145 articles for X Zheng
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Cmpds
Data
Article Title
Organization
60
Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRa) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs).
East China University of Science and Technology
66
3D-QSAR studies of 3-(3,4-dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic acids as AKR1C3 inhibitors: Highlight the importance of molecular docking in conformation generation.
Guangzhou Medical University
68
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.
Genentech
42
Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents.
East China University of Science and Technology
33
Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase.
Bristol Myers Squibb
4
Discovery of imidazopyridine derivatives as highly potent respiratory syncytial virus fusion inhibitors.
Roche Innovation Center Shanghai
33
Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.
Genentech
29
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Forma Therapeutics
42
Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Genentech
25
Discovery and preclinical characterization of the cyclopropylindolobenzazepine BMS-791325, a potent allosteric inhibitor of the hepatitis C virus NS5B polymerase.
Bristol Myers Squibb
61
Fragment-based design of 3-aminopyridine-derived amides as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Genentech
14
Discovery of potent and efficacious cyanoguanidine-containing nicotinamide phosphoribosyltransferase (Nampt) inhibitors.
Forma Therapeutics
36
Identification of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Genentech
60
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
Forma Therapeutics
39
Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties.
Genentech
49
Structure-based identification of ureas as novel nicotinamide phosphoribosyltransferase (Nampt) inhibitors.
Forma Therapeutics
76
3D QSAR studies on a series of potent and high selective inhibitors for three kinases of RTK family.
Dalian University
25
Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO.
AstraZeneca
19
Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.
AstraZeneca
21
Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists.
Neurogen
35
Heterobiaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part II.
AMRI
43
Biaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part I.
AMRI
30
Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor.
Okayama University Graduate School of Medicine
4
Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215
Bristol Myers Squibb
64
Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent.
AstraZeneca
37
Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration.
AstraZeneca
19
Pyrido[2,3-b]pyrazines, discovery of TRPV1 antagonists with reduced potential for the formation of reactive metabolites.
Neurogen
3
Selective benzimidazole inhibitors of the antigen receptor-mediated NF-kappaB activation pathway.
Human Biomolecular Research Institute
14
3-amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile.
AstraZeneca
7
Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.
AstraZeneca
32
Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer.
AstraZeneca
42
Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution.
Neurogen
11
Discovery of 2,4-dianilinopyrimidine derivatives as novel p90 ribosomal S6 protein kinase (RSK) inhibitors.
Changzhi University
27
Discovery of Isobenzofuran-1(3H)-one Derivatives as Selective TREK-1 Inhibitors with In Vitro and In Vivo Neuroprotective Effects.
Chinese Academy of Medical Sciences and Peking Union Medical College
9
Discovery of Novel 2,4,5-Trisubstituted Pyrimidine Derivatives as Potent and Selective FGFR Inhibitors against Gatekeeper Mutants for the Treatment of NSCLC.
Wenzhou Medical University
31
Discovery of the Clinical Candidate YY2201 as a Highly Potent and Selective ATR Inhibitor.
Chinese Academy of Medical Sciences & Peking Union Medical College
25
Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor.
AstraZeneca
55
Design, Synthesis, and Bioevaluation of Novel NLRP3 Inhibitor with IBD Immunotherapy from the Virtual Screen.
Fudan University
27
Discovery of C-3 isoxazole substituted thiochromone S,S-dioxide derivatives as potent and selective inhibitors for monoamine oxidase B (MAO-B).
University of South China
22
Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B-Cell Lymphoma.
Kymera Therapeutics
5
Discovery of LC-MI-3: A Potent and Orally Bioavailable Degrader of Interleukin-1 Receptor-Associated Kinase 4 for the Treatment of Inflammatory Diseases.
Hangzhou Medical College
26
Design, synthesis and evaluation of C-5 substituted pyrrolopyridine derivatives as potent Janus Kinase 1 inhibitors with excellent selectivity.
University of South China
10
The mechanisms of multidrug resistance of breast cancer and research progress on related reversal agents.
University of South China
12
Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors.
AstraZeneca
8
Discovery of Potent, Dual-Inhibitors of Diacylglycerol Kinases Alpha and Zeta Guided by Phenotypic Optimization.
Bristol Myers Squibb
31
Discovery of C-5 Pyrazole-Substituted Pyrrolopyridine Derivatives as Potent and Selective Inhibitors for Janus Kinase 1.
University of South China
6
Review of bioactivity and structure-activity relationship on baicalein (5,6,7-trihydroxyflavone) and wogonin (5,7-dihydroxy-8-methoxyflavone) derivatives: Structural modifications inspired from flavonoids in Scutellaria baicalensis.
Shaanxi University of Chinese Medicine
17
Structure Based Design of Non-Natural Peptidic Macrocyclic Mcl-1 Inhibitors.
AstraZeneca
7
Analgesic agents without gastric damage: design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors.
Okayama University Graduate School of Medicine
22
Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect.
Northwest University
64
From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.
Neurogen
14
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.
Bristol Myers Squibb
19
Discovery of Small Molecules Simultaneously Targeting NAD(P)H:Quinone Oxidoreductase 1 and Nicotinamide Phosphoribosyltransferase: Treatment of Drug-Resistant Non-small-Cell Lung Cancer.
China Pharmaceutical University
14
Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma.
Wenzhou Medical University
16
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
Pharmaceutical Research Institute
38
Identification of TUL01101: A Novel Potent and Selective JAK1 Inhibitor for the Treatment of Rheumatoid Arthritis.
Zhuhai United Laboratories
25
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-
AstraZeneca
15
Design, synthesis and biological evaluation of novel osimertinib derivatives as reversible EGFR kinase inhibitors.
College of Pharmacy of Liaoning University
22
Progress of thrombus formation and research on the structure-activity relationship for antithrombotic drugs.
Northwest University
35
Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.
Bristol Myers Squibb
8
Research progress in biological activities of isochroman derivatives.
Shaanxi University of Chinese Medicine
20
Design, synthesis and activity evaluation of isopropylsulfonyl-substituted 2,4- diarylaminopyrimidine derivatives as FAK inhibitors for the potential treatment of pancreatic cancer.
Dalian Medical University
21
Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors.
Bristol Myers Squibb
22
Synthesis and evaluation of hydrazinyl-containing pyrrolo[2,3-d]pyrimidine series as potent, selective and oral JAK1 inhibitors for the treatment of rheumatoid arthritis.
Wuxi Apptec (Shanghai) Co.
9
Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template.
Bristol Myers Squibb
16
Noncovalent EGFR T790M/L858R inhibitors based on diphenylpyrimidine scaffold: Design, synthesis, and bioactivity evaluation for the treatment of NSCLC.
Dalian Medical University
38
GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.
Genentech
44
5-Aminonaphthalene derivatives as selective nonnucleoside nuclear receptor binding SET domain-protein 2 (NSD2) inhibitors for the treatment of multiple myeloma.
Chinese Academy of Sciences
8
Design, synthesis, molecular modeling studies, and calpain inhibitory activity of novel alpha-ketoamides incorporating polar residues at the P1'-position.
University of Tennessee Health Science Center
3
Discovery of GNE-502 as an orally bioavailable and potent degrader for estrogen receptor positive breast cancer.
Genentech
37
Design, synthesis, and biological evaluation of indazole derivatives as selective and potent FGFR4 inhibitors for the treatment of FGF19-driven hepatocellular cancer.
Wenzhou Medical University
14
Discovery of 4-amino-1H-pyrazolo[3,4-d]pyrimidin derivatives as novel discoidin domain receptor 1 (DDR1) inhibitors.
China Pharmaceutical University
4
Sensitive fluorogenic substrates for sirtuin deacylase inhibitor discovery.
Xihua University
43
Design, Synthesis, and Biological Activity of Substrate Competitive SMYD2 Inhibitors.
AstraZeneca
16
Optimization of a series of potent, selective and orally bioavailable SYK inhibitors.
AstraZeneca
17
Discovery of KT-474─a Potent, Selective, and Orally Bioavailable IRAK4 Degrader for the Treatment of Autoimmune Diseases.
Kymera Therapeutics
9
Significance of hydrogen bonding at the S(1)' subsite of calpain I.
The University of Tennessee
19
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.
Genentech
10
Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis.
Dalian Medical University
27
Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254).
AstraZeneca
5
Synthesis and calpain inhibitory activity of alpha-ketoamides with 2,3-methanoleucine stereoisomers at the P2 position.
The University of Tennessee Health Science Center
43
Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.
Genentech
10
Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.
Genentech
46
Design and Synthesis of Potent, Selective Inhibitors of Protein Arginine Methyltransferase 4 against Acute Myeloid Leukemia.
Chinese Academy of Sciences
15
Development of the "hidden" multifunctional agents for Alzheimer's disease.
Zhejiang Academy of Medical Sciences
30
Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927.
Genentech
1
Discovery of Ziresovir as a Potent, Selective, and Orally Bioavailable Respiratory Syncytial Virus Fusion Protein Inhibitor.
Roche Pharma Research and Early Development
13
Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
Northwest University
5
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
Research Triangle Institute
2
Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
Northwest University
22
Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.
AstraZeneca
27
Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507.
AstraZeneca
10
Synthesis and SAR studies of novel heteroaryl fused tetracyclic indole-diamide compounds: potent allosteric inhibitors of the hepatitis C virus NS5B polymerase.
Bristol Myers Squibb
33
Screening, synthesis, crystal structure, and molecular basis of 6-amino-4-phenyl-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitriles as novel AKR1C3 inhibitors.
Guangzhou Medical University
39
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
East China University of Science and Technology
32
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.
AstraZeneca
25
Design, synthesis, and discovery of 5-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)pyrimidine-2,4,6(1H,3H,5H)-triones and related derivatives as novel inhibitors of mPGES-1.
University of Kentucky
49
Discovery of Benzoazepinequinoline (BAQ) Derivatives as Novel, Potent, Orally Bioavailable Respiratory Syncytial Virus Fusion Inhibitors.
Roche Pharma Research and Early Development
2
Discovery of novel piperonyl derivatives as diapophytoene desaturase inhibitors for the treatment of methicillin-, vancomycin- and linezolid-resistant Staphylococcus aureus infections.
East China University of Science and Technology
33
Discovery of methylsulfonyl indazoles as potent and orally active respiratory syncytial Virus(RSV) fusion inhibitors.
Roche Innovation Center Shanghai
22
Discovery of novel N-hydroxy-2-arylisoindoline-4-carboxamides as potent and selective inhibitors of HDAC11.
Forma Therapeutics
36
Development of a Series of Kynurenine 3-Monooxygenase Inhibitors Leading to a Clinical Candidate for the Treatment of Acute Pancreatitis.
Glaxosmithkline
39
From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.
Genentech
94
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
East China University of Science and Technology
27
CONFORMATIONALLY-CONSTRAINED INHIBITORS OF 3C OR 3C-LIKE PROTEASES
Kansas State University Research Foundation
5
COMPOSITIONS AND METHODS FOR THE PREVENTION AND/OR TREATMENT OF MITOCHONDRIAL DISEASE, INCLUDING FRIEDREICH'S ATAXIA
Stealth Biotherapeutics
59
Cyano cyclobutyl compounds for CBL-B inhibition and uses thereof
Nurix Therapeutics
30
INHIBITORS TARGETING UBIQUITIN SPECIFIC PROTEASE 7 (USP7)
Dana-Farber Cancer Institute
61
Sulfonimidoylpurinone compounds and methods of treatment using the same
Hoffmann-La Roche
31
Piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
Bristol Myers Squibb
23
Substituted 3,4,5,6,8,10,14,14a-octahydro-2h-2,6-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazocines and methods for treating viral infections
Gilead Sciences
1
Bicyclic compounds and their use as antibacterial agents and β-lactamase inhibitors
Fedora Pharmaceuticals
5
The androgen-regulated protease TMPRSS2 activates a proteolytic cascade involving components of the tumor microenvironment and promotes prostate cancer metastasis.
Fred Hutchinson Cancer Research Center
4
3-arylidene-5-(4-isobutylphenyl)-2(3H)-furanones: a new series of anti-inflammatory and analgesic compounds having antimicrobial activity.
Jamia Hamdard
2
Exploiting sp(2) -Hybridisation in the Development of Potent 1,5-a-l-Arabinanase Inhibitors.
University of Western Australia
167
TETRAHYDRONAPHTHALENE DERIVATIVES AS ESTROGEN RECEPTOR DEGRADERS
Regent Of The University Of Michigan
5
Structure-Activity Relationships of Benzenesulfonamide-Based Inhibitors towards Carbonic Anhydrase Isoform Specificity.
University of Florida
52
Aniline derivatives, their preparation and their therapeutic application
Fovea Pharmaceuticals
8
Intramolecular hydrogen-bonded nitric oxide synthase inhibitors
Northwestern University
45
Heterocyclic derivatives and their use in the treatment of neurological disorders
Novartis