Laurie J. Gordon

发表

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.

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.

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

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

6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors.

S. Bromidge, L. Gordon, J. Watson, 2008, Bioorganic & medicinal chemistry letters.

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.

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.

Design and synthesis of novel tricyclic benzoxazines as potent 5-HT(1A/B/D) receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045).

S. Bromidge, J. Watson, A. Worby, 2010, 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.

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 Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.

P. Bamborough, R. Prinjha, C. Chung, 2018, Journal of medicinal chemistry.

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.

Prediction of intracellular exposure bridges the gap between target- and cell-based drug discovery

M. Hann, P. Artursson, B. Seashore-Ludlow, 2017, Proceedings of the National Academy of Sciences.

Optimization of a Series of RIPK2 PROTACs.

Aditya R. Thawani, I. E. Smith, R. Nagilla, 2021, Journal of medicinal chemistry.

Configuration of a High-Content Imaging Platform for Hit Identification and Pharmacological Assessment of JMJD3 Demethylase Enzyme Inhibitors

Melanie Leveridge, Emma Jones, John Liddle, 2012, Journal of biomolecular screening.

Direct Measurement of Intracellular Compound Concentration by RapidFire Mass Spectrometry Offers Insights into Cell Permeability

M. Hann, P. Artursson, A. Mateus, 2016, Journal of biomolecular screening.

The structure based design of dual HDAC/BET inhibitors as novel epigenetic probes

Kathryn A. Giblin, G. Drewes, M. Bantscheff, 2014 .

Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).

David M. Wilson, P. Bamborough, R. Prinjha, 2012, Bioorganic & medicinal chemistry letters.

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.

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.

Cellular Target Engagement Approaches to Monitor Epigenetic Reader Domain Interactions

Aaron T. Cheng, D. J. Brierley, Antonia J Lewis, 2019, SLAS discovery : advancing life sciences R & D.

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.

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

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

Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.

David M. Wilson, P. Bamborough, C. Chung, 2012, Journal of medicinal chemistry.

Development of an intracellular quantitative assay to measure compound binding kinetics.

Kris D. McCombe, Kristin M. Riching, Daniel A. Thomas, 2021, Cell 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.

Pharmacological profile of antipsychotics at monoamine receptors: atypicality beyond 5-HT2A receptor blockade.

C. Davies, C. Scott, G. Riley, 2006, CNS & neurological disorders drug targets.

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.

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.

In vitro and in vivo characterization of the novel GABAB receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2-piperidinyl}ethanol (CMPPE)

A. Capelli, M. Corsi, L. Gordon, 2011, Neuropharmacology.

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.

8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands.

D. Middlemiss, C. Scott, G. W. Price, 2005, Bioorganic & Medicinal Chemistry Letters.

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.

5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3.

A. Capelli, S. Bromidge, A. Worby, 2010, Bioorganic & medicinal chemistry letters.

Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.

Paul W Smith, C. Scott, K. Thewlis, 2008, Journal of medicinal chemistry.

Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.

C. Scott, S. Ward, L. Gordon, 2005, Journal of medicinal chemistry.

SB-649915, a novel, potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor in native tissue.

Christopher J Langmead, Jeannette Watson, C. Langmead, 2006, European journal of pharmacology.