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PI3K inhibitors are finally coming of age

Nature reviews. Drug discovery, 2021-10, Vol.20 (10), p.741-769

2021

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Scaffold-hopping with zwitterionic CCR3 antagonists: Identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092

Bioorganic & medicinal chemistry letters, 2012-11, Vol.22 (21), p.6694-6699

2012

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Apolipoprotein E modulates glial activation and the endogenous central nervous system inflammatory response

Journal of neuroimmunology, 2001-03, Vol.114 (1), p.107-113

2001

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14-3-3 modulation of the inflammatory response

Pharmacological research, 2021-01, Vol.163, p.105236-105236, Article 105236

2021

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Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases

Journal of medicinal chemistry, 2019-05, Vol.62 (10), p.4783-4814

2019

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The discovery of CCR3/H1 dual antagonists with reduced hERG risk

Bioorganic & medicinal chemistry letters, 2012-11, Vol.22 (21), p.6688-6693

2012

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Designing novel building blocks is an overlooked strategy to improve compound quality

Drug discovery today, 2015-01, Vol.20 (1), p.11-17

2015

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Surprising lipophilicity observations identify unexpected conformational effects

Bioorganic & medicinal chemistry letters, 2022-08, Vol.69, p.128786, Article 128786

2022

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Design, Synthesis, and Biological Evaluation of MEK PROTACs

Journal of medicinal chemistry, 2020-01, Vol.63 (1), p.157-162

2020

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Structural and conformational determinants of macrocycle cell permeability

Nature chemical biology, 2016-12, Vol.12 (12), p.1065-1074

2016

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Stabilization of protein-protein interactions in drug discovery

Expert opinion on drug discovery, 2017-09, Vol.12 (9), p.925-940

2017

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Glucocorticoid receptor Thr524 phosphorylation by MINK1 induces interactions with 14-3-3 protein regulators

The Journal of biological chemistry, 2021-01, Vol.296, p.100551-100551, Article 100551

2021

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A class of highly selective inhibitors bind to an active state of PI3Kγ

Nature chemical biology, 2019-04, Vol.15 (4), p.348-357

2019

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Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3‑Kinase (PI3K)‑γ Inhibitors

Journal of medicinal chemistry, 2018-06, Vol.61 (12), p.5435-5441

2018

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Designing Selective Drug-like Molecular Glues for the Glucocorticoid Receptor/14-3‑3 Protein–Protein Interaction

Journal of medicinal chemistry, 2022-12, Vol.65 (24), p.16818-16828

2022

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Impact of Stereospecific Intramolecular Hydrogen Bonding on Cell Permeability and Physicochemical Properties

Journal of medicinal chemistry, 2014-03, Vol.57 (6), p.2746-2754

2014

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Discovery of AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma

Journal of medicinal chemistry, 2021-06, Vol.64 (12), p.8053-8075

2021

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On the absolute configuration of 1-cyclopropylethan-1-amine

Tetrahedron: asymmetry, 2017-09, Vol.28 (9), p.1135-1138

2017

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Identification of Phosphate-Containing Compounds as New Inhibitors of 14-3-3/c-Abl Protein–Protein Interaction

ACS chemical biology, 2020-04, Vol.15 (4), p.1026-1035

2020

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Spiro-fused Pyrrolidine, Piperidine, and Oxindole Scaffolds from Lactams

Organic letters, 2012-09, Vol.14 (18), p.4846-4849

2012

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One-Pot, Three-Component Copper-Catalysed ‘Click’ Triazole Synthesis Utilising the Inexpensive, Shelf-Stable Diazotransfer Reagent Imidazole-1-sulfonyl Azide Hydrochloride

Synlett, 2009-06, Vol.2009 (9), p.1391-1394

2009

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A Practical Method for Targeted Library Design Balancing Lead-like Properties with Diversity

ChemMedChem, 2009-05, Vol.4 (5), p.800-808

2009

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Apolipoprotein E suppresses glial cell secretion of TNF α

Journal of neuroimmunology, 1997-06, Vol.76 (1), p.70-74

1997

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[3 + 2] cycloaddition reactions of 4-alkyl-3-hydroxy-2H-pyrazolo[4,3-c]isoquinolinium inner salts

Journal of organic chemistry, 2003-10, Vol.68 (22), p.8700-8703

2003

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Neurotrophins affect the pattern of DRG neurite growth in a bioassay that presents a choice of CNS and PNS substrates

Development (Cambridge), 1995-05, Vol.121 (5), p.1301-1309

1995

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PI3K inhibitors are finally coming of age

Scaffold-hopping with zwitterionic CCR3 antagonists: Identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092

Apolipoprotein E modulates glial activation and the endogenous central nervous system inflammatory response

14-3-3 modulation of the inflammatory response

Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases

The discovery of CCR3/H1 dual antagonists with reduced hERG risk

Designing novel building blocks is an overlooked strategy to improve compound quality

Surprising lipophilicity observations identify unexpected conformational effects

Design, Synthesis, and Biological Evaluation of MEK PROTACs

Structural and conformational determinants of macrocycle cell permeability

Stabilization of protein-protein interactions in drug discovery

Glucocorticoid receptor Thr524 phosphorylation by MINK1 induces interactions with 14-3-3 protein regulators

A class of highly selective inhibitors bind to an active state of PI3Kγ

Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3‑Kinase (PI3K)‑γ Inhibitors

Designing Selective Drug-like Molecular Glues for the Glucocorticoid Receptor/14-3‑3 Protein–Protein Interaction

Impact of Stereospecific Intramolecular Hydrogen Bonding on Cell Permeability and Physicochemical Properties

Discovery of AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma

On the absolute configuration of 1-cyclopropylethan-1-amine

Identification of Phosphate-Containing Compounds as New Inhibitors of 14-3-3/c-Abl Protein–Protein Interaction

Spiro-fused Pyrrolidine, Piperidine, and Oxindole Scaffolds from Lactams

One-Pot, Three-Component Copper-Catalysed ‘Click’ Triazole Synthesis Utilising the Inexpensive, Shelf-Stable Diazotransfer Reagent Imidazole-1-sulfonyl Azide Hydrochloride

A Practical Method for Targeted Library Design Balancing Lead-like Properties with Diversity

Apolipoprotein E suppresses glial cell secretion of TNF α

[3 + 2] cycloaddition reactions of 4-alkyl-3-hydroxy-2H-pyrazolo[4,3-c]isoquinolinium inner salts

Neurotrophins affect the pattern of DRG neurite growth in a bioassay that presents a choice of CNS and PNS substrates

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