burns, 2010, Journal of medicinal chemistry.

Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance.

R. V. van Montfort, P. Workman, A. Faisal, 2015, Cancer research.

Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2022, Journal of medicinal chemistry.

Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2022, Journal of medicinal chemistry.

Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2021, Journal of medicinal chemistry.

Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2022, Scientific Reports.

Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2020, Journal of medicinal chemistry.

Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.

K. Boxall, G. Aherne, R. Bayliss, 2012, Journal of medicinal chemistry.

Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: SAR, structural biology and cellular activity

Swen, K. Boxall, G. Aherne, 2012 .

Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4-d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine (BOS172722)

R. V. van Montfort, A. Faisal, N. Cronin, 2018, Journal of medicinal chemistry.

Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2023, Journal of Medicinal Chemistry.

4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.

Mike Wood, Brian Dymock, Xavier Barril, 2007, Journal of medicinal chemistry.

In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors.

L. Pearl, P. Workman, R. Marais, 2007, Cancer research.

Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).

R. V. van Montfort, K. Boxall, G. Aherne, 2016, Journal of medicinal chemistry.

A RIPK1-specific PROTAC degrader achieves potent antitumor activity by enhancing immunogenic cell death.

V. Roulstone, T. Tenev, S. Hoelder, 2024, Immunity.

Identification of inhibitors of checkpoint kinase 1 through template screening.

R. V. van Montfort, M. Walton, K. Boxall, 2009, Journal of medicinal chemistry.