54 articles for P Bamborough
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.
Glaxosmithkline
Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.
Glaxosmithkline
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.
Glaxosmithkline
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors.
Glaxosmithkline
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.
Glaxosmithkline
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Glaxosmithkline
Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.
Glaxosmithkline
p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.
Glaxosmithkline
3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-ß.
Glaxosmithkline
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.
Glaxosmithkline
Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).
Glaxosmithkline
Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.
Glaxosmithkline
4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.
Glaxosmithkline
Discovery and characterization of small molecule inhibitors of the BET family bromodomains.
Glaxosmithkline
The discovery and initial optimisation of pyrrole-2-carboxamides as inhibitors of p38alpha MAP kinase.
Glaxosmithkline
Potent small molecule inhibitors of spleen tyrosine kinase (Syk).
Aventis Pharmaceuticals
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.
Glaxosmithkline
Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery.
Glaxosmithkline
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.
Glaxosmithkline
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.
Glaxosmithkline
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.
Glaxosmithkline
Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease.
University of Dundee
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.
Gsk
Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate.
Glaxosmithkline R&D
Investigation of Janus Kinase (JAK) Inhibitors for Lung Delivery and the Importance of Aldehyde Oxidase Metabolism.
Gsk
Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Glaxosmithkline
Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Glaxosmithkline
Optimization of Naphthyridones into Selective TATA-Binding Protein Associated Factor 1 (TAF1) Bromodomain Inhibitors.
Glaxosmithkline R&D
GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.
Glaxosmithkline
Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition.
Glaxosmithkline R&D
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.
Gsk
The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.
Glaxosmithkline
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.
Glaxosmithkline Medicines Research Centre
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.
Glaxosmithkline R&D
Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.
Gsk
Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode.
University of Strathclyde
3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent.
Glaxosmithkline
A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification.
Cellzome
Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors.
Glaxosmithkline
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
University of Strathclyde
Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors.
Neurodegeneration Dpu
1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors
Angelini Acraf
Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors.
Merck Research Laboratories
Suzuki-type Pd(0) coupling reactions in the synthesis of 2-arylpurines as Cdk inhibitors.
Institut Curie