287 articles for thisTarget
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Potent Body Weight-Lowering Effect of a Neuromedin U Receptor 2-selective PEGylated Peptide.
Takeda Pharmaceutical
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part II: Optimization of 4-(pyrrolidin-1-yl)benzonitrile derivatives.
Takeda Pharmaceutical
Discovery of 4-chloro-2-(2,4-dichloro-6-methylphenoxy)-1-methyl-7-(pentan-3-yl)-1H-benzimidazole, a novel CRF
Takeda Pharmaceutical
Parallel fluorescent probe synthesis based on the large-scale preparation of BODIPY FL propionic acid.
Takeda Pharmaceutical
Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure.
Takeda Pharmaceutical
Design, synthesis, and biological activity of novel, potent, and highly selective fused pyrimidine-2-carboxamide-4-one-based matrix metalloproteinase (MMP)-13 zinc-binding inhibitors.
Takeda Pharmaceutical
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH
Takeda Pharmaceutical
Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor.
Takeda Pharmaceutical
Novel approach of fragment-based lead discovery applied to renin inhibitors.
Takeda Pharmaceutical
Structure-based design of a new series of N-(piperidin-3-yl)pyrimidine-5-carboxamides as renin inhibitors.
Takeda Pharmaceutical
Design, synthesis, and biological evaluation of a novel series of peripheral-selective noradrenaline reuptake inhibitors - Part 3.
Takeda Pharmaceutical
Design and synthesis of potent and selective pyridazin-4(1H)-one-based PDE10A inhibitors interacting with Tyr683 in the PDE10A selectivity pocket.
Takeda Pharmaceutical
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.
Takeda Pharmaceutical
Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Activea1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities.
Takeda Pharmaceutical
Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel non-basic 1-(2H-indazole-5-yl)pyridin-2(1H)-one derivatives and mitigation of mutagenicity in Ames test.
Takeda Pharmaceutical
Design and Synthesis of Benzimidazoles As Novel Corticotropin-Releasing Factor 1 Receptor Antagonists.
Takeda Pharmaceutical
Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel 1-(1H-benzimidazol-6-yl)pyridin-2(1H)-one derivatives and design to avoid CYP3A4 time-dependent inhibition.
Takeda Pharmaceutical
Melanin-Concentrating Hormone Receptor 1 Antagonists Lacking an Aliphatic Amine: Synthesis and Structure-Activity Relationships of Novel 1-(Imidazo[1,2-a]pyridin-6-yl)pyridin-2(1H)-one Derivatives.
Takeda Pharmaceutical
Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors.
Takeda Pharmaceutical
Optimization of tetrahydronaphthalene inhibitors of Raf with selectivity over hERG.
Takeda Pharmaceutical
Design and synthesis of a novel 2-oxindole scaffold as a highly potent and brain-penetrant phosphodiesterase 10A inhibitor.
Takeda Pharmaceutical
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
Takeda Pharmaceutical
Design, synthesis and biological evaluation of a novel series of peripheral-selective noradrenaline reuptake inhibitor.
Takeda Pharmaceutical
MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors.
Takeda Pharmaceutical
Discovery of a Novel Series of N-Phenylindoline-5-sulfonamide Derivatives as Potent, Selective, and Orally Bioavailable Acyl CoA:Monoacylglycerol Acyltransferase-2 Inhibitors.
Takeda Pharmaceutical
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part I.
Takeda Pharmaceutical
Design, synthesis, and biological activities of 1-aryl-1,4-diazepan-2-one derivatives as novel triple reuptake inhibitors.
Takeda Pharmaceutical
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
Takeda Pharmaceutical
A simple and widely applicable hit validation strategy for protein-protein interaction inhibitors based on a quantitative ligand displacement assay.
Takeda Pharmaceutical
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1¿ binding site.
Takeda Pharmaceutical
Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists.
Takeda Pharmaceutical
Discovery of the first potent and orally available agonist of the orphan G-protein-coupled receptor 52.
Takeda Pharmaceutical
Discovery of potent Mcl-1/Bcl-xL dual inhibitors by using a hybridization strategy based on structural analysis of target proteins.
Takeda Pharmaceutical
Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.
Takeda Pharmaceutical
Design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors.
Takeda Pharmaceutical
Discovery of a novel series of indoline carbamate and indolinylpyrimidine derivatives as potent GPR119 agonists.
Takeda Pharmaceutical
Structure-based design, synthesis, and evaluation of imidazo[1,2-b]pyridazine and imidazo[1,2-a]pyridine derivatives as novel dual c-Met and VEGFR2 kinase inhibitors.
Takeda Pharmaceutical
Design, synthesis, and biological activities of novel hexahydropyrazino[1,2-a]indole derivatives as potent inhibitors of apoptosis (IAP) proteins antagonists with improved membrane permeability across MDR1 expressing cells.
Takeda Pharmaceutical
Design, synthesis, and biological evaluation of novel investigational nonapeptide KISS1R agonists with testosterone-suppressive activity.
Takeda Pharmaceutical
Design, synthesis, and structure-activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists.
Takeda Pharmaceutical
Design, stereoselective synthesis, and biological evaluation of novel tri-cyclic compounds as inhibitor of apoptosis proteins (IAP) antagonists.
Takeda Pharmaceutical
Synthetic studies of centromere-associated protein-E (CENP-E) inhibitors: 1.Exploration of fused bicyclic core scaffolds using electrostatic potential map.
Takeda Pharmaceutical
Design, synthesis, and evaluation of novel VEGFR2 kinase inhibitors: discovery of [1,2,4]triazolo[1,5-a]pyridine derivatives with slow dissociation kinetics.
Takeda Pharmaceutical
Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor.
Takeda Pharmaceutical
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.
Takeda Pharmaceutical
Discovery and characterization of novel allosteric FAK inhibitors.
Takeda Pharmaceutical
Structure-based discovery of cellular-active allosteric inhibitors of FAK.
Takeda Pharmaceutical
Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists.
Takeda Pharmaceutical
Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors.
Takeda Pharmaceutical
Structure-Based Approach for the Discovery of Pyrrolo[3,2-d]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors.
Takeda Pharmaceutical
Design and synthesis of potent inhibitor of apoptosis (IAP) proteins antagonists bearing an octahydropyrrolo[1,2-a]pyrazine scaffold as a novel proline mimetic.
Takeda Pharmaceutical
Discovery of pyrrolo[3,2-c]quinoline-4-one derivatives as novel hedgehog signaling inhibitors.
Takeda Pharmaceutical
Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors.
Takeda Pharmaceutical
Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors.
Takeda Pharmaceutical
Discovery of the investigational drug TAK-441, a pyrrolo[3,2-c]pyridine derivative, as a highly potent and orally active hedgehog signaling inhibitor: modification of the core skeleton for improved solubility.
Takeda Pharmaceutical
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.
Takeda Pharmaceutical
Trypsin resistance of a decapeptide KISS1R agonist containing an N¿-methylarginine substitution.
Takeda Pharmaceutical
Serum stability of selected decapeptide agonists of KISS1R using pseudopeptides.
Takeda Pharmaceutical
Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy.
Takeda Pharmaceutical
Symmetrical approach of spiro-pyrazolidinediones as acetyl-CoA carboxylase inhibitors.
Takeda Pharmaceutical
Synthesis, structure-activity relationship, and pharmacological studies of novel melanin-concentrating hormone receptor 1 antagonists 3-aminomethylquinolines: reducing human ether-a-go-go-related gene (hERG) associated liabilities.
Takeda Pharmaceutical
Optimization of (2,3-dihydro-1-benzofuran-3-yl)acetic acids: discovery of a non-free fatty acid-like, highly bioavailable G protein-coupled receptor 40/free fatty acid receptor 1 agonist as a glucose-dependent insulinotropic agent.
Takeda Pharmaceutical
Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders.
Takeda Pharmaceutical
Discovery of phenylpropanoic acid derivatives containing polar functionalities as potent and orally bioavailable G protein-coupled receptor 40 agonists for the treatment of type 2 diabetes.
Takeda Pharmaceutical
Design, synthesis, and structure-activity relationships of novel spiro-piperidines as acetyl-CoA carboxylase inhibitors.
Takeda Pharmaceutical
Melanin-concentrating hormone receptor 1 antagonists. Synthesis and structure-activity relationships of novel 3-(aminomethyl)quinolines.
Takeda Pharmaceutical
Identification of fused-ring alkanoic acids with improved pharmacokinetic profiles that act as G protein-coupled receptor 40/free fatty acid receptor 1 agonists.
Takeda Pharmaceutical
Structure-activity relationships and key structural feature of pyridyloxybenzene-acylsulfonamides as new, potent, and selective peroxisome proliferator-activated receptor (PPAR)¿ Agonists.
Takeda Pharmaceutical
Identification of 3-aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones: a new class of potent, selective, and orally active non-peptide dipeptidyl peptidase IV inhibitors that form a unique interaction with Lys554.
Takeda Pharmaceutical
17,20-lyase inhibitors. Part 4: design, synthesis and structure-activity relationships of naphthylmethylimidazole derivatives as novel 17,20-lyase inhibitors.
Takeda Pharmaceutical
Discovery of a 3-pyridylacetic acid derivative (TAK-100) as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor.
Takeda Pharmaceutical
2-acylamino-4,6-diphenylpyridine derivatives as novel GPR54 antagonists with good brain exposure and in vivo efficacy for plasma LH level in male rats.
Takeda Pharmaceutical
Synthesis and biological evaluation of the metabolites of 2-(1-{3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl}piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one.
Takeda Pharmaceutical
Docking model of drug binding to the human ether-à-go-go potassium channel guided by tandem dimer mutant patch-clamp data: a synergic approach.
Takeda Pharmaceutical
Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (2).
Takeda Pharmaceutical
Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.
Takeda Pharmaceutical
Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (1).
Takeda Pharmaceutical
Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors.
Takeda Pharmaceutical
Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists.
Takeda Pharmaceutical
Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists.
Takeda Pharmaceutical
Novel 3-phenylpiperidine-4-carboxamides as highly potent and orally long-acting neurokinin-1 receptor antagonists with reduced CYP3A induction.
Takeda Pharmaceutical
A new class of non-thiazolidinedione, non-carboxylic-acid-based highly selective peroxisome proliferator-activated receptor (PPAR)¿ agonists: design and synthesis of benzylpyrazole acylsulfonamides.
Takeda Pharmaceutical
Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
Takeda Pharmaceutical
Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists.
Takeda Pharmaceutical
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.
Takeda Pharmaceutical
Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer.
Takeda Pharmaceutical
Melanin-concentrating hormone receptor 1 antagonists: synthesis, structure-activity relationship, docking studies, and biological evaluation of 2,3,4,5-tetrahydro-1H-3-benzazepine derivatives.
Takeda Pharmaceutical
Design, structure-activity relationship, and highly efficient asymmetric synthesis of 3-phenyl-4-benzylaminopiperidine derivatives as novel neurokinin-1 receptor antagonists.
Takeda Pharmaceutical
Design, synthesis, and structure-activity relationships of spirolactones bearing 2-ureidobenzothiophene as acetyl-CoA carboxylases inhibitors.
Takeda Pharmaceutical
Discovery of spiropiperidine-based potent and selective Orexin-2 receptor antagonists.
Takeda Pharmaceutical
Discovery of potent, selective, orally active benzoxazepine-based Orexin-2 receptor antagonists.
Takeda Pharmaceutical
Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2.
Takeda Pharmaceutical
Discovery, synthesis, and structure-activity relationship of 6-aminomethyl-7,8-dihydronaphthalenes as human melanin-concentrating hormone receptor 1 antagonists.
Takeda Pharmaceutical
3-benzhydryl-4-piperidones as novel neurokinin-1 receptor antagonists and their efficient synthesis.
Takeda Pharmaceutical
Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554.
Takeda Pharmaceutical
Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor.
Takeda Pharmaceutical
Synthesis of a novel series of tricyclic dihydrofuran derivatives: discovery of 8,9-dihydrofuro[3,2-c]pyrazolo[1,5-a]pyridines as melatonin receptor (MT1/MT2) ligands.
Takeda Pharmaceutical
1,6-Dihydro-2H-indeno[5,4-b]furan derivatives: design, synthesis, and pharmacological characterization of a novel class of highly potent MT2-selective agonists.
Takeda Pharmaceutical
17,20-Lyase inhibitors. Part 3: Design, synthesis, and structure-activity relationships of biphenylylmethylimidazole derivatives as novel 17,20-lyase inhibitors.
Takeda Pharmaceutical
Discovery of pyrrolo[2,3-d]pyrimidin-4-ones as corticotropin-releasing factor 1 receptor antagonists with a carbonyl-based hydrogen bonding acceptor.
Takeda Pharmaceutical
Novel and potent calcium-sensing receptor antagonists: discovery of (5R)-N-[1-ethyl-1-(4-ethylphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide monotosylate (TAK-075) as an orally active bone anabolic agent.
Takeda Pharmaceutical
Design, synthesis, and biological activity of potent and orally available G protein-coupled receptor 40 agonists.
Takeda Pharmaceutical
Discovery of novel and potent orally active calcium-sensing receptor antagonists that stimulate pulselike parathyroid hormone secretion: synthesis and structure-activity relationships of tetrahydropyrazolopyrimidine derivatives.
Takeda Pharmaceutical
Design and synthesis of 3-pyridylacetamide derivatives as dipeptidyl peptidase IV (DPP-4) inhibitors targeting a bidentate interaction with Arg125.
Takeda Pharmaceutical
Synthesis and structure-activity relationship of tetrahydropyrazolopyrimidine derivatives--a novel structural class of potent calcium-sensing receptor antagonists.
Takeda Pharmaceutical
N-phenyl-N'-[4-(5H-pyrrolo[3,2-d]pyrimidin-4-yloxy)phenyl]ureas as novel inhibitors of VEGFR and FGFR kinases.
Takeda Pharmaceutical
Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine derivatives: novel VEGFR2 kinase inhibitors binding to inactive kinase conformation.
Takeda Pharmaceutical
Synthesis and structure-activity relationships of 2-acylamino-4,6-diphenylpyridine derivatives as novel antagonists of GPR54.
Takeda Pharmaceutical
Discovery of a tetrahydropyrimidin-2(1H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor.
Takeda Pharmaceutical
Novel acyl coenzyme A (CoA): diacylglycerol acyltransferase-1 inhibitors: synthesis and biological activities of diacylethylenediamine derivatives.
Takeda Pharmaceutical
2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.
Takeda Pharmaceutical
Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.
Takeda Pharmaceutical
Discovery of a Novel Series of Potent, Selective, Orally Available, and Brain-Penetrable C1s Inhibitors for Modulation of the Complement Pathway.
Takeda Pharmaceutical
Discovery of a novel series of medium-sized cyclic enteropeptidase inhibitors.
Takeda Pharmaceutical
Design, synthesis, and structure-activity relationship of TAK-418 and its derivatives as a novel series of LSD1 inhibitors with lowered risk of hematological side effects.
Takeda Pharmaceutical
New Series of Potent Allosteric Inhibitors of Deoxyhypusine Synthase.
Takeda Pharmaceutical
Design and synthesis of 6-methylpyridin-2-one derivatives as novel and potent GluN2A positive allosteric modulators for the treatment of cognitive impairment.
Takeda Pharmaceutical
Discovery of Soticlestat, a Potent and Selective Inhibitor for Cholesterol 24-Hydroxylase (CH24H).
Takeda Pharmaceutical
Discovery of a piperidine-4-carboxamide CCR5 antagonist (TAK-220) with highly potent Anti-HIV-1 activity.
Takeda Pharmaceutical
Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety.
Takeda Pharmaceutical
Photoredox-based late-stage functionalization in SAR study for in vivo potent glucosylceramide synthase inhibitor.
Takeda Pharmaceutical
Discovery of Pyrazolo[1,5-a]pyrazin-4-ones as Potent and Brain Penetrant GluN2A-Selective Positive Allosteric Modulators Reducing AMPA Receptor Binding Activity.
Takeda Pharmaceutical
Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent.
Takeda Pharmaceutical
Design, Synthesis, and Biological Evaluation of a Novel Series of 4-Guanidinobenzoate Derivatives as Enteropeptidase Inhibitors with Low Systemic Exposure for the Treatment of Obesity.
Takeda Pharmaceutical
Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist.
Takeda Pharmaceutical
Discovery of Brain-Penetrant Glucosylceramide Synthase Inhibitors with a Novel Pharmacophore.
Takeda Pharmaceutical
Discovery of Novel 3-Piperidinyl Pyridine Derivatives as Highly Potent and Selective Cholesterol 24-Hydroxylase (CH24H) Inhibitors.
Takeda Pharmaceutical
Discovery of a Potent and Orally Bioavailable Melatonin Receptor Agonist.
Takeda Pharmaceutical
Discovery of a novel series of GPR119 agonists: Design, synthesis, and biological evaluation of N-(Piperidin-4-yl)-N-(trifluoromethyl)pyrimidin-4-amine derivatives.
Takeda Pharmaceutical
Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2
Takeda Pharmaceutical
Discovery of a novel series of indolinylpyrimidine-based GPR119 agonists: Elimination of ether-a-go-go-related gene liability using a hydrogen bond acceptor-focused approach.
Takeda Pharmaceutical
Design, synthesis, and biological evaluation of a novel series of peripheral-selective noradrenaline reuptake inhibitors-Part 2.
Takeda Pharmaceutical
Design and synthesis of a monocyclic derivative as a selective ACC1 inhibitor by chemical modification of biphenyl ACC1/2 dual inhibitors.
Takeda Pharmaceutical
Discovery of 1,8-naphthyridin-2-one derivative as a potent and selective sphingomyelin synthase 2 inhibitor.
Takeda Pharmaceutical
Efficient synthesis of tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylates: Highly functionalized 2-pyrrolidinone enabling access to novel macrocyclic Tyk2 inhibitors.
Takeda Pharmaceutical
Discovery of a 7-arylaminobenzimidazole series as novel CRF1 receptor antagonists.
Takeda Pharmaceutical
T-3364366 Targets the Desaturase Domain of Delta-5 Desaturase with Nanomolar Potency and a Multihour Residence Time.
Takeda Pharmaceutical
Design and synthesis of fused bicyclic inhibitors targeting the L5 loop site of centromere-associated protein E.
Takeda Pharmaceutical
The identification and pharmacological evaluation of potent, selective and orally available ACC1 inhibitor.
Takeda Pharmaceutical
Discovery of Potent, Selective, and Brain-Penetrant 1 H-Pyrazol-5-yl-1 H-pyrrolo[2,3- b]pyridines as Anaplastic Lymphoma Kinase (ALK) Inhibitors.
Takeda Pharmaceutical
Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist.
Takeda Pharmaceutical
Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase.
Takeda Pharmaceutical
Design and synthesis of a novel 1H-pyrrolo[3,2-b]pyridine-3-carboxamide derivative as an orally available ACC1 inhibitor.
Takeda Pharmaceutical
A new class of pentapeptide KISS1 receptor agonists with hypothalamic-pituitary-gonadal axis activation.
Takeda Pharmaceutical
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.
Takeda Pharmaceutical
Novel triple reuptake inhibitors with low risk of CAD associated liabilities: design, synthesis and biological activities of 4-[(1S)-1-(3,4-dichlorophenyl)-2-methoxyethyl]piperidine and related compounds.
Takeda Pharmaceutical
The synergic modeling for the binding of fluoroquinolone antibiotics to the hERG potassium channel.
Takeda Pharmaceutical
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 2. Synthesis and characterization of a novel imide-type prodrug for improving oral absorption.
Takeda Pharmaceutical
Identification of a novel series of potent and selective CCR6 inhibitors as biological probes.
Takeda Pharmaceutical
Discovery of novel serine palmitoyltransferase inhibitors as cancer therapeutic agents.
Takeda Pharmaceutical
Design and synthesis of 1-(1-benzothiophen-7-yl)-1H-pyrazole, a novel series of G protein-coupled receptor 52 (GPR52) agonists.
Takeda Pharmaceutical
Discovery of 1,2,3,4-tetrahydropyrimido[1,2-a]benzimidazoles as novel class of corticotropin releasing factor 1 receptor antagonists.
Takeda Pharmaceutical
Identification of novel quinazolinedione derivatives as RORγt inverse agonist.
Takeda Pharmaceutical
Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors.
Takeda Pharmaceutical
Antiobesity and emetic effects of a short-length peptide YY analog and its PEGylated and alkylated derivatives.
Takeda Pharmaceutical
Design, Synthesis, and Evaluation of Piperazinyl Pyrrolidin-2-ones as a Novel Series of Reversible Monoacylglycerol Lipase Inhibitors.
Takeda Pharmaceutical
Identification of 3,4-dihydro-2H-thiochromene 1,1-dioxide derivatives with a phenoxyethylamine group as highly potent and selective α
Takeda Pharmaceutical
Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds.
Takeda Pharmaceutical
Discovery of orally efficacious RORγt inverse agonists. Part 2: Design, synthesis, and biological evaluation of novel tetrahydroisoquinoline derivatives.
Takeda Pharmaceutical
Design and synthesis of a novel series of orally active, selective somatostatin receptor 2 agonists for the treatment of type 2 diabetes.
Takeda Pharmaceutical
Highly potent antiobesity effect of a short-length peptide YY analog in mice.
Takeda Pharmaceutical
Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones.
Takeda Pharmaceutical
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 and characterization of selective human sphingomyelin synthase 2 inhibitors.
Takeda Pharmaceutical
Targeting the Allosteric Site of Oncoprotein BCR-ABL as an Alternative Strategy for Effective Target Protein Degradation.
Takeda Pharmaceutical
Discovery of benzimidazole derivatives as orally active renin inhibitors: Optimization of 3,5-disubstituted piperidine to improve pharmacokinetic profile.
Takeda Pharmaceutical
Potent antiobesity effect of a short-length peptide YY-analogue continuously administered in mice.
Takeda Pharmaceutical
Discovery of novel somatostatin receptor subtype 5 (SSTR5) antagonists: Pharmacological studies and design to improve pharmacokinetic profiles and human Ether-a-go-go-related gene (hERG) inhibition.
Takeda Pharmaceutical
Discovery of Novel and Potent Stearoyl Coenzyme A Desaturase 1 (SCD1) Inhibitors as Anticancer Agents.
Takeda Pharmaceutical
Discovery of a B-Cell Lymphoma 6 Protein-Protein Interaction Inhibitor by a Biophysics-Driven Fragment-Based Approach.
Takeda Pharmaceutical
Discovery of Novel 1,4-Diacylpiperazines as Selective and Cell-Active eIF4A3 Inhibitors.
Takeda Pharmaceutical
Investigation on cellular uptake and pharmacodynamics of DOCK2-inhibitory peptides conjugated with cell-penetrating peptides.
Takeda Pharmaceutical
Discovery of a novel B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor by utilizing structure-based drug design.
Takeda Pharmaceutical
Discovery of spiro[indole-3,2'-pyrrolidin]-2(1H)-one based inhibitors targeting Brr2, a core component of the U5 snRNP.
Takeda Pharmaceutical
Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders.
Takeda Pharmaceutical
Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders.
Takeda Pharmaceutical
Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure.
Takeda Pharmaceutical
Crystal Structure of a Human K-Ras G12D Mutant in Complex with GDP and the Cyclic Inhibitory Peptide KRpep-2d.
Takeda Pharmaceutical
Antiobesity Effect of a Short-Length Peptide YY Analogue after Continuous Administration in Mice.
Takeda Pharmaceutical
A potent and selective natriuretic peptide receptor-3 blocker 11-mer peptide created by hybridization of musclin and atrial natriuretic peptide.
Takeda Pharmaceutical
Design of potent dipeptidyl peptidase IV (DPP-4) inhibitors by employing a strategy to form a salt bridge with Lys554.
Takeda Pharmaceutical
2-Aminomethylthieno[3,2-d]pyrimidin-4(3H)-ones bearing 3-methylpyrazole hinge binding moiety: Highly potent, selective, and time-dependent inhibitors of Cdc7 kinase.
Takeda Pharmaceutical
Design, synthesis, and pharmacological evaluation of 4-azolyl-benzamide derivatives as novel GPR52 agonists.
Takeda Pharmaceutical
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
Discovery of Novel Selective Acetyl-CoA Carboxylase (ACC) 1 Inhibitors.
Takeda Pharmaceutical
Discovery of 3,5-Diphenyl-4-methyl-1,3-oxazolidin-2-ones as Novel, Potent, and Orally AvailableΔ-5 Desaturase (D5D) Inhibitors.
Takeda Pharmaceutical
Discovery of 7-Oxo-2,4,5,7-tetrahydro-6 H-pyrazolo[3,4- c]pyridine Derivatives as Potent, Orally Available, and Brain-Penetrating Receptor Interacting Protein 1 (RIP1) Kinase Inhibitors: Analysis of Structure-Kinetic Relationships.
Takeda Pharmaceutical
Investigation of the structural requirements of K-Ras(G12D) selective inhibitory peptide KRpep-2d using alanine scans and cysteine bridging.
Takeda Pharmaceutical
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs) Part III: Discovery of 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2f as a clinical candidate.
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
Potent and selective oxytocin receptor agonists without disulfide bridges.
Takeda Pharmaceutical
Practical application of 3-substituted-2,6-difluoropyridines in drug discovery: Facile synthesis of novel protein kinase C theta inhibitors.
Takeda Pharmaceutical
5-[7-(3,4-DIHYDRO-1H-ISOQUINOLINE-2-CARBONYL)-1,2,3,4 TETRAHYDROISOQUINOLIN-6-YL]-1H-PYRROLE-3-CARBOXAMIDE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USES AS PRO-APOPTOTIC AGENTS
Les Laboratoires Servier
PHARMACEUTICAL COMPOUNDS AND METHODS OF MAKING AND USING THE SAME
Athos Therapeutics
FUSED IMIDAZOLE DERIVATIVE, PREPARATION METHOD THEREFOR, AND MEDICAL USE THEREOF
Jiangsu Hengrui Medicine
Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, Rasopathies, and fibrotic disease
Shy Therapeutics
Phenyl and pyridinyl substituted imidazoles as modulators of RORγT
Janssen Pharmaceutica
Alpha-hydroxy phenylacetic acid pharmacophore or bioisostere Mcl-1 protein antagonists
Amgen
Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors
Astrazeneca
(S)-2-(1-cyclopropylethyl)-5-(4-methyl-2-((6-(2-oxopyrrolidin-1-yl)pyridin-2-yl)amino) thiazol-5-yl)-7-(methylsulfonyl)isoindolin-1-one as a phosphatidylinositol 3-kinase inhibitor
Astrazeneca
Substituted N-[2-(4-phenoxypiperidin-1-yl)-2-(1,3-thiazol-5-yl)ethyl]benzamide and N-[2-(4-benzyloxypiperidin-1-yl)-2-(1,3-thiazol-5-yl)ethyl]benzamide derivatives P2X7 receptor antagonists
Axxam
Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
Saint Louis University
Discovery of potent inhibitors of PLproCoV2 by screening a library of selenium-containing compounds
University Ofamsterdam
Compositions and methods for treating neoplasia, inflammatory disease and other disorders
Dana-Farber Cancer Institute
3-substituted estra-1,3,5(10),16-tetraene derivatives, methods for the production thereof, pharmaceutical preparations containing same, and use thereof for the production of medicaments
Bayer Pharma Aktiengesellschaft
4-alkoxy/aralkoxy-5-substituted-pyrrolopyrimidine compounds as TAK1 inhibitors in disease treatment
Confluence Life Sciences
Glucokinase activator compounds, compositions containing such compounds, and methods of treatment
Merck Sharp & Dohme
Inhibition of mammalian carbonic anhydrases I-XIV with grayanotoxin III: solution and in silico studies.
University of Calgary
Novel coumarins and benzocoumarins acting as isoform-selective inhibitors against the tumor-associated carbonic anhydrase IX.
S.G.S.I.T.S.
Phenolic phytochemical displaying SARS-CoV papain-like protease inhibition from the seeds of Psoralea corylifolia.
Gyeongsang National University
Evaluation of a dithiocarbamate derivative as an inhibitor of human glutaredoxin-1.
South Dakota State University
Compounds act at multiple prostaglandin receptors giving a general anti-inflammatory response
Allergan
Synthesis and binding study of certain 6-arylalkanamides as molecular probes for cannabinoid receptor subtypes.
Cairo University
Inhibitory effect of novel pyrazole carboxamide derivatives on human carbonic anhydrase enzyme.
Dumlupinar University
Design, synthesis, and biological evaluation of pyrimidine derivatives as potential inhibitors of human calcium/calmodulin-dependent protein kinase IV.
B.R. Ambedkar Bihar University
Fragment Profiling Approach to Inhibitors of the Orphan M. tuberculosis P450 CYP144A1.
University of Cambridge
1,4-dihydro-naphthyridine derivative and pharmaceutical composition and use thereof
Jiangsu Simovay Pharmaceutical
Tricyclic amino containing compounds for treatment or prevention of symptoms associated with endocrine dysfunction
Emory University
Identifying New Drug Targets for Potent Phospholipase D Inhibitors: Combining Sequence Alignment, Molecular Docking, and Enzyme Activity/Binding Assays.
Roxbury Community College
Synthesis of 4-[2-(3,4-dimethoxybenzyl)cyclopentyl]-1,2-dimethoxybenzene Derivatives and Evaluations of Their Carbonic Anhydrase Isoenzymes Inhibitory Effects.
Ataturk University
Substituted piperidinyl-pyridazinyl derivatives useful as SCD 1 inhibitors
Janssen Pharmaceutica
Substituted 3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals
Sanofi
Design and synthesis of newer potential 4-(N-acetylamino)phenol derived piperazine derivatives as potential cognition enhancers.
Panjab University
Use of azaphilone compounds for the modulation of the activity of a nuclear hormone receptor
Food Industry Research and Development Institute
Inhibitors of dimethylarginine dimethylaminohydrolase
Christian-Albrechts-Universitaet Zu Kiel
Identification of Inhibitors of PvdQ, an Enzyme Involved in the Synthesis of the Siderophore Pyoverdine.
The Broad Institute , Cambridge, Massachusetts 02142, United States
17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
Universitaet Des Saarlandes
Synthesis and biological evaluation of new donepezil-like Thiaindanones as AChE inhibitors.
Centre D'Etudes Et De Recherche Sur Le MÉDicament De Normandie
Desensitization of the human motilin receptor by motilides.
Katholieke Universiteit Leuven
Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen.
Harvard Medical School
A tertiary alcohol analog of gamma-hydroxybutyric acid as a specific gamma-hydroxybutyric acid receptor ligand.
University of Maryland
Mechanisms of Osteoclastogenesis Inhibition by a Novel Class of Biphenyl-Type Cannabinoid CB(2) Receptor Inverse Agonists.
University of Bern
Novel small-molecule inhibitors of anthrax lethal factor identified by high-throughput screening.
Montana State University