D. Mitchell

发表

Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors.

P. Grandi, A. Michon, P. Bamborough, 2015, Journal of medicinal chemistry.

A Chemical Probe for the ATAD2 Bromodomain.

Andrew J. Bannister, S. Robson, P. Grandi, 2016, Angewandte Chemie.

A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification.

P. Grandi, A. Michon, Christina Rau, 2019, Journal of medicinal chemistry.

Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.

P. Grandi, A. Michon, Christina Rau, 2015, Journal of medicinal chemistry.

Identification of a Series of N-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins.

P. Grandi, A. Michon, I. Wall, 2021, Journal of medicinal chemistry.

Modulation of macrophage inflammatory function through selective inhibition of the epigenetic reader protein SP140

D. Zwijnenburg, W. D. de Jonge, R. Prinjha, 2020, bioRxiv.

The Optimisation of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode.

P. Bamborough, R. Prinjha, C. Chung, 2020, Journal of medicinal chemistry.

Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors.

P. Grandi, A. Michon, Christina Rau, 2018, Journal of medicinal chemistry.

1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.

David J. Fallon, P. Grandi, A. Michon, 2014, ACS medicinal chemistry letters.

Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.

A. Muir, G. Sanger, Christopher N. Johnson, 2009, Journal of medicinal chemistry.

Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors.

P. Grandi, I. Wall, James M. Woolven, 2021, Journal of medicinal chemistry.

The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.

Michael A. Briggs, G. Macdonald, G. Sanger, 2008, Bioorganic & medicinal chemistry letters.

Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists.

Michael A. Briggs, S. Bromidge, A. Medhurst, 2005, Bioorganic & medicinal chemistry letters.

Definition of the heterocyclic pharmacophore of bacterial methionyl tRNA synthetase inhibitors: potent antibacterially active non-quinolone analogues.

A. K. Forrest, Murray J. B. Brown, R. Copley, 2004, Bioorganic & medicinal chemistry letters.

The design of 8,8-dimethyl[1,6]naphthyridines as potential anticonvulsant agents.

G. Macdonald, G. Riley, N. Upton, 2003, Bioorganic & medicinal chemistry letters.

The Optimisation of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.

P. Grandi, A. Michon, I. Wall, 2020, Journal of medicinal chemistry.

Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.

R. Prinjha, P. Soden, C. Chung, 2021, Journal of medicinal chemistry.

Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.

Darren L. Poole, Tony W Dean, I. Wall, 2020, Journal of medicinal chemistry.

Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.

G. Stemp, M. Gunthorpe, John B Davis, 2008, Bioorganic & medicinal chemistry letters.

Modulation of macrophage inflammatory function through selective inhibition of the epigenetic reader protein SP140

D. Zwijnenburg, W. D. de Jonge, R. Prinjha, 2022, BMC Biology.

GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.

P. Grandi, A. Michon, I. Wall, 2020, ACS Medicinal Chemistry Letters.

Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.

James M. Woolven, P. Bamborough, R. Prinjha, 2020, Journal of medicinal chemistry.

The Design and Synthesis of a Highly Selective and In Vivo Capable Inhibitor of the Second Bromodomain (BD2) of the Bromodomain and Extra Terminal Domain (BET) Family of Proteins.

P. Grandi, A. Michon, I. Wall, 2020, Journal of medicinal chemistry.

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

David J. Fallon, P. Grandi, A. Michon, 2016, ACS medicinal chemistry letters.

Design and Characterization of 1,3-Dihydro-2H-benzo[d]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors.

P. Bamborough, R. Prinjha, P. Soden, 2023, ACS medicinal chemistry letters.

Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins

P. Grandi, A. Michon, James M. Woolven, 2020, Journal of Medicinal Chemistry.