PMID

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Article Title

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Discovery of novel CDK8 inhibitors using multiple crystal structures in docking-based virtual screening.

West China Hospital of Sichuan University

Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.

University of Nebraska Medical Center

Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.

Merck

2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19.

The Institute of Cancer Research

Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.

Genentech

Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.

The Institute of Cancer Research

Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.

Merck

Discovery and Anti-Inflammatory Activity Evaluation of a Novel CDK8 Inhibitor through Upregulation of IL-10 for the Treatment of Inflammatory Bowel Disease

Anhui Medical University

Discovery of 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and selective CDK9 inhibitors that enable transient target engagement for the treatment of hematologic malignancies.

China Pharmaceutical University

From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.

The People'S Hospital of Xinjiang Uyghur Autonomous Region

Target-Focused Library Design by Pocket-Applied Computer Vision and Fragment Deep Generative Linking.

Umr7200 Cnrs-Universit£

A Selective and Orally Bioavailable Quinoline-6-Carbonitrile-Based Inhibitor of CDK8/19 Mediator Kinase with Tumor-Enriched Pharmacokinetics.

University of South Carolina

Identification of 3, 4-disubstituted pyridine derivatives as novel CDK8 inhibitors.

Chinese Academy of Medical Sciences and Peking Union Medical College

Discovery of

China Pharmaceutical University

Development of Highly Potent and Selective Pyrazolopyridine Inhibitor of CDK8/19.

Dana-Farber Cancer Institute

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

University of South Australia

Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity.

China Pharmaceutical University

Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.

University of South Australia

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

Astrazeneca

Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.

China Pharmaceutical University

Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures.

The First Affiliated Hospital of Zhengzhou University

Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13.

Harvard Medical School

Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8.

Genentech

CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.

Shaoxing University

Discovery of 4-Piperazine Isoquinoline Derivatives as Potent and Brain-Permeable Tau Prion Inhibitors with CDK8 Activity.

University of California

Shape-based virtual screen for the discovery of novel CDK8 inhibitor chemotypes.

Wannan Medical College

Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-

Takeda Pharmaceutical

Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88

Astrazeneca

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

Takeda Pharmaceutical

Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.

Astrazeneca

Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor.

Chinese Academy of Sciences

Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?

University of South Australia

Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors.

Takeda Pharmaceutical

Discovery of potent and selective CDK8 inhibitors through FBDD approach.

Roche Innovation Center Shanghai

Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML.

Chinese Academy of Sciences

Design and synthesis of selective CDK8/19 dual inhibitors: Discovery of 4,5-dihydrothieno[3',4':3,4]benzo[1,2-d]isothiazole derivatives.

Takeda Pharmaceutical

Studies of CDK 8/19 inhibitors: Discovery of novel and selective CDK8/19 dual inhibitors and elimination of their CYP3A4 time-dependent inhibition potential.

Takeda Pharmaceutical