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Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase

Journal of medicinal chemistry, 2020-09, Vol.63 (18), p.10460-10473

2020

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Discovery of Novel 3‑Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase

Journal of medicinal chemistry, 2016-07, Vol.59 (13), p.6281-6292

2016

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Tricyclic IndazolesA Novel Class of Selective Estrogen Receptor Degrader Antagonists

Journal of medicinal chemistry, 2019-02, Vol.62 (3), p.1593-1608

2019

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Design of rigid protein-protein interaction inhibitors enables targeting of undruggable Mcl-1

Proceedings of the National Academy of Sciences - PNAS, 2023-05, Vol.120 (21), p.e2221967120-e2221967120

2023

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Discovery and characterisation of quinazolines and 8-Azaquinazolines as NLRP3 agonists with oral bioavailability in mice

Bioorganic & medicinal chemistry letters, 2023-11, Vol.96, p.129518-129518, Article 129518

2023

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Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2‑(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor‑1 Receptor (IGF-1R)

Journal of medicinal chemistry, 2016-05, Vol.59 (10), p.4859-4866

2016

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Identification and optimisation of a pyrimidopyridone series of IRAK4 inhibitors

Bioorganic & medicinal chemistry, 2022-06, Vol.63, p.116729-116729, Article 116729

2022

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Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors

Bioorganic & medicinal chemistry, 2020-12, Vol.28 (23), p.115815-115815, Article 115815

2020

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Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4

Bioorganic & medicinal chemistry, 2018-02, Vol.26 (4), p.913-924

2018

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Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat

ACS medicinal chemistry letters, 2016-01, Vol.7 (1), p.94-99

2016

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Lowering Lipophilicity by Adding Carbon: One-Carbon Bridges of Morpholines and Piperazines

Journal of medicinal chemistry, 2018-10, Vol.61 (19), p.8934-8943

2018

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Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}- N -methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs

Journal of medicinal chemistry, 2021-10, Vol.64 (19), p.14498-14512

2021

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Investigation of (E)‑3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

Journal of medicinal chemistry, 2015-04, Vol.58 (8), p.3522-3533

2015

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Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3

Journal of medicinal chemistry, 2015-04, Vol.58 (8), p.3611-3625

2015

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Discovery of a Series of 5‑Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88L265P Mutant Diffuse Large B Cell Lymphoma

Journal of medicinal chemistry, 2019-11, Vol.62 (21), p.9918-9930

2019

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Lowering Lipophilicity by Adding Carbon: AzaSpiroHeptanes, a logD Lowering Twist

ACS medicinal chemistry letters, 2019-08, Vol.10 (8), p.1198-1204

2019

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Correction to Discovery of Novel 3‑Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase

Journal of medicinal chemistry, 2018-07, Vol.61 (14), p.6398-6398

2018

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Compound Passport Service: supporting corporate collection owners in open innovation

Drug discovery today, 2015-10, Vol.20 (10), p.1250-1255

2015

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Correction to Investigation of (E)‑3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

Journal of medicinal chemistry, 2016-04, Vol.59 (7), p.3576-3576

2016

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Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin‑1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B‑Cell Lymphoma

Journal of medicinal chemistry, 2017-12, Vol.60 (24), p.10071-10091

2017

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Lowering Lipophilicity by Adding Carbon: AzaSpiroHeptanes, a log D Lowering Twist

ACS medicinal chemistry letters, 2019-08, Vol.10 (8), p.1198-1204

2019

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Synthesis of novel, functionalised tricycles utilising the interrupted Pummerer reaction

Tetrahedron letters, 2016-01, Vol.57 (1), p.152-154

2016

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Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase

Discovery of Novel 3‑Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase

Tricyclic IndazolesA Novel Class of Selective Estrogen Receptor Degrader Antagonists

Design of rigid protein-protein interaction inhibitors enables targeting of undruggable Mcl-1

Discovery and characterisation of quinazolines and 8-Azaquinazolines as NLRP3 agonists with oral bioavailability in mice

Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2‑(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor‑1 Receptor (IGF-1R)

Identification and optimisation of a pyrimidopyridone series of IRAK4 inhibitors

Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors

Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4

Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat

Lowering Lipophilicity by Adding Carbon: One-Carbon Bridges of Morpholines and Piperazines

The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro‑2H‑pyran-4-yl)-1,3-dihydro‑2H‑imidazo[4,5‑c]quinolin-2-one)

Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}- N -methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs

The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one)

Orally Bioavailable and Blood-Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice

Investigation of (E)‑3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3

Discovery of a Series of 5‑Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88L265P Mutant Diffuse Large B Cell Lymphoma

Lowering Lipophilicity by Adding Carbon: AzaSpiroHeptanes, a logD Lowering Twist

Correction to Discovery of Novel 3‑Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase

Compound Passport Service: supporting corporate collection owners in open innovation

Correction to Investigation of (E)‑3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin‑1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B‑Cell Lymphoma

Lowering Lipophilicity by Adding Carbon: AzaSpiroHeptanes, a log D Lowering Twist

Synthesis of novel, functionalised tricycles utilising the interrupted Pummerer reaction

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