43 articles for thisTarget
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Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex.

University of Cambridge
Fragment-Based Approaches to the Development of Mycobacterium tuberculosis CYP121 Inhibitors.

University of Cambridge
Synthesis and Initial in Vivo Studies with [(11)C]SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3.

University of Cambridge
Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists.

University of Cambridge
Is NMR Fragment Screening Fine-Tuned to Assess Druggability of Protein-Protein Interactions?

University of Cambridge
Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release.

University of Cambridge
Synthesis of an array of potential matrix metalloproteinase inhibitors using a sequence of polymer-supported reagents.

University of Cambridge
Synthetic partial agonists reveal key steps in IP3 receptor activation.

University of Cambridge
Proposed structural basis of interaction of piperine and related compounds with monoamine oxidases.

University of Cambridge
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.

University of Cambridge
Selective Aurora A-TPX2 Interaction Inhibitors Have In Vivo Efficacy as Targeted Antimitotic Agents.

University of Cambridge
Hit-to-Lead Optimization of Heterocyclic Carbonyloxycarboximidamides as Selective Antagonists at Human Adenosine A3 Receptor.

University of Cambridge
Evaluation of ketoclomazone and its analogues as inhibitors of 1-deoxy-d-xylulose 5-phosphate synthases and other thiamine diphosphate (ThDP)-dependent enzymes.

University of Cambridge
Thiamine analogues featuring amino-oxetanes as potent and selective inhibitors of pyruvate dehydrogenase.

University of Cambridge
The rational design of ARUK2007145, a dual inhibitor of the α and γ isoforms of the lipid kinase phosphatidylinositol 5-phosphate 4-kinase (PI5P4K).

University of Cambridge
Deconvoluting low yield from weak potency in direct-to-biology workflows with machine learning.

University of Cambridge
Identification of macrocyclic peptides which activate bacterial cylindrical proteases.

University of Cambridge
The Identification of Potent, Selective, and Brain Penetrant PI5P4Kγ Inhibitors as In Vivo-Ready Tool Molecules.

University of Cambridge
Identification of ARUK2002821 as an isoform-selective PI5P4Kα inhibitor.

University of Cambridge
Inhibition of Thiamine Diphosphate-Dependent Enzymes by Triazole-Based Thiamine Analogues.

University of Cambridge
Novel structural features of CDK inhibition revealed by an ab initio computational method combined with dynamic simulations.

University of Cambridge
Discovery of a High Affinity Adenosine A

University of Cambridge
A fragment-based approach leading to the discovery of inhibitors of CK2α with a novel mechanism of action.

University of Cambridge
Thiamine analogues as inhibitors of pyruvate dehydrogenase and discovery of a thiamine analogue with non-thiamine related antiplasmodial activity.

University of Cambridge
Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode.

University of Cambridge
Proposed Allosteric Inhibitors Bind to the ATP Site of CK2α.

University of Cambridge
Fragment-Based Design of

University of Cambridge
Inhibition of human telomerase by PNA-cationic peptide conjugates.

University of Cambridge
Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain.

University of Cambridge
Rational approaches to improving selectivity in drug design.

University of Cambridge
Structure-based design of allosteric calpain-1 inhibitors populating a novel bioactivity space.

University of Cambridge
Novel non-ATP competitive small molecules targeting the CK2 α/β interface.

University of Cambridge
A fragment-based approach leading to the discovery of a novel binding site and the selective CK2 inhibitor CAM4066.

University of Cambridge
1-(triazin-3-yl/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions therefor for inhibiting the activity of SHP2

Novartis
Kallikrein 7 inhibitors

Sixera Pharma
Bicyclic inhibitors

Kalvista Pharmaceuticals
Selective androgen receptor modulators

Radius Health
Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors

Merck Sharp & Dohme
Pyranonaphthoquinone lactones: a new class of AKT selective kinase inhibitors alkylate a regulatory loop cysteine.

Wyeth Research
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2.

Gnf
Structural insights into the design of nonpeptidic isothiazolidinone-containing inhibitors of protein-tyrosine phosphatase 1B.

Incyte