R. Watson

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.

Navigating CYP1A Induction and Arylhydrocarbon Receptor Agonism in Drug Discovery. A Case History with S1P1 Agonists.

E. Demont, J. Witherington, Simon Taylor, 2015, Journal of medicinal chemistry.

Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.

P. Grandi, I. Wall, James M. Woolven, 2021, 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.

GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.

P. Grandi, P. Bamborough, R. Prinjha, 2020, 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 Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.

S. Dowell, E. Demont, J. Witherington, 2016, Journal of medicinal chemistry.

Isolation and characterisation of the potential immunomodulatory principles from Astragalus membranaceus

R. Watson, Robert J. Watson, 2006 .

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.

Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.

S. Dowell, K. Philpott, T. Heightman, 2011, Journal of medicinal chemistry.

Multigram Synthesis of Tetrasubsituted Dihydrobenzofuran GSK973 Enabled by High-Throughput Experimentation and a Claisen Rearrangement in Flow

Leanna E. Shuster, Chelsea A. Huff, E. Demont, 2022, Organic Process Research & Development.

Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit.

P. Grandi, I. Wall, R. Prinjha, 2021, Journal of medicinal chemistry.

Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.

I. Wall, K. Philpott, T. Heightman, 2014, 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.

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.

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.

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.

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.

Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate.

S. Dowell, E. Demont, J. Witherington, 2011, ACS 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.

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.