PMID

Data

Article Title

Organization

Locking PDK1 in DFG-out conformation through 2-oxo-indole containing molecules: Another tools to fight glioblastoma.

University Of Pisa

Discovery of novel 7-azaindoles as PDK1 inhibitors.

Merck

Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.

Zhejiang 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

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.

Novartis Institutes For Biomedical Research

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

Small-Molecule Allosteric Modulators of the Protein Kinase PDK1 from Structure-Based Docking.

Bioinformatics Institute (Bii)

Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.

Nerviano Medical Sciences

Exploitation of the ability of¿-tocopherol to facilitate membrane co-localization of Akt and PHLPP1 to develop PHLPP1-targeted Akt inhibitors.

The Ohio State University

Synthesis and biological evaluation of 2-anilino-4-substituted-7H-pyrrolopyrimidines as PDK1 inhibitors.

La Trobe University

Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.

Nerviano Medical Sciences

Synthesis and biological evaluation of substituted 3-anilino-quinolin-2(1H)-ones as PDK1 inhibitors.

La Trobe University

Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.

Lexicon Pharmaceuticals

Stereoselective synthesis and anti-proliferative effects on prostate cancer evaluation of 5-substituted-3,4-diphenylfuran-2-ones.

Henan University Of Traditional Chinese Medicine

Selective 3-phosphoinositide-dependent kinase 1 (PDK1) inhibitors: dissecting the function and pharmacology of PDK1.

Glaxosmithkline

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

Abbott Laboratories

Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKe kinases.

Mrc Technology

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

2-(3-Oxo-1,3-diphenylpropyl)malonic acids as potent allosteric ligands of the PIF pocket of phosphoinositide-dependent kinase-1: development and prodrug concept.

Saarland University

Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.

Exelixis

Inverse Virtual Screening allows the discovery of the biological activity of natural compounds.

Universit£

Thieno[3,2-d]pyrimidin-4(3H)-one derivatives as PDK1 inhibitors discovered by fragment-based screening.

S*Bio

2-anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1.

S*Bio

Structure-based optimization of potent PDK1 inhibitors.

Nerviano Medical Sciences

Design and synthesis of benzoazepin-2-one analogs as allosteric binders targeting the PIF pocket of PDK1.

Genomics Institute Of The Novartis Research Foundation

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.

Novartis Institute For Biomedical Research

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

New inhibitor of 3-phosphoinositide dependent protein kinase-1 identified from virtual screening.

Central China Normal University

Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).

Pfizer

Structure-based design of PDK1 inhibitors.

S Bio

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.

Glaxosmithkline

Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2.

Osi Pharmaceuticals

Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.

TBA

Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.

TBA

Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors.

Novartis Institutes For Biomedical Research

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

Ambit Biosciences

The identification of 8,9-dimethoxy-5-(2-aminoalkoxy-pyridin-3-yl)-benzo[c][2,7]naphthyridin-4-ylamines as potent inhibitors of 3-phosphoinositide-dependent kinase-1 (PDK-1).

Wyeth Research

Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.

Wyeth Research

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

Abbott Laboratories

3,5-Diphenylpent-2-enoic acids as allosteric activators of the protein kinase PDK1: structure-activity relationships and thermodynamic characterization of binding as paradigms for PIF-binding pocket-targeting compounds.

Saarland University

3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.

Johnson & Johnson Pharmaceutical Research & Development

Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.

Boehringer Ingelheim Pharmaceuticals

Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.

Novartis Institutes For Biomedical Research

Inhibition of mammalian carbonic anhydrases I-XIV with grayanotoxin III: solution and in silico studies.

University Of Calgary

Price for Opening the Transient Specificity Pocket in Human Aldose Reductase upon Ligand Binding: Structural, Thermodynamic, Kinetic, and Computational Analysis.

Philipps-Universität Marburg

 

Efficient synthesis of novel dialkyl-3-cyanopropylphosphate derivatives and evaluation of their anticholinesterase activity

University Of Carthage

An Unusual Protector-Protégé Strategy for the Biosynthesis of Purine Nucleoside Antibiotics.

Wuhan University

Carbohydrazones as new class of carbonic anhydrase inhibitors: Synthesis, kinetics, and ligand docking studies.

University Of Karachi

Synthesis, molecular docking and biological evaluation of some newer 2-substituted-4-(benzo[d][1,3]dioxol-5-yl)-6-phenylpyridazin-3(2H)-ones as potential anti-inflammatory and analgesic agents.

Panjab University

Design and synthesis of quinazoline-3,4-(4H)-diamine endowed with thiazoline moiety as new class for DPP-4 and DPPH inhibitor.

Jamia Hamdard (Hamdard University)

Small-Molecule Chemical Probe Rescues Cells from Mono-ADP-Ribosyltransferase ARTD10/PARP10-Induced Apoptosis and Sensitizes Cancer Cells to DNA Damage.

University Of Oulu

Novel N-allyl/propargyl tetrahydroquinolines: Synthesis via Three-component Cationic Imino Diels-Alder Reaction, Binding Prediction, and Evaluation as Cholinesterase Inhibitors.

Universidad De Talcaa

Indolequinone inhibitors of NRH:quinone oxidoreductase 2. Characterization of the mechanism of inhibition in both cell-free and cellular systems.

University Of Colorado Denver

Drug design with a new transition state analog of the hydrated carbonyl: silicon-based inhibitors of the HIV protease.

State University Of New York

Benzo[c][2,7]naphthyridines as inhibitors of PDK-1.

Wyeth Research