127 articles for NS Gray
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
A benzo[b]thiophene-based selective type 4 S1P receptor agonist.
Harvard Medical School
Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor.
Harvard Medical School
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase
Genomics Institute of The Novartis Research Foundation
X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor.
University of Oxford
Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator.
Genomics Institute of The Novartis Research Foundation
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.
Glaxosmithkline
Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1.
TBA
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.
University of California
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
Harvard Medical School
Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors.
TBA
Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability.
Dana-Farber Cancer Institute
Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.
Dana-Farber Cancer Institute
Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer.
Dana-Farber Cancer Institute
Rational design of inhibitors that bind to inactive kinase conformations.
Novartis Research Foundation
Allosteric inhibitors of Bcr-abl-dependent cell proliferation.
Genomics Institute of The Novartis Research Foundation
A type-II kinase inhibitor capable of inhibiting the T315I"gatekeeper" mutant of Bcr-Abl.
Harvard Medical School
Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.
Genomics Institute of The Novartis Research Foundation
Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.
Genomics Institute of The Novartis Research Foundation
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.
The Scripps Research Institute
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.
Genomics Institute of The Novartis Research Foundation
Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration.
Xiamen University
Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases.
University of Dundee
Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2).
Harvard Medical School
Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones.
Harvard Medical School
Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.
The Scripps Research Institute
Discovery of bivalent small molecule degraders of cyclin-dependent kinase 7 (CDK7).
Stanford University
Discovery of Potent Antimalarial Type II Kinase Inhibitors with Selectivity over Human Kinases.
Stanford University
ZNL0325, a Pyrazolopyrimidine-Based Covalent Probe, Demonstrates an Alternative Binding Mode for Kinases.
Stanford University
Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions.
Dana-Farber Cancer Institute
Development of a Covalent Inhibitor of c-Jun N-Terminal Protein Kinase (JNK) 2/3 with Selectivity over JNK1.
Stanford University
Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC.
Dana-Farber Cancer Institute
Synthesis and Structure-Activity relationships of cyclin-dependent kinase 11 inhibitors based on a diaminothiazole scaffold.
Stanford University
Novel Macrocyclic Peptidomimetics Targeting the Polo-Box Domain of Polo-Like Kinase 1.
Korea University
Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma.
Harvard Medical School
Development of Highly Potent and Selective Pyrazolopyridine Inhibitor of CDK8/19.
Dana-Farber Cancer Institute
Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma.
Dana-Farber Cancer Institute
Discovery of a series of benzopyrimidodiazepinone TNK2 inhibitors via scaffold morphing.
Dana-Farber Cancer Institute
Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor.
Dana-Farber Cancer Institute
Discovery of estrogen sulfotransferase inhibitors from a purine library screen.
University of California
Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface.
Dana-Farber Cancer Institute
Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6
Harvard Medical School
Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13.
Harvard Medical School
Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14.
Harvard Medical School
Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors.
Dana-Farber Cancer Institute
Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine.
Harvard Medical School
Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors.
Dana-Farber Cancer Institute
Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold.
Dana Farber Cancer Institute
Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.
Dana-Farber Cancer Institute
Synthesis and biological evaluation of myoseverin derivatives: microtubule assembly inhibitors.
New York University
First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia.
Korea University
Characterization of a highly selective inhibitor of the Aurora kinases.
Harvard Medical School
Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK).
Harvard Medical School
Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors.
Uit The Arctic University of Norway
Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8.
Dana-Farber Cancer Institute
Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors.
University of Science and Technology of China
Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors.
Dana-Farber Cancer Institute
Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent.
Dana-Farber Cancer Institute
NOVEL BENZOFURANYL HYDROXYPHENYL METHANONE DERIVATIVE COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
Innovo Therapeutics
SUBSTITUTED 6,7-DIHYDRO-5H-BENZO[7]ANNULENE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOF
Sanofi
3-[(1H-PYRAZOL-4-YL)OXY]PYRAZIN-2-AMINE COMPOUNDS AS HPK1 INHIBITOR AND USE THEREOF
BeiGene
PROTEASE INHIBITORS FOR TREATING OR PREVENTING CORONAVIRUS INFECTION
Merck Sharp & Dohme
Crystalline succinate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine as a Syk inhibitor
Kronos Bio
OXAZOLE, OXADIAZOLE, AND INDOLE DERIVATIVES FOR THE INHIBITION OF USP28
Carmot Therapeutics
Nitrogen-Containing Heterocyclic Compound, Pharmaceutical Compositions thereof and Use thereof
280 Bio
FUSED TETRACYCLIC QUINAZOLINE DERIVATIVES AS INHIBITORS OF ERBB2
Enliven Therapeutics
Therapeutic agent for non-motor symptoms associated with Parkinson's disease
Sumitomo Pharma
Fused piperidinyl bicyclic and related compounds as modulators of C5A receptor
Inflarx
N4-hydroxycytidine and derivatives and anti-viral uses related thereto
Emory University
Quinazolinones and azaquinazolinones as ubiquitin-specific protease 7 inhibitors
Valo Early Discovery
6-aryl-7-substituted-3-(1H-pyrazol-5-yl)-7H-[1,2,4]triazolo[3,4-B][1,3,4]thiadiazines as inhibitors of the STAT3 pathway with anti-proliferative activity
University of Pittsburgh
2,4-disubstituted 7H-pyrrolo[2,3-d]pyrimidine derivative, preparation method and medicinal use thereof
Shanghai Haiyan Pharmaceutical Technology
Heterocyclic GSK-3 allosteric modulators
Consejo Superior de Investigaciones Cientificas (CSIC)
Isatin based Schiff bases as inhibitors of a-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies.
Hazara University
(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives, preparation thereof and pharmaceutical use thereof as AKT(PKB) phosphorylation inhibitors
Sanofi
Opioids and efflux transporters. Part 2: P-glycoprotein substrate activity of 3- and 6-substituted morphine analogs.
University of Maryland
Modulation of Anopheles gambiae Epsilon glutathione transferase activity by plant natural products in vitro.
University of Zimbabwe
Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
University of Arizona
Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.
Amgen
Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles.
Wyeth Research
Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.
Wyeth Research
Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity.
F. Hoffmann-La Roche