39 articles for thisTarget
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Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries.
Chugai Pharmaceutical
Discovery of [5-Amino-1-(2-methyl-3H-benzimidazol-5-yl)pyrazol-4-yl]-(1H-indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.
Chugai Pharmaceutical
Discovery of a potent and highly selective transforming growth factorß receptor-associated kinase 1 (TAK1) inhibitor by structure based drug design (SBDD).
Chugai Pharmaceutical
Optimization of the phenylurea moiety in a phosphoinositide 3-kinase (PI3K) inhibitor to improve water solubility and the PK profile by introducing a solubilizing group and ortho substituents.
Chugai Pharmaceutical
Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning.
Chugai Pharmaceutical
The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors.
Chugai Pharmaceutical
Lead optimization of a dihydropyrrolopyrimidine inhibitor against phosphoinositide 3-kinase (PI3K) to improve the phenol glucuronic acid conjugation.
Chugai Pharmaceutical
New description of protein-ligand interactions using a spherical self-organizing map.
Chugai Pharmaceutical
Design and evaluation of azaindole-substituted N-hydroxypyridones as glyoxalase I inhibitors.
Chugai Pharmaceutical
Discovery of tofogliflozin, a novel C-arylglucoside with an O-spiroketal ring system, as a highly selective sodium glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.
Chugai Pharmaceutical
C-Aryl 5a-carba-ß-d-glucopyranosides as novel sodium glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Chugai Pharmaceutical
Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
Chugai Pharmaceutical
Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists.
Chugai Pharmaceutical
Discovery of 7alpha-substituted dihydrotestosterones as androgen receptor pure antagonists and their structure-activity relationships.
Chugai Pharmaceutical
Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation.
Chugai Pharmaceutical
Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802).
Chugai Pharmaceutical
Design and synthesis of novel macrocyclic 2-amino-6-arylpyrimidine Hsp90 inhibitors.
Chugai Pharmaceutical
Lead generation of heat shock protein 90 inhibitors by a combination of fragment-based approach, virtual screening, and structure-based drug design.
Chugai Pharmaceutical
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.
Chugai Pharmaceutical
5a-Carba-ß-D-glucopyranose derivatives as novel sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Chugai Pharmaceutical
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.
Chugai Pharmaceutical
Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799.
Chugai Pharmaceutical
Design and synthesis of novel allosteric MEK inhibitor CH4987655 as an orally available anticancer agent.
Chugai Pharmaceutical
Host sphingolipid biosynthesis as a target for hepatitis C virus therapy.
Chugai Pharmaceutical
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.
Chugai Pharmaceutical
Discovery of novel motilin antagonists: Conversion of tetrapeptide leads to orally available peptidomimetics.
Chugai Pharmaceutical
Synthesis of new camptothecin analogs with improved antitumor activities.
Chugai Pharmaceutical
Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination.
Chugai Pharmaceutical
Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists.
Chugai Pharmaceutical
Discovery of CH7057288 as an Orally Bioavailable, Selective, and Potent pan-TRK Inhibitor.
Chugai Pharmaceutical
Design and synthesis of motilin antagonists derived from the [1-4] fragment of porcine motilin.
Chugai Pharmaceutical
Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 1. 2-(3, 5-di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones.
Chugai Pharmaceutical
Lead Optimization and Avoidance of Reactive Metabolite Leading to PCO371, a Potent, Selective, and Orally Available Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist.
Chugai Pharmaceutical
Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability.
Chugai Pharmaceutical
Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. 2. 4-(3-Pyridyl)-1(2H)-phthalazinones.
Chugai Pharmaceutical
Design and synthesis of 2-amino-6-(1H,3H-benzo[de]isochromen-6-yl)-1,3,5-triazines as novel Hsp90 inhibitors.
Chugai Pharmaceutical
Fluorine Scanning by Nonselective Fluorination: Enhancing Raf/MEK Inhibition while Keeping Physicochemical Properties.
Chugai Pharmaceutical
Synthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors.
Chugai Pharmaceutical