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93 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI
Abbvie Bioresearch Center
Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach.EBI
Purdue University
The juxtamembrane region of TrkA kinase is critical for inhibitor selectivity.EBI
Osaka Prefecture University
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI
Merck
Targeting the Nerve Growth Factor (NGF) Pathway in Drug Discovery. Potential Applications to New Therapies for Chronic Pain.EBI
Eli Lilly
The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.EBI
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.EBI
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).EBI
Icahn School of Medicine At Mount Sinai
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.EBI
Genomics Institute of The Novartis Research Foundation
UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.EBI
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 expoEBI
Pfizer
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.EBI
Pfizer
Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.EBI
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).EBI
Glaxosmithkline
Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models.EBI
TBA
A quantitative analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI
Harvard Medical School
Comprehensive analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI
Ambit Biosciences
Switch type I to type II TRK inhibitors for combating clinical resistance induced by xDFG mutation for cancer therapy.EBI
Jinan University
Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules.EBI
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.EBI
Jinan University
Design, synthesis and biological evaluation of novel indolin-2-one derivatives as potent second-generation TRKs inhibitors.EBI
Shenyang Pharmaceutical University
Design, synthesis and anti-tumor efficacy of novel phenyl thiazole/triazole derivatives as selective TrkA inhibitors.EBI
Shenyang Pharmaceutical University
Design, development and evaluation of a prodrug-type TrkA-selective inhibitor with antinociceptive effects in vivo.EBI
Fudan University
A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.EBI
China Pharmaceutical University
Design, synthesis and biological evaluation of pyrazolo[3,4-EBI
Shenyang Pharmaceutical University
Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors.EBI
Astrazeneca
Imidazo[1,2-b]pyridazine as privileged scaffold in medicinal chemistry: An extensive review.EBI
Universite de Tours
Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance.EBI
Jinan University
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.EBI
University of Arkansas For Medical Sciences
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.EBI
China Pharmaceutical University
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.EBI
Zhengzhou University
Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold.EBI
Shenyang Pharmaceutical University
Discovery of quinazoline derivatives CZw-124 as a pan-TRK inhibitor with potent anticancer effects in vitro and in vivo.EBI
Shenyang Pharmaceutical University
Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.EBI
Ain Shams University
Discovery of CH7057288 as an Orally Bioavailable, Selective, and Potent pan-TRK Inhibitor.EBI
Chugai Pharmaceutical
Identification and structural analysis of a selective tropomyosin receptor kinase C (TRKC) inhibitor.EBI
China Pharmaceutical University
Discovery of D6808, a Highly Selective and Potent Macrocyclic c-Met Inhibitor for Gastric Cancer Harboring EBI
Jinan University
Design and synthesis of novel orally selective and type II pan-TRK inhibitors to overcome mutations by property-driven optimization.EBI
National Health Research Institutes
Discovery of novel TrkA allosteric inhibitors: Structure-based virtual screening, biological evaluation and preliminary SAR studies.EBI
Jinan University
Structural Optimization and Structure-Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6EBI
Sichuan University
Discovery of the Next-Generation Pan-TRK Kinase Inhibitors for the Treatment of Cancer.EBI
Yantai University
Design, synthesis and biological evaluation of macrocyclic derivatives as TRK inhibitors.EBI
China Pharmaceutical University
Design, synthesis, biological evaluation and pharmacophore model analysis of novel tetrahydropyrrolo[3,4-c]pyrazol derivatives as potential TRKs inhibitors.EBI
Shenyang Pharmaceutical University
UNC5293, a potent, orally available and highly MERTK-selective inhibitor.EBI
University of North Carolina At Chapel Hill
Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-EBI
The Genomics Institute of The Novartis Research Foundation
Discovery of EBI
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.EBI
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.EBI
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.EBI
Chinese Academy of Sciences
Design, synthesis, and Structure-Activity Relationships (SAR) of 3-vinylindazole derivatives as new selective tropomyosin receptor kinases (Trk) inhibitors.EBI
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.EBI
Sichuan University/Collaborative Innovation Center of Biotherapy
Indole-like Trk receptor antagonists.EBI
University of Tartu
Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase.EBI
Astrazeneca
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.EBI
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.EBI
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.EBI
Pfizer
Pyrazolo[1,5-a]pyrimidine based Trk inhibitors: Design, synthesis, biological activity evaluation.EBI
Jiangnan University
Identification of EBI
China Pharmaceutical University
Efficacy and Tolerability of Pyrazolo[1,5-EBI
The Genomics Institute of The Novartis Research Foundation
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.EBI
Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.EBI
Merck And
Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.EBI
Chinese Academy of Sciences
2-Amino-2,3-dihydro-1EBI
Jinan University
Discovery of 4EBI
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.EBI
Chinese Academy of Sciences
Targeting tropomyosin receptor kinase for cancer therapy.EBI
China Pharmaceutical University
Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application.EBI
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.EBI
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.EBI
Montana State University
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.EBI
Takeda Pharmaceutical
Modulation of Tropomyosin Receptor Kinase for the Treatment of Neurotrophin Diseases: Alzheimer's, Huntington's and Parkinson's.EBI
Usona Institute
Discovery of Allosteric, Potent, Subtype Selective, and Peripherally Restricted TrkA Kinase Inhibitors.EBI
Pfizer
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.EBI
Abbvie Bioresearch Center
A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.EBI
Northwestern University
Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.EBI
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.EBI
Sichuan University/Collaborative Innovation Center of Biotherapy
Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain.EBI
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.EBI
Jinan University
Design, synthesis and SAR of substituted indoles as selective TrkA inhibitors.EBI
Merck
PYRROLOPYRIDINE-3- AND 4-CARBOXAMIDE COMPOSITIONS AND METHODS FOR CELLULAR PROLIFERATIONBDB
Rockefeller University
Heterocyclylmethylidene derivatives and their use as modulators of mGluR5 receptorsBDB
Recordati Industria Chimica E Farmacentica
Amino acid compounds with unbranched linkers and methods of useBDB
Pliant Therapeutics
Substituted imidazo[1,2-A]pyridines as IRAK 1/4 and flt3 inhibitorsBDB
Children''S Hospital Medical Center
KV1.3 inhibitors and their medical applicationBDB
4Sc
Therapeutic compoundsBDB
Celgene Quanticel Research
Neuroactive substituted cyclopenta[b]phenanthrenes as modulators for GABA type-A receptorsBDB
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 treatmentBDB
Bayer Intellectual Property
Protease inhibitorsBDB
Medivir
Differential agonist inhibition identifies multiple epibatidine binding sites in mouse brain.BDB
University of Colorado
Inverse in silico screening for identification of kinase inhibitor targets.BDB
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.BDB
Johnson & Johnson Pharmaceutical