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Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect isletβ-cells from apoptosis.

East China Normal University

Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.

Principia Biopharma

Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding.

High Magnetic Field Laboratory

Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locke

Bristol-Myers Squibb Research and Development

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

Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.

Amgen

Development of Selective Covalent Janus Kinase 3 Inhibitors.

Harvard Medical School

Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton's Tyrosine Kinase.

Takeda California

Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.

Sichuan University

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

Merck

Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.

Peking University

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

Exelixis

Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.

Abbott Laboratories

Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.

Cellzome

Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.

Hoffmann-La Roche

Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c

Cephalon

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

Discovery and development of aurora kinase inhibitors as anticancer agents.

Vertex Pharmaceuticals

Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.

Abbott Laboratories

Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.

Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories

Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase.

Serono Pharmaceutical Research Institute

Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).

Ansaris

Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.

Pfizer

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

Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.

Center For Molecular Medicine of The Austrian Academy of Sciences

Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.

Abbott Laboratories

Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.

Cgi Pharmaceuticals

2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.

Abbott Laboratories

Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.

Glaxosmithkline

Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.

The Scripps Research Institute

Discovery of a Dual Tubulin and Neuropilin-1 (NRP1) Inhibitor with Potent In Vivo Anti-Tumor Activity via Pharmacophore-based Docking Screening, Structure Optimization, and Biological Evaluation.

China Pharmaceutical University

Discovery of 2,5-diaminopyrimidine derivatives as the first series of selective monomeric degraders of B-lymphoid tyrosine kinase.

Peking University

Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.

Galapagos

Controlling Ibrutinib's Conformations about Its Heterobiaryl Axis to Increase BTK Selectivity.

San Diego State University

Discovery of BGB-8035, a Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase for B-Cell Malignancies and Autoimmune Diseases.

Beigene (Beijing) Co.

Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.

Targegen

Discovery of selective irreversible inhibitors of B-Lymphoid tyrosine kinase (BLK).

Peking University

Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.

Janssen Research & Development

Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.

Biogen

Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib.

Nantong University

Discovery of Reversible Covalent Bruton's Tyrosine Kinase Inhibitors PRN473 and PRN1008 (Rilzabrutinib).

Principia Biopharma, A Sanofi

Discovery of the Bruton's Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (

Takeda California

Structure-activity relationship investigation for imidazopyrazole-3-carboxamide derivatives as novel selective inhibitors of Bruton's tyrosine kinase.

Henan Normal University

Discovery of 1-Amino-1

Henan Normal University

Discovery of Potent Antiallergic Agents Based on an

Chinese Academy of Sciences

Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-

The Genomics Institute of The Novartis Research Foundation

Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold.

China Pharmaceutical 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

From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer.

Sichuan University

Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.

Merck

Discovery of quinoline-based irreversible BTK inhibitors.

Acerta Pharma

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

Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.

Merck Research Laboratories

Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.

Abbott Bioresearch Center

Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.

Bristol Myers Squibb Research

Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity

University of Nottingham

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

Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).

Bristol-Myers Squibb Research and Development

4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors.

Chinese Academy of Sciences

Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.

TBA

Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.

Zhejiang University

Discovery of a potent dual ALK and EGFR T790M inhibitor.

Harvard Medical School

Discovery of 4

TBA

Identification of a new family of pyrazolo[3,4-d]pyrimidine derivatives as multitarget Fyn-Blk-Lyn inhibitors active on B- and T-lymphoma cell lines.

University of Siena

Design, Synthesis, and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.

Jinan University

Discovery of 7H-pyrrolo[2,3-d]pyrimidine derivatives as selective covalent irreversible inhibitors of interleukin-2-inducible T-cell kinase (Itk).

Peking University

Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis.

Sichuan University and Collaborative Innovation Center

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

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

Takeda Pharmaceutical

Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.

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

Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.

Pfizer

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

ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.

Vertex Pharmaceuticals

ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.

Vertex Pharmaceuticals

Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.

China Pharmaceutical University

Recent advances in JAK3 inhibition: Isoform selectivity by covalent cysteine targeting.

Eberhard-Karls-University Tuebingen

Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors.

University of Science and Technology of China

Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC.

Sichuan University and Collaborative Innovation Center

Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.

Merck

Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.

High Magnetic Field Laboratory

Small molecules inhibit STAT3 activation, autophagy, and cancer cell anchorage-independent growth.

Indiana University School of Medicine

HETEROARYL AMIDES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF

Merck Sharp & Dohme

Pyrazolo[3,4-B]pyridines and imidazo[1,5-B]pyridazines as PDE1 inhibitors

H. Lundbeck

Pyrimidinones as factor XIA inhibitors

Bristol-Myers Squibb

Imidazopyridines Syk inhibitors

Kronos Bio

Compositions and methods for treating KIT- and PDGFRA-mediated diseases

Blueprint Medicines

Spiro-fused cyclic ureas as inhibitors of rock

Bristol-Myers Squibb

Compositions for binding sphingosine-1-phosphate receptor 1 (S1P1), imaging of S1P1, and methods of use thereof

Washington University

Substituted quinazolines for inhibiting kinase activity

Neupharma

N-azaspirocycloalkane substituted N-heteroaryl compounds and compositions for inhibiting the activity of SHP2

Novartis

Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity

Boehringer Ingelheim International

3-(indol-3-yl)-pyridine derivatives, pharmaceutical compositions and methods for use

Iteos Therapeutics

Substituted spirocycles

Boehringer Ingelheim International

Matrix metalloproteinase inhibitors and methods for the treatment of pain and other diseases

TBA

Substituted 7-azabicycles and their use as orexin receptor modulators

Janssen Pharmaceutica

Tyrosinase inhibitory activities of the compounds isolated from Neolitsea aciculata (Blume) Koidz.

Jeju National University

Carbonic anhydrase inhibitors: in vitro inhibition of a isoforms (hCA I, hCA II, bCA III, hCA IV) by flavonoids.

Ondokuz Mayis University

Pyridinedione carboxamide inhibitors of endothelial lipase

Bristol-Myers Squibb

Quinoxaline carboxamide derivatives as protein tyrosine kinase inhibitors

Novartis

Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex.

Case Western Reserve University

Cloning, molecular characterization, and chromosomal assignment of a gene encoding a second D1 dopamine receptor subtype: differential expression pattern in rat brain compared with the D1A receptor.

Duke University

Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.

Amgen