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Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases

Journal of medicinal chemistry, 2020-08, Vol.63 (15), p.7957-7985

2020

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Monomeric Targeted Protein Degraders

Journal of medicinal chemistry, 2020-10, Vol.63 (20), p.11330-11361

2020

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Heterobifunctional Molecules Induce Dephosphorylation of Kinases–A Proof of Concept Study

Journal of medicinal chemistry, 2020-03, Vol.63 (6), p.2807-2813

2020

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Overcoming Preclinical Safety Obstacles to Discover (S)‑N‑((1,2,3,5,6,7-Hexahydro‑s‑indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro‑5H‑pyrazolo[5,1‑b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor

Journal of medicinal chemistry, 2022-11, Vol.65 (21), p.14721-14739

2022

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Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα)

Bioorganic & medicinal chemistry letters, 2020-02, Vol.30 (4), p.126907, Article 126907

2020

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Discovery of 2‑{3-[2-(1-Isopropyl-3-methyl‑1H‑1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl]‑1H‑pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β‑Sparing Phosphoinositide 3‑Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity

Journal of medicinal chemistry, 2013-06, Vol.56 (11), p.4597-4610

2013

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Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability

Journal of medicinal chemistry, 2019-08, Vol.62 (15), p.7032-7041

2019

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The Rational Design of Selective Benzoxazepin Inhibitors of the α‑Isoform of Phosphoinositide 3‑Kinase Culminating in the Identification of (S)‑2-((2-(1-Isopropyl‑1H‑1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326)

Journal of medicinal chemistry, 2016-02, Vol.59 (3), p.985-1002

2016

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Structure-Based Design of Potent, Selective, and Orally Bioavailable VPS34 Kinase Inhibitors

Journal of medicinal chemistry, 2022-09, Vol.65 (17), p.11500-11512

2022

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Filling a nick in NIK: Extending the half-life of a NIK inhibitor through structure-based drug design

Bioorganic & medicinal chemistry letters, 2023-06, Vol.89, p.129277-129277, Article 129277

2023

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Back Pocket Flexibility Provides Group II p21-Activated Kinase (PAK) Selectivity for Type I 1/2 Kinase Inhibitors

Journal of medicinal chemistry, 2014-02, Vol.57 (3), p.1033-1045

2014

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Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform

Journal of medicinal chemistry, 2011-11, Vol.54 (22), p.7815-7833

2011

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Structure Based Design of Potent Selective Inhibitors of Protein Kinase D1 (PKD1)

ACS medicinal chemistry letters, 2019-09, Vol.10 (9), p.1260-1265

2019

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Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles

ACS medicinal chemistry letters, 2017-09, Vol.8 (9), p.936-940

2017

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Cis-Amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase

Bioorganic & medicinal chemistry letters, 2013-02, Vol.23 (3), p.897-901

2013

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Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform

Bioorganic & medicinal chemistry letters, 2013-05, Vol.23 (9), p.2606-2613

2013

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Structure-based design of thienobenzoxepin inhibitors of PI3-kinase

Bioorganic & medicinal chemistry letters, 2011-07, Vol.21 (13), p.4054-4058

2011

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Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase

Bioorganic & medicinal chemistry letters, 2010-10, Vol.20 (20), p.6048-6051

2010

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Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties

Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases

Monomeric Targeted Protein Degraders

Heterobifunctional Molecules Induce Dephosphorylation of Kinases–A Proof of Concept Study

Overcoming Preclinical Safety Obstacles to Discover (S)‑N‑((1,2,3,5,6,7-Hexahydro‑s‑indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro‑5H‑pyrazolo[5,1‑b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor

Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα)

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα

Discovery of 2‑{3-[2-(1-Isopropyl-3-methyl‑1H‑1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl]‑1H‑pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β‑Sparing Phosphoinositide 3‑Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity

Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability

The Rational Design of Selective Benzoxazepin Inhibitors of the α‑Isoform of Phosphoinositide 3‑Kinase Culminating in the Identification of (S)‑2-((2-(1-Isopropyl‑1H‑1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326)

Structure-Based Design of Potent, Selective, and Orally Bioavailable VPS34 Kinase Inhibitors

Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase

Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K)

Filling a nick in NIK: Extending the half-life of a NIK inhibitor through structure-based drug design

Back Pocket Flexibility Provides Group II p21-Activated Kinase (PAK) Selectivity for Type I 1/2 Kinase Inhibitors

Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform

Structure Based Design of Potent Selective Inhibitors of Protein Kinase D1 (PKD1)

Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles

Cis-Amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase

Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase

Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy

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