PMID

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Article Title

Organization

Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity.

Merck

Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.

Merck

Carboxamide Spleen Tyrosine Kinase (Syk) Inhibitors: Leveraging Ground State Interactions To Accelerate Optimization.

Merck

Potent, selective and orally bioavailable leucine-rich repeat kinase 2 (LRRK2) inhibitors.

Merck Research Laboratories

Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).

Icahn School of Medicine At Mount Sinai

Chemical Biology of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors.

Genentech

Discovery of LRRK2 inhibitors using sequential in silico joint pharmacophore space (JPS) and ensemble docking.

Acelot

Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors.

Merck

Optimisation of LRRK2 inhibitors and assessment of functional efficacy in cell-based models of neuroinflammation.

University of Sydney

Inhibitors of c-Jun N-terminal kinases: an update.

Eberhard Karls Universit£T T£Bingen

Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.

Pfizer

Kinase domain inhibition of leucine rich repeat kinase 2 (LRRK2) using a [1,2,4]triazolo[4,3-b]pyridazine scaffold.

Pfizer

Indolinone based LRRK2 kinase inhibitors with a key hydrogen bond.

Technische Universit£T Darmstadt

Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

Genentech

Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.

Glaxosmithkline

Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.

Califia Bio

Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2.

Novartis Institutes For Biomedical Research

The development of CNS-active LRRK2 inhibitors using property-directed optimisation.

The University of Sydney

Triazolopyridazine LRRK2 kinase inhibitors.

Elan Pharmaceuticals

Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors.

Elan Pharmaceuticals

Novel cinnoline-based inhibitors of LRRK2 kinase activity.

Elan Pharmaceuticals

Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor.

Genentech

GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.

Glaxosmithkline

Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

Genentech

Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling.

Genentech

Brain Penetrant LRRK2 Inhibitor.

TBA

Inhibitors of LRRK2 as Treatment for Parkinson's Disease: Patent Highlight.

TBA

Characterization of TAE684 as a potent LRRK2 kinase inhibitor.

University of Dundee

Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity.

Boehringer Ingelheim Pharmaceuticals

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.

Newcastle University Centre For Cancer

Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy.

Stanford University

Unraveling the Design and Discovery of c-Jun N-Terminal Kinase Inhibitors and Their Therapeutic Potential in Human Diseases.

National Clinical Research Center For Geriatrics

Discovery of 1

Stanford University

2-Aminoquinazolines as LRRK2 Inhibitors for Treating Parkinson's Disease.

Smith, Gambrell & Russell

Novel N-Linked Isoquinoline Amides as LRRK2 Inhibitors for Treating Parkinson's Disease.

Smith, Gambrell & Russell

A survey of the clinical pipeline in neuroscience.

Jnana Therapeutics

Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors.

Merck

Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.

University of North Carolina At Chapel Hill

Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors.

Merck

Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia.

Sanford Burnham Prebys Medical Discovery Institute

Design and Synthesis of Pyrrolo[2,3-

Vernalis (R&D)

Structure-Guided Optimization Provides a Series of TTK Protein Inhibitors with Potent Antitumor Activity.

Bristol Myers Squibb

Novel Macrocyclic LRRK2 Inhibitors for Treating Parkinson's Disease.

Smith, Gambrell & Russell

Novel

Smith, Gambrell & Russell

Discovery of a potent, highly selective, and orally bioavailable inhibitor of CDK8 through a structure-based optimisation.

University of South Australia

Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors.

Gsk Pharmaceuticals R&D

Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.

Beijing Normal University

Novel N-Heteroaryl Indazole Derivatives as LRRK2 Inhibitors for Treating Parkinson's Disease.

Smith, Gambrell & Russell

1-Pyrazolyl-5,6-Disubstituted Indazole Derivatives as LRRK2 Inhibitors for Treating Parkinson's Disease.

Smith, Gambrell & Russell

Monomeric Targeted Protein Degraders.

TBA

Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.

Genentech

Identification of

China Pharmaceutical University

Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6

Harvard Medical School

Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.

Merck

Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.

Merck And

Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.

Glaxosmithkline R&D

LRRK2 Kinase Inhibitors as Possible Therapy for Parkinson's Disease and Other Neurodegenerative Disorders.

Therachem Research Medilab

Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors.

Glaxosmithkline R&D

Benzothiazole-Based LRRK2 Inhibitors as Wnt Enhancers and Promoters of Oligodendrocytic Fate.

Csic

Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach.

Glaxosmithkline R&D

Discovery of 4

TBA

5-Substituted-N-pyridazinylbenzamides as potent and selective LRRK2 inhibitors: Improved brain unbound fraction enables efficacy.

Gsk Pharmaceuticals R&D

Design and Optimization Leading to an Orally Active TTK Protein Kinase Inhibitor with Robust Single Agent Efficacy.

Celgene

Imidazoquinolines as Novel Inhibitors of LRRK2 Kinase Activity.

Drexel University

Discovery of potent and selective 5-azaindazole inhibitors of leucine-rich repeat kinase 2 (LRRK2) - Part 1.

Lifearc

Discovery of potent azaindazole leucine-rich repeat kinase 2 (LRRK2) inhibitors possessing a key intramolecular hydrogen bond - Part 2.

Genentech

ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.

University of Florida

Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.

Eppley Institute For Research In Cancer and Allied Diseases

Identification of chemicals to inhibit the kinase activity of leucine-rich repeat kinase 2 (LRRK2), a Parkinson's disease-associated protein.

Inje University

Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease.

Glaxosmithkline R&D

Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N

The Institute of Cancer Research

Leucine rich repeat kinase 2 (LRRK2) inhibitors based on indolinone scaffold: Potential pro-neurogenic agents.

Centro De Investigaciones Biol�Gicas-Csic

Characterization of a highly selective inhibitor of the Aurora kinases.

Harvard Medical School

Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors.

Neurodegeneration Dpu

The design and SAR of a novel series of 2-aminopyridine based LRRK2 inhibitors.

H. Lundbeck

Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1).

Vernalis (R&D)

Discovery of LRRK2 inhibitors by using an ensemble of virtual screening methods.

Charles River Discovery Research Services

Rationalizing the Binding Kinetics for the Inhibition of the Burkholderia pseudomallei FabI1 Enoyl-ACP Reductase.

Stony Brook University

Type I and type II GABAA-benzodiazepine receptors produced in transfected cells.

UniversitÄT Heidelberg

Insight into binding of calyculin A to protein phosphatase 1: isolation of hemicalyculin a and chemical transformation of calyculin A.

The University of Tokyo

Synthesis of substituted diarylmethylenepiperidines (DAMPs), a novel class of anti-HIV agents.

Purdue University

Thermodynamic and structure guided design of statin based inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase.

Boehringer Ingelheim Pharmaceuticals

Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class.

Upjohn

Use of binding enthalpy to drive an allosteric transition.

University of Maryland