P. Humphreys

发表

Application of Atypical Acetyl-Lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains.

Melanie V. Leveridge, P. Grandi, A. Michon, 2020, Journal of medicinal chemistry.

Advancements in the Development of non‐BET Bromodomain Chemical Probes

R. Prinjha, Michael A Clegg, N. Tomkinson, 2019, ChemMedChem.

Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach.

Martin C Fillmore, R. Prinjha, N. Galwey, 2018, ACS chemical biology.

Clegg, Michael and Tomkinson, Nicholas C. O. and Prinjah, Rab K. and Humphreys, Philip G. (2017) Small molecules and their roles in effective

R. Prinjha, Michael A Clegg, N. Tomkinson, 2018 .

Small molecules and their role in effective preclinical target validation.

R. Prinjha, Michael A Clegg, N. Tomkinson, 2017, Future medicinal chemistry.

Fragment-Based Identification of Ligands for Bromodomain-Containing Factor 3 of Trypanosoma cruzi.

P. Biggin, D. Hewings, Laura E. Jennings, 2020, ACS infectious diseases.

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition.

Andrew J. Bannister, Melanie V. Leveridge, S. Robson, 2016, Journal of medicinal chemistry.

Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.

Darren L. Poole, I. Wall, P. Bamborough, 2022, 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.

Alkene Syn- and Anti-Oxyamination with Malonoyl Peroxides

A. Kennedy, N. Tomkinson, P. Humphreys, 2020, Organic Letters.

Lithiation-induced migrations from nitrogen to carbon in terminal aziridines.

J. Ward, D. M. Hodgson, P. Humphreys, 2007, Angewandte Chemie.

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives.

David M. Wilson, Melanie V. Leveridge, G. Drewes, 2016, Journal of medicinal chemistry.

Dimerization and Isomerization Reactions of α-Lithiated Terminal Aziridines

J. Ward, S. Miles, D. M. Hodgson, 2007 .

Widening the usefulness of epoxides and aziridines in synthesis

D. M. Hodgson, P. Humphreys, Steven P Hughes, 2007 .

Substituted aziridines by lithiation-electrophile trapping of terminal aziridines.

J. Ward, Philip G Humphreys, D. M. Hodgson, 2005, Organic letters.

Total synthesis of the strychnos alkaloid (+)-minfiensine: tandem enantioselective intramolecular Heck-iminium ion cyclization.

L. Overman, A. Wrobleski, P. Humphreys, 2008, Journal of the American Chemical Society.

The Aza‐Cope/Mannich Reaction

L. Overman, G. Welmaker, P. Humphreys, 2011 .

BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.

P. Biggin, A. Mapp, E. Hammond, 2018, Bioorganic & medicinal chemistry.

Intramolecular cyclopropanation of unsaturated terminal aziridines.

J. Ward, D. M. Hodgson, P. Humphreys, 2006, Organic letters.

Alkene anti-Dihydroxylation with Malonoyl Peroxides.

A. Kennedy, M. Rawling, M. Campbell, 2015, Organic letters.

Interrogating the Druggability of the 2-Oxoglutarate-Dependent Dioxygenase Target Class by Chemical Proteomics.

David M. Wilson, G. Drewes, Markus Boesche, 2016, ACS chemical biology.

Progress in the Development of non‐BET Bromodomain Chemical Probes

R. Prinjha, N. Tomkinson, P. Humphreys, 2016, ChemMedChem.

Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.

P. Grandi, A. Michon, P. Bamborough, 2017, Journal of medicinal chemistry.

Clinical progress and pharmacology of small molecule bromodomain inhibitors.

R. Prinjha, Natalie H Theodoulou, Nicholas Co Tomkinson, 2016, Current opinion in chemical biology.

Optimization of Naphthyridones into Selective TATA-Binding Protein Associated Factor 1 (TAF1) Bromodomain Inhibitors.

P. Bamborough, R. Prinjha, C. Chung, 2021, ACS medicinal chemistry letters.

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives.

Douglas W. Thomson, David M. Wilson, Melanie V. Leveridge, 2016, 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.

Expanding the Utility of Lithiated Epoxides and Aziridines in Synthesis

P. Humphreys, C. D. Bray, D. Hodgson, 2006 .