PMID
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Article Title
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Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.

Abbvie Bioresearch Center
Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach.

Purdue University
The juxtamembrane region of TrkA kinase is critical for inhibitor selectivity.

Osaka Prefecture University
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.

Merck
Targeting the Nerve Growth Factor (NGF) Pathway in Drug Discovery. Potential Applications to New Therapies for Chronic Pain.

Eli Lilly
The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.

St. John'S University
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.

Nerviano Medical Sciences
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
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.

Genomics Institute of The Novartis Research Foundation
UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.

University of North Carolina At Chapel Hill
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain expo

Pfizer
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.

Pfizer
Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.

Genentech
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).

Glaxosmithkline
Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models.

TBA
A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.

Harvard Medical School
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
Switch type I to type II TRK inhibitors for combating clinical resistance induced by xDFG mutation for cancer therapy.

Jinan University
Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules.

University of Arkansas
Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations.

Jinan University
Design, synthesis and biological evaluation of novel indolin-2-one derivatives as potent second-generation TRKs inhibitors.

Shenyang Pharmaceutical University
Design, synthesis and anti-tumor efficacy of novel phenyl thiazole/triazole derivatives as selective TrkA inhibitors.

Shenyang Pharmaceutical University
Design, development and evaluation of a prodrug-type TrkA-selective inhibitor with antinociceptive effects in vivo.

Fudan University
A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.

China Pharmaceutical University
Design, synthesis and biological evaluation of pyrazolo[3,4-

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

Astrazeneca
Imidazo[1,2-b]pyridazine as privileged scaffold in medicinal chemistry: An extensive review.

Universite de Tours
Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance.

Jinan University
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.

University of Arkansas For Medical Sciences
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.

China Pharmaceutical University
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.

Zhengzhou University
Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold.

Shenyang Pharmaceutical University
Discovery of quinazoline derivatives CZw-124 as a pan-TRK inhibitor with potent anticancer effects in vitro and in vivo.

Shenyang Pharmaceutical University
Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.

Ain Shams University
Discovery of CH7057288 as an Orally Bioavailable, Selective, and Potent pan-TRK Inhibitor.

Chugai Pharmaceutical
Identification and structural analysis of a selective tropomyosin receptor kinase C (TRKC) inhibitor.

China Pharmaceutical University
Discovery of D6808, a Highly Selective and Potent Macrocyclic c-Met Inhibitor for Gastric Cancer Harboring

Jinan University
Design and synthesis of novel orally selective and type II pan-TRK inhibitors to overcome mutations by property-driven optimization.

National Health Research Institutes
Discovery of novel TrkA allosteric inhibitors: Structure-based virtual screening, biological evaluation and preliminary SAR studies.

Jinan University
Structural Optimization and Structure-Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6

Sichuan University
Discovery of the Next-Generation Pan-TRK Kinase Inhibitors for the Treatment of Cancer.

Yantai University
Design, synthesis and biological evaluation of macrocyclic derivatives as TRK inhibitors.

China Pharmaceutical University
Design, synthesis, biological evaluation and pharmacophore model analysis of novel tetrahydropyrrolo[3,4-c]pyrazol derivatives as potential TRKs inhibitors.

Shenyang Pharmaceutical University
UNC5293, a potent, orally available and highly MERTK-selective inhibitor.

University of North Carolina At Chapel Hill
Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-

The Genomics Institute of The Novartis Research Foundation
Discovery of

China Pharmaceutical University
Design, synthesis, and biological evaluation of 2,4-diamino pyrimidine derivatives as potent FAK inhibitors with anti-cancer and anti-angiogenesis activities.

Guizhou Medical University
Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation.

University of Arkansas For Medical Sciences
Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants.

Chinese Academy of Sciences
Design, synthesis, and Structure-Activity Relationships (SAR) of 3-vinylindazole derivatives as new selective tropomyosin receptor kinases (Trk) inhibitors.

Jinan University
Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.

Sichuan University/Collaborative Innovation Center of Biotherapy
Indole-like Trk receptor antagonists.

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

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

Beijing Normal University
Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis.

Sichuan University and Collaborative Innovation Center
The Discovery of a Potent, Selective, and Peripherally Restricted Pan-Trk Inhibitor (PF-06273340) for the Treatment of Pain.

Pfizer
Pyrazolo[1,5-a]pyrimidine based Trk inhibitors: Design, synthesis, biological activity evaluation.

Jiangnan University
Identification of

China Pharmaceutical University
Efficacy and Tolerability of Pyrazolo[1,5-

The Genomics Institute of The Novartis Research Foundation
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.

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

Merck And
Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.

Chinese Academy of Sciences
2-Amino-2,3-dihydro-1

Jinan University
Discovery of 4

TBA
Design, synthesis and biological evaluation of 3-(imidazo[1,2-a]pyrazin-3-ylethynyl)-2-methylbenzamides as potent and selective pan-tropomyosin receptor kinase (TRK) inhibitors.

Chinese Academy of Sciences
Targeting tropomyosin receptor kinase for cancer therapy.

China Pharmaceutical University
Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application.

University of Arkansas For Medical Sciences
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, biological evaluation, and molecular modeling of 11H-indeno[1,2-b]quinoxalin-11-one derivatives and tryptanthrin-6-oxime as c-Jun N-terminal kinase inhibitors.

Montana State University
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.

Takeda Pharmaceutical
Modulation of Tropomyosin Receptor Kinase for the Treatment of Neurotrophin Diseases: Alzheimer's, Huntington's and Parkinson's.

Usona Institute
Discovery of Allosteric, Potent, Subtype Selective, and Peripherally Restricted TrkA Kinase Inhibitors.

Pfizer
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.

Abbvie Bioresearch Center
A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.

Northwestern University
Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.

Unc Eshelman School of Pharmacy
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
Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain.

Pfizer
Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.

Jinan University
Design, synthesis and SAR of substituted indoles as selective TrkA inhibitors.

Merck
PYRROLOPYRIDINE-3- AND 4-CARBOXAMIDE COMPOSITIONS AND METHODS FOR CELLULAR PROLIFERATION

Rockefeller University
Heterocyclylmethylidene derivatives and their use as modulators of mGluR5 receptors

Recordati Industria Chimica E Farmacentica
Amino acid compounds with unbranched linkers and methods of use

Pliant Therapeutics
Substituted imidazo[1,2-A]pyridines as IRAK 1/4 and flt3 inhibitors

Children''S Hospital Medical Center
KV1.3 inhibitors and their medical application

4Sc
Therapeutic compounds

Celgene Quanticel Research
Neuroactive substituted cyclopenta[b]phenanthrenes as modulators for GABA type-A receptors

Washington University
(5s,8s)-3-(4′-chlor-3′-fluor-4-methlybiphenyl-3-yl)-4-hydroxy-8-methoxy-1-azaspiro[4.5] dec-3-en-2-one (compound A) for treatment

Bayer Intellectual Property
Protease inhibitors

Medivir
Differential agonist inhibition identifies multiple epibatidine binding sites in mouse brain.

University of Colorado
Inverse in silico screening for identification of kinase inhibitor targets.

University of Munich
In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.

Johnson & Johnson Pharmaceutical