237 articles for Q Liu
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Discovery of 2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) Kinase Inhibitor.
High Magnetic Field Laboratory
Novel dabigatran derivatives with a fluorine atom at the C-2 position of the terminal benzene ring: Design, synthesis and anticoagulant activity evaluation.
Shanghai Institute of Technology
Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-ß-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease.
Sichuan University
Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding.
High Magnetic Field Laboratory
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
China Pharmaceutical University
Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locke
Bristol-Myers Squibb Research and Development
Structural and Thermodynamic Characterization of Protein-Ligand Interactions Formed between Lipoprotein-Associated Phospholipase A2 and Inhibitors.
Shanghaitech University
Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs).
Chinese Academy of Sciences
Discovery of 6-(difluoro(6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b][1,2,4]triazin-3-yl)methyl)quinoline as a highly potent and selective c-Met inhibitor.
Chinese Academy of Sciences (Cas)
Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia.
High Magnetic Field Laboratory
Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents.
Sun Yat-Sen University
Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia.
Chinese Academy of Sciences
Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).
Bristol-Myers Squibb Pharmaceutical Research Institute
Benzylated and prenylated flavonoids from the root barks of Cudrania tricuspidata with pancreatic lipase inhibitory activity.
Chungbuk National University
Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant ROR¿t Inhibitors.
Fudan University
Discovery of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as potent ROR¿t inverse agonists.
Fudan University
Design, synthesis and evaluation of chromone-2-carboxamido-alkylbenzylamines as multifunctional agents for the treatment of Alzheimer's disease.
Sichuan University
9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.
Bristol-Myers Squibb
Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease.
Sichuan University
Involvement of organic anion-transporting polypeptides in the hepatic uptake of dioscin in rats and humans.
Dalian Medical University
Pancreatic lipase inhibitory constituents from Morus alba leaves and optimization for extraction conditions.
Chungbuk National University
Multifunctional scutellarin-rivastigmine hybrids with cholinergic, antioxidant, biometal chelating and neuroprotective properties for the treatment of Alzheimer's disease.
Sichuan University
Novel fatty acid binding protein 4 (FABP4) inhibitors: virtual screening, synthesis and crystal structure determination.
Chinese Academy of Sciences
Development of 2-aminooxazoline 3-azaxanthenes as orally efficaciousß-secretase inhibitors for the potential treatment of Alzheimer's disease.
Amgen
Bioactive diterpenoids and flavonoids from the aerial parts of Scoparia dulcis.
Institute of Chinese Materia Medica
Discovery of Anilinopyrimidines as Dual Inhibitors of c-Met and VEGFR-2: Synthesis, SAR, and Cellular Activity.
Shanghai Institute of Materia Medica
Structure-assisted discovery of the first non-retinoid ligands for Retinol-Binding Protein 4.
Amgen
Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2.
University of Copenhagen
Synthesis and evaluation of several oleanolic acid glycoconjugates as protein tyrosine phosphatase 1B inhibitors.
North-West University
Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
Sun Yat-Sen University
Design, synthesis and evaluation of genistein-O-alkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease.
Sichuan University
Discovery of Tertiary Amine and Indole Derivatives as Potent RORγt Inverse Agonists.
Glaxosmithkline
Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent ROR¿t inhibitors.
Glaxosmithkline
Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
Novartis Institutes For Biomedical Research
Discovery of 2-methylpyridine-based biaryl amides as¿-secretase modulators for the treatment of Alzheimer's disease.
Amgen
Aminopyrazole-Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies.
Amgen
Potent and Orally Bioavailable GPR142 Agonists as Novel Insulin Secretagogues for the Treatment of Type 2 Diabetes.
Daiichi Sankyo
Design, synthesis, and biological evaluation of a series of benzo[de][1,7]naphthyridin-7(8H)-ones bearing a functionalized longer chain appendage as novel PARP1 inhibitors.
Chinese Academy of Sciences
Effect of daurisoline on HERG channel electrophysiological function and protein expression.
Huazhong University of Science and Technology
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).
Glaxosmithkline
Phenylalanine derivatives as GPR142 agonists for the treatment of type II diabetes.
Amgen
Cyclobutane derivatives as novel nonpeptidic small molecule agonists of glucagon-like peptide-1 receptor.
The National Center For Drug Screening
Multisubstituted quinoxalines and pyrido[2,3-d]pyrimidines: synthesis and SAR study as tyrosine kinase c-Met inhibitors.
China Pharmaceutical University
Identification of benzoxazole analogs as novel, S1P(3) sparing S1P(1) agonists.
Glaxosmithkline
A new pancreatic lipase inhibitor from Broussonetia kanzinoki.
Chungbuk National University
Novel L-xylose derivatives as selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Lexicon Pharmaceuticals
Identification of novel, exosite-binding matrix metalloproteinase-13 inhibitor scaffolds.
Scripps Florida
Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability.
Dana-Farber Cancer Institute
3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation.
Amgen
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.
Glaxosmithkline
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
The discovery of potent inhibitors of aldosterone synthase that exhibit selectivity over 11-beta-hydroxylase.
Novartis Institutes For Biomedical Research
Aryl sulfonamides containing tetralin allylic amines as potent and selective bradykinin B1 receptor antagonists.
Amgen
Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.
Amgen
Lead optimization and structure-based design of potent and bioavailable deoxycytidine kinase inhibitors.
Lexicon Pharmaceuticals
5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase.
Lexicon Pharmaceuticals
Substituted 3-(4-(1,3,5-triazin-2-yl)-phenyl)-2-aminopropanoic acids as novel tryptophan hydroxylase inhibitors.
Lexicon Pharmaceuticals
Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma.
Lexicon Pharmaceuticals
Inhibition of sphingosine-1-phosphate lyase for the treatment of autoimmune disorders.
Lexicon Pharmaceuticals
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
Amgen
Modulation of peripheral serotonin levels by novel tryptophan hydroxylase inhibitors for the potential treatment of functional gastrointestinal disorders.
Lexicon Pharmaceuticals
A nonpeptidic agonist of glucagon-like peptide 1 receptors with efficacy in diabetic db/db mice.
National Center For Drug Screening
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum.
Chinese Academy of Sciences
Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase.
GlaxoSmithKline
Discovery of dihydropyridinone derivative as a covalent EZH2 degrader.
Chinese Academy of Sciences
Discovery of Pyrazolo[1,5-a]pyrimidine derivative as a potent and selective PI3Kγ/δ dual inhibitor.
Chinese Academy of Sciences
Structure-based screening, optimization and biological evaluation of novel chrysin-based derivatives as selective PPARγ modulators for the treatment of T2DM and hepatic steatosis.
Guangzhou Medical University
Re-Evaluating PIN1 as a Therapeutic Target in Oncology Using Neutral Inhibitors and PROTACs.
Sichuan Kelun-Biotech Biopharmaceutical
Discovery of Pyrazolo[1,5-a]pyridine Derivatives as Potent and Selective PI3Kγ/δ Inhibitors.
Chinese Academy of Sciences
Development of Degraders of Cyclin-Dependent Kinases 4 and 6 Based on Rational Drug Design.
East China Normal University
Discovery of a Covalent Inhibitor That Overcame Resistance to Venetoclax in AML Cells Overexpressing BFL-1.
University of Chinese Academy of Sciences
Discovery of novel SOS1 inhibitors using machine learning.
University of Nottingham Ningbo China
Application of Novel Degraders Employing Autophagy for Expediting Medicinal Research.
Chengdu University of Traditional Chinese Medicine
Structure-based discovery of IHMT-IDH1-053 as a potent irreversible IDH1 mutant selective inhibitor.
Chinese Academy of Sciences
Ligand-Directed Photodegradation of Interacting Proteins: Oxidative HER2/HER3 Heterodimer Degradation with a Lapatinib-Derived Photosensitizer.
Shandong University
Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.
Amgen
Discovery of Pyrrolo[2,3-d]pyrimidine derivatives as potent and selective colony stimulating factor 1 receptor kinase inhibitors.
Chinese Academy of Sciences
Modified Podophyllotoxin Phenoxyacetamide Phenylacetate Derivatives: Tubulin/AKT1 Dual-Targeting and Potential Anticancer Agents for Human NSCLC.
Changzhou University
Discovery of N-(4-(6-Acetamidopyrimidin-4-yloxy)phenyl)-2-(2-(trifluoromethyl)phenyl)acetamide (CHMFL-FLT3-335) as a Potent FMS-like Tyrosine Kinase 3 Internal Tandem Duplication (FLT3-ITD) Mutant Selective Inhibitor for Acute Myeloid Leukemia.
Hefei Institutes of Physical Science
Design, synthesis, and biological evaluation of novel HDAC inhibitors with a 3-(benzazol-2-yl)quinoxaline framework.
Southeast University
Combination of NSAIDs with donepezil as multi-target directed ligands for the treatment of Alzheimer's disease.
Southeast University
Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors.
East China University of Science & Technology
Clofazimine derivatives as potent broad-spectrum antiviral agents with dual-target mechanism.
Peking Union Medical College
Discovery of BP3 as an efficacious proteolysis targeting chimera (PROTAC) degrader of HSP90 for treating breast cancer.
Fujian Medical University (Fmu)
A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core.
Amgen
Discovery and radiosensitization research of ursolic acid derivatives as SENP1 inhibitors.
Peking Union Medical College
Discovery of IHMT-MST1-58 as a Novel, Potent, and Selective MST1 Inhibitor for the Treatment of Type 1/2 Diabetes.
Chinese Academy of Sciences
Discovery of Natural Ursane-type SENP1 Inhibitors and the Platinum Resistance Reversal Activity Against Human Ovarian Cancer Cells: A Structure-Activity Relationship Study.
Peking Union Medical College
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.
Amgen
Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.
Amgen
Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway.
Southeast University
Identification of the Benzoimidazole Compound as a Selective FLT3 Inhibitor by Cell-Based High-Throughput Screening of a Diversity Library.
Sun Yat-Sen University Cancer Center
Discovery of Highly Potent and Selective IRAK1 Degraders to Probe Scaffolding Functions of IRAK1 in ABC DLBCL.
Janssen Research & Development
Discovery of memantyl urea derivatives as potent soluble epoxide hydrolase inhibitors against lipopolysaccharide-induced sepsis.
Shenyang Pharmaceutical University
Synthesis of methylphenidate analogues and their binding affinities at dopamine and serotonin transport sites.
State University of New York
Design, Synthesis, and Biological Evaluation of APN and AKT Dual-Target Inhibitors.
Shandong University
Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors.
Southeast University
Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate.
Chinese Academy of Sciences
Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants.
Chinese Academy of Sciences
Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II.
Guilford Pharmaceuticals
Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
Guilford Pharmaceuticals
Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer activity.
Chongqing University
Discovery of 6-(7-Nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol Derivatives as Glutathione Transferase Inhibitors with Favorable Selectivity and Tolerated Toxicity.
Southeast University
Structure-based virtual screening and biological evaluation of novel non-bisphosphonate farnesyl pyrophosphate synthase inhibitors.
Jiangsu Institute of Nuclear Medicine
Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors.
Gsk Pharmaceuticals R&D
Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.
Bristol Myers Squibb
Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity.
Southeast University
Discovery of 6'-chloro-N-methyl-5'-(phenylsulfonamido)-[3,3'-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium.
Chinese Academy of Sciences
Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach.
Bristol Myers Squibb
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.
Bristol Myers Squibb
Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).
Bristol-Myers Squibb Research and Development
3-Arylpropionylhydroxamic acid derivatives as Helicobacter pylori urease inhibitors: Synthesis, molecular docking and biological evaluation.
Jishou University
Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kinase.
High Magnetic Field Laboratory
Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).
Bristol-Myers Squibb Research and Development
Discovery of small molecule inhibitors of human uridine-cytidine kinase 2 by high-throughput screening.
Stanford University
Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants including T315I for chronic myeloid leukemia.
Chinese Academy of Sciences
Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.
University of Connecticut
Synthesis and Structure-Activity Relationship Correlations of Gnidimacrin Derivatives as Potent HIV-1 Inhibitors and HIV Latency Reversing Agents.
Toho University
5-Substituted-N-pyridazinylbenzamides as potent and selective LRRK2 inhibitors: Improved brain unbound fraction enables efficacy.
Gsk Pharmaceuticals R&D
Design, synthesis and biological evaluation of novel 4-anilinoquinazoline derivatives as hypoxia-selective EGFR and VEGFR-2 dual inhibitors.
Peking Union Medical College
Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.
TBA
Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin Inhibitors.
Novartis Institutes For Biomedical Research
Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Bristol-Myers Squibb
Discovery of Benzamidine- and 1-Aminoisoquinoline-Based Human MAS-Related G-Protein-Coupled Receptor X1 (MRGPRX1) Agonists.
Eisai
Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor.
Novartis Institutes For Biomedical Research
Peptidomimetics of Arg-Phe-NH2 as small molecule agonists of Mas-related gene C (MrgC) receptors.
Johns Hopkins University
Design, synthesis, and biological evaluation of 1,2,4-triazole bearing 5-substituted biphenyl-2-sulfonamide derivatives as potential antihypertensive candidates.
China Pharmaceutical University
Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.
Unc Eshelman School of Pharmacy
Structure-based drug design: Synthesis and biological evaluation of quinazolin-4-amine derivatives as selective Aurora A kinase inhibitors.
Sun Yat-Sen University
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
Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.
Purdue University
Design and synthesis of 2-(4,5,6,7-tetrahydrothienopyridin-2-yl)-benzoimidazole carboxamides as novel orally efficacious Poly(ADP-ribose)polymerase (PARP) inhibitors.
Chinese Academy of Sciences
Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine.
TBA
Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series.
Bristol-Myers Squibb
The synthesis and evaluation of phenoxyacylhydroxamic acids as potential agents for Helicobacter pylori infections.
Jishou University
Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia.
Chinese Academy of Sciences
Novel 8-hydroxyquinoline derivatives targeting β-amyloid aggregation, metal chelation and oxidative stress against Alzheimer's disease.
Pharmaceutical University
Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.
China Pharmaceutical University
Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor.
Chinese Academy of Sciences
Arylamino containing hydroxamic acids as potent urease inhibitors for the treatment of Helicobacter pylori infection.
Jishou University
Synthesis and biological evaluation of aurora kinases inhibitors based on N-trisubstituted pyrimidine scaffold.
Sun Yat-Sen University
Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR associated drug resistant mutants in NSCLC.
Chinese Academy of Sciences
Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors.
China Pharmaceutical University
Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors.
University of Science and Technology of China
Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.
High Magnetic Field Laboratory
Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent.
Dana-Farber Cancer Institute
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
Structure-Guided Discovery of Novel, Potent, and Orally Bioavailable Inhibitors of Lipoprotein-Associated Phospholipase A2.
Shanghaitech University
Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor.
University of Science and Technology of China
Structural Basis of Inhibition of ERα-Coactivator Interaction by High-Affinity N-Terminus Isoaspartic Acid Tethered Helical Peptides.
Shenzhen Graduate School of Peking University
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinaseδ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.
Bristol-Myers Squibb
INHIBITORS OF FATTY ACID BINDING PROTEINS (FABPs), METHODS OF USE AND METHODS OF MAKING
Celloram
PYRROLOTRIAZINONE COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR, AND USE THEREOF
Shanghaitech University
Benzimidazole compounds and derivatives as EGFR inhibitors
Boehringer Ingelheim International
Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
Shy Therapeutics
Phenylate derivative, preparation method therefor, and pharmaceutical composition and uses thereof
Institute of Materia Medica, Chinese Academy of Medical Sciences
Oxopicolinamide derivative, preparation method therefor and pharmaceutical use thereof
Jinagsu Hengrui Medicine
2-substituted indazoles, methods for producing same, pharmaceutical preparations that contain same, and use of same to produce drugs
Bayer Pharma Aktiegesellschaft
Quinazoline derivative, preparation method therefor, and pharmaceutical composition and application thereof
Arromax Pharmatech
Substituted tricyclic heterocycles as histamine 4 receptor inhibitors
C&C Research Laboratories
Substituted 7-azabicycles and their use as orexin receptor modulators
Janssen Pharmaceutica
Simple methanesulfonates are hydrolyzed by the sulfatase carbonic anhydrase activity.
Agri Ibrahim Cecen University
Effects of some drugs on human cord blood erythrocyte carbonic anhydrases I and II: an in vitro study.
Erzincan University
Method for dual inhibition of SGLT1 and SGLT2 using diphenylmethane derivatives
Green Cross
Interaction of Azole-Based Environmental Pollutants with the Coelomic Hemoglobin from Amphitrite ornata: A Molecular Basis for Toxicity.
North Carolina State University
Iminothiadiazine dioxide compounds as brace inhibitors, compositions, and their use
Merck Sharp & Dohme
Synthesis of Novel Hybrids Inspired from Bromopyrrole Alkaloids Inhibiting MMP-2 and -12 as Antineoplastic Agents.
University of Kwazulu-Nata
Interactive binding between the substrate and allosteric sites of carbamoyl-phosphate synthetase.
Pennsylvania State University
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
SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist.
Smithkline Beecham Pharmaceuticals
Ligand binding to thromboxane receptors on human platelets: correlation with biological activity.
University of Edinburgh
Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity.
University Hospital Basel