PMID
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Article Title
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Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.

Queen Mary University of London
 
Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-Interacting Protein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome.

National Institute of Biological Sciences
 
Non-kinase targets of protein kinase inhibitors.

The University of Sydney
 
DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.

Glaxosmithkline
 
Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.

Glaxosmithkline
 
A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences
 
Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences
 
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Ambit Biosciences
 
LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2.

Eli Lilly and Company
 
Azaindole derivatives as potential kinase inhibitors and their SARs elucidation.

Hunan University of Science and Technology
 
Exploring positions 6 and 7 of a quinazoline-based scaffold leads to changes in selectivity and potency towards RIPK2/3 kinases.

Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences
 
Identification of Pyrido[3,4-d]pyrimidine derivatives as RIPK3-Mediated necroptosis inhibitors.

Korea University
 
Synthesis and evaluation of dihydrofuro[2,3-b]pyridine derivatives as potent IRAK4 inhibitors.

Soochow University
 
Preclinical Evaluation of Dihydropyrazole-Cored Positron Emission Tomography (PET) Ligands for Imaging of Receptor-Interacting Serine/Threonine Protein Kinase 1 (RIPK1) in the Brain.

Beijing Normal University
 
Design, synthesis and anti-necroptosis activity of fused heterocyclic MLKL inhibitors.

Ningxia Medical University
 
From Hit to Lead: Structure-Based Optimization of Novel Selective Inhibitors of Receptor-Interacting Protein Kinase 1 (RIPK1) for the Treatment of Inflammatory Diseases.

Sichuan University
 
Discovery of 4-amino-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one derivatives as potential receptor-interacting serine/threonine-protein kinase 1 (RIPK1) inhibitors.

West China Hospital of Sichuan University
 
RIPK1 inhibitors: A key to unlocking the potential of necroptosis in drug development.

Lanzhou University Second Hospital
 
Scaffold hopping derived novel benzoxazepinone receptor-interacting protein kinase 1 (RIP1) inhibitors as anti-necroptosis agents: Anti-inflammatory effect in systemic inflammatory response syndrome (SIRS) and epilepsy.

Ningxia Medical University
 
Discovery of Sibiriline derivatives as novel receptor-interacting protein kinase 1 inhibitors.

China Pharmaceutical University
 
Targeting Receptor-Interacting Protein Kinase 1 by Novel Benzothiazole Derivatives: Treatment of Acute Lung Injury through the Necroptosis Pathway.

Ningxia Medical University
 
Insight from Linker Investigations: Discovery of a Novel Phenylbenzothiazole Necroptosis Inhibitor Targeting Receptor-Interacting Protein Kinase 1 (RIPK1) from a Phenoxybenzothiazole Compound with Dual RIPK1/3 Targeting Activity.

Zhejiang University
 
The Hitchhiker's Guide to Deep Learning Driven Generative Chemistry.

Insilico Medicine Hong Kong
 
Novel Fused Triazole Compounds as RIPK1 Inhibitors for Treating Neurodegenerative, Autoimmune, and Inflammatory Diseases.

Smith, Gambrell & Russell
 
From (Tool)Bench to Bedside: The Potential of Necroptosis Inhibitors.

The Walter and Eliza Hall Institute of Medical Research
 
Novel Isoxazolidines as RIPK1 Inhibitors for Treating Alzheimer's Disease, Multiple Sclerosis, and Amyotrophic Lateral Sclerosis.

Smith, Gambrell & Russell
 
Scaffold hopping derived novel benzoxazepinone RIPK1 inhibitors as anti-necroptosis agents.

Ningxia Medical University
 
Structure-Based Design of Novel Alkynyl Thio-Benzoxazepinone Receptor-Interacting Protein Kinase-1 Inhibitors: Extending the Chemical Space from the Allosteric to ATP Binding Pockets.

Ningxia Medical University
 
Design, synthesis, and structure-activity relationship of novel RIPK2 inhibitors.

Soochow University
 
Small-Molecule Receptor-Interacting Protein 1 (RIP1) Inhibitors as Therapeutic Agents for Multifaceted Diseases: Current Medicinal Chemistry Insights and Emerging Opportunities.

West China Hospital
 
Investigation on the chemical space of the substituted triazole thio-benzoxazepinone RIPK1 inhibitors.

Ningxia Medical University
 
Discovery of novel 2,8-diazaspiro[4.5]decan-1-one derivatives as potent RIPK1 kinase inhibitors.

China Pharmaceutical University
 
Discovery of Potent and Selective Receptor-Interacting Serine/Threonine Protein Kinase 2 (RIPK2) Inhibitors for the Treatment of Inflammatory Bowel Diseases (IBDs).

West China Hospital
 
Discovery of a Trifluoromethoxy Cyclopentanone Benzothiazole Receptor-Interacting Protein Kinase 1 Inhibitor as the Treatment for Alzheimer's Disease.

China Pharmaceutical University
 
Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity.

Soochow University
 
Novel RIPK1 Inhibitors for Treating Neurodegenerative, Autoimmune, and Inflammatory Diseases.

Smith, Gambrell & Russell
 
Enantiomeric profiling of a chiral benzothiazole necroptosis inhibitor.

Ningxia Medical University
 
Ring closure strategy leads to potent RIPK3 inhibitors.

Soochow University
 
Discovery of simplified benzazole fragments derived from the marine benzosceptrin B as necroptosis inhibitors involving the receptor interacting protein Kinase-1.

Paris-Saclay University
 
Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.

Genentech
 
-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[

Ningxia Medical University
 
Discovery of 4

TBA
 
Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives.

Fudan University
 
Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.

Glaxosmithkline
 
Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage.

Bristol-Myers Squibb Research & Development
 
Heterocyclic Amides as Kinase Inhibitors.

Usona Institute
 
Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.

Glaxosmithkline
 
Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.

Sichuan University/Collaborative Innovation Center of Biotherapy
 
Tozasertib Analogues as Inhibitors of Necroptotic Cell Death.

University of Antwerp
 
Discovery of 7-Oxo-2,4,5,7-tetrahydro-6 H-pyrazolo[3,4- c]pyridine Derivatives as Potent, Orally Available, and Brain-Penetrating Receptor Interacting Protein 1 (RIP1) Kinase Inhibitors: Analysis of Structure-Kinetic Relationships.

Takeda Pharmaceutical
 
PIPERIDINYL-METHYLPURINE PYRIMIDINES AND RELATED COMPOUNDS AND THEIR USE IN TREATING DISEASES AND CONDITIONS

K36 Therapeutics
 
2,6,9-TRISUBSTITUTED PURINES

Astrazeneca
 
PYRAZOLE MEMBRANE-ASSOCIATED TYROSINE-AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF

Insilico Medicine Ip
 
BIFUNCTIONAL ARYLSULPHONAMIDE COMPOUNDS

Anaxis Pharma
 
JAK1 pathway inhibitors for the treatment of prurigo nodularis

Incyte
 
COMPOSITIONS AND METHODS OF USE TO TREAT 12-LIPOXYGENASE (12-LOX) MEDIATED DISEASES

Veralox Therapeutics
 
SUBSTITUTED FUSED HETEROCYCLIC COMPOUND, AND PREPARATION METHOD THEREFOR AND USE THEREOF

Shanghai Annova Biotechnology
 
COMPOUND BASED ON QUINAZOLINE-SUBSTITUTED GLUTARIMIDE SKELETON AND USE THEREOF

Gluetacs Therapeutics (Shanghai) Co.
 
Pharmaceutical compositions comprising heterocycle fused gamma carboline prodrugs

Intra-Cellular Therapies
 
COMPOSITION FOR PREVENTING OR TREATING GRAVES' DISEASE COMPRISING COMPOUND CONTAINING AN IMIDAZOPYRIDINE STRUCTURE AS ACTIVE INGREDIENT

Esgelbio
 
PYRIMIDINE DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER COMPRISING SAME AS ACTIVE INGREDIENT

Korea Reserarch Institute of Chemical Technology
 
NAMPT ACTIVATORS FOR TREATING METABOLIC AND NEUROLOGICAL DISORDERS

University of Illinois
 
NAPHTHYRIDONE COMPOUNDS FOR INHIBITION OF RAF KINASES AND/OR BCR-ABL TYROSINE KINASES

Enliven
 
Tie-2 activators targeting the Schlemm's canal

EyePoint Pharmaceuticals, Inc.
 
Benzothiophene-based selective estrogen receptor downregulator compounds

University of Illinois
 
Pyrrole-substituted indolone derivative or pharmaceutically acceptable salts thereof, and preparation method therefor and application thereof

Suzhou Genhouse Pharmaceutical Co.
 
MODULATORS OF FPR1 AND METHODS OF USING THE SAME

Biofront
 
ADENOSINE ANALOGS FOR THE TREATMENT OF DISEASE

Biointervene
 
SMALL MOLECULE INHIBITORS OF BACTERIAL TOXINS

Artizan Biosciences
 
TKI permeability enhancers

City of Hope
 
5-heteroaryl substituted indazole-3-carboxamides and preparation and use thereof

Biosplice Therapeutics
 
CDK inhibitors and their use as pharmaceuticals

Prelude Therapeutics
 
Substituted piperazines as BTK inhibitors

Hutchison Medipharma
 
Methylamine derivatives as lysysl oxidase inhibitors for the treatment of cancer

The Institute of Cancer Research: Royal Cancer Hospital
 
Bicyclic heterocycles as FGFR inhibitors

Incyte
 
Fluoroalkyl-oxadiazoles and uses thereof

Tenaya Therapeutics
 
Heterocyclic compounds as immunomodulators

Incyte
 
Phosphonate linkers and their use to facilitate cellular retention of compounds

Merck Sharp & Dohme
 
Pyrazolo[1,5-a]pyrazin-4-yl derivatives

Pfizer
 
Cyclic di-nucleotide compounds as sting agonists

Merck Sharp & Dohme
 
Kinase inhibitors

Insilico Medicine Ip
 
Small molecule activators of Parkin enzyme function

Mayo Foundation For Medical Education and Research
 
Therapeutic compounds and uses thereof

Kala Pharmaceuticals
 
CRBN ligands and uses thereof

Kymera Therapeutics
 
Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof

La Jolla Institute of Allergy & Immunology
 
Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors

Array Biopharma
 
Aryl-or heteroaryl-substituted benzene compounds

Epizyme
 
Fused heterocyclic derivatives, their preparation methods thereof and medical uses thereof

Beijing Innocare Pharma Tech
 
Piperazinyl norbenzomorphan compounds and methods for using the same

University Of Texas
 
Alpha-truxillic acid derivatives and pharmaceutical compositions thereof

The State University of New York
 
Kinase inhibitors

Oxular Acquisitions
 
HDAC inhibitor compounds and methods of treatment

University of Florida Research Foundation
 
5-aromatic alkynyl substituted benzamide compound and preparation method, pharmaceutical composition, and use thereof

Shanghai Institute of Material Medica, Chinese Academy of Sciences
 
Inhibitors of cellular necrosis and related methods

President and Fellows of Harvard College
 
[1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds

Bristol-Myers Squibb
 
2-amino 6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl-1,3-thiazol-4-yl amides

Pfizer
 
Evaluation of in vitro effects of some analgesic drugs on erythrocyte and recombinant carbonic anhydrase I and II.

Balikesir University
 
Methods of treatment of histamine H-4 receptor-related pruritus associated with nerve disorders

Bridge Pharma
 
Thienopyrimidine derivatives, processes for the preparation thereof and therapeutic uses thereof

Sanofi
 
Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B.

Abbott Laboratories