139 articles for X Zhu
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
a-Conotoxin [S9A]TxID Potently Discriminates betweena3ß4 anda6/a3ß4 Nicotinic Acetylcholine Receptors.
Hainan University
[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.
Bristol-Myers Squibb Research and Development
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
Genentech
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.
Ariad Pharmaceuticals
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).
Constellation Pharmaceuticals
Novel Small Molecule Inhibitors of Choline Kinase Identified by Fragment-Based Drug Discovery.
Ariad Pharmaceuticals
Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series.
Arena Pharmaceuticals
Design and synthesis of new tricyclic indoles as potent modulators of the S1P1 receptor.
Arena Pharmaceuticals
Design, synthesis and evaluation of highly selective pyridone-based class II MET inhibitors.
Central China Normal University
Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.
Merck Research Laboratories
(7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists.
Arena Pharmaceuticals
Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.
Arena Pharmaceuticals
Discovery of 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamides as potent and selective CB2 receptor agonists.
Arena Pharmaceuticals
Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent.
Sun Yat-Sen University
Structure-based design and synthesis of bicyclic fused-pyridines as MEK inhibitors.
Shanghai Hengrui Pharmaceutical
Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties.
Merck Research Laboratories
Characterization of a novela-conotoxin TxID from Conus textile that potently blocks rata3ß4 nicotinic acetylcholine receptors.
Hainan University
Discovery ofβ2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.
University of Dundee
Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors.
Ariad Pharmaceuticals
Structure-based discovery of highly selective phosphodiesterase-9A inhibitors and implications for inhibitor design.
Sun Yat-Sen University
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.
Amgen
Fused tricyclic indoles as S1P1 agonists with robust efficacy in animal models of autoimmune disease.
Arena Pharmaceuticals
Discovery of SCH 900271, a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia.
TBA
Identification of diaryl ether-based ligands for estrogen-related receptora as potential antidiabetic agents.
Johnson & Johnson Pharmaceutical Research and Development
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation.
Fudan University
N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.
Amgen
Discovery of small-molecule inhibitors of Bcl-2 through structure-based computer screening.
Georgetown University Medical Center
Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious¿-secretase modulators in vivo.
Schering-Plough Research Institute
SAR studies of C2 ethers of 2H-pyrano[2,3-d]pyrimidine-2,4,7(1H,3H)-triones as nicotinic acid receptor (NAR) agonist.
Merck Research Laboratory
A three-step protocol for lead optimization: quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors.
Merck Research Laboratories
Pyrrolo[2,3-c]azepine derivatives: a new class of potent protein tyrosine phosphatase 1B inhibitors.
Sun Yat-Sen University
Identification of pentacyclic triterpenes derivatives as potent inhibitors against glycogen phosphorylase based on 3D-QSAR studies.
Chinese Academy of Sciences
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Ariad Pharmaceuticals
Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.
Amgen
Discovery of a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia
TBA
Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.
Ariad Pharmaceuticals
Design and synthesis of a simplified inhibitor for XIAP-BIR3 domain.
Institute For Medical Research
Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.
The Schering Plough Research Institute
9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation.
Ariad Pharmaceuticals
Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands.
The Schering Plough Research Institute
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.
Ariad Pharmaceuticals
Identification and validation of human DNA ligase inhibitors using computer-aided drug design.
University of Maryland
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum.
Chinese Academy of Sciences
The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models.
ARIAD Pharmaceuticals, Inc.
Design, Synthesis, and Biological Activity of Novel Quinone Derivatives as Potent STAT3 Inhibitors for Psoriasis Treatment.
Central South University
Discovery and preclinical evaluations of TQB3616, a novel CDK4-biased inhibitor.
WuXi AppTec
Design, synthesis and evaluate of indazolylaminoquinazoline derivatives as potent Tropomyosin receptor kinase (TRK) inhibitors.
Shanghai Institute of Pharmaceutical Industry Co., Ltd
Design, Synthesis, and Activity Evaluation of Fluorine-Containing Scopolamine Analogues as Potential Antidepressants.
Henan Normal University
Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B-Cell Lymphoma.
Kymera Therapeutics
Design, synthesis, and biological evaluation of 3-phenyl substituted pyridine derivatives as potential dual inhibitors of XOR and URAT1.
South China University of Technology
Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.
Schering-Plough Research Institute
Benzothiazole derivatives as histone deacetylase inhibitors for the treatment of autosomal dominant polycystic kidney disease.
Xuzhou Medical University
Structure-Activity Relationships of Alanine Scan Mutants αO-Conotoxins GeXIVA[1,2] and GeXIVA[1,4].
Guangxi University
Design, synthesis and biological evaluation of dual Topo II/HDAC inhibitors bearing pyrimido[5,4-b]indole and pyrazolo[3,4-d]pyrimidine motifs.
Hebei University
Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.
Amgen
Structure-based discovery of potent USP28 inhibitors derived from Vismodegib.
Anhui University of Chinese Medicine
Discovery and Development of a Selective Inhibitor of the ER Resident Chaperone Grp78.
University of Arizona
Discovery, Characterization, and Engineering of LvIC, an α4/4-Conotoxin That Selectively Blocks Rat α6/α3β4 Nicotinic Acetylcholine Receptors.
Guangxi University
Discovery of imidazo[1,2-b]pyridazine macrocyclic derivatives as novel ALK inhibitors capable of combating multiple resistant mutants.
Shanghai Institute of Pharmaceutical Industry Co.
Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non-small cell lung cancer.
Ariad Pharmaceuticals
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
Design, synthesis and biological evaluation of novel macrocyclic derivatives bearing aniline pyrimidine scaffolds as EGFR-TKIs.
China State Institute of Pharmaceutical Industry Co.
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol.
Florida A&M University
Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD).
Wuxi Apptec
Discovery and optimization of new 6, 7-dihydroxy-1, 2, 3, 4-tetrahydroisoquinoline derivatives as potent influenza virus PA
South China Agricultural University
Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
Yantai University
Engineered Conotoxin Differentially Blocks and Discriminates Rat and Human α7 Nicotinic Acetylcholine Receptors.
Hainan University
Discovery of Non-Nucleotide Small-Molecule STING Agonists
Bristol Myers Squibb Research and Development
Synthesis and evaluation of novel and potent protease activated receptor 4 (PAR4) antagonists based on a quinazolin-4(3H)-one scaffold.
China Pharmaceutical University
Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
Yantai University
Flavonoid Monomers as Potent, Nontoxic, and Selective Modulators of the Breast Cancer Resistance Protein (ABCG2).
Hong Kong Polytechnic University
Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors.
Bristol Myers Squibb Research and Development
Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors.
Emd Serono Research & Development Institute
Protease activated receptor 4 (PAR4) antagonists: Research progress on small molecules in the field of antiplatelet agents.
China Pharmaceutical University
Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway.
Genomics Institute of The Novartis Research Foundation
Discovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy.
Bristol Myers Squibb Research and Development
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.
Genomics Institute of The Novartis Research Foundation
Novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines as potent and selective agonists of the 5-HT
Arena Pharmaceuticals
High Selectivity of an α-Conotoxin LvIA Analogue for α3β2 Nicotinic Acetylcholine Receptors Is Mediated by β2 Functionally Important Residues.
Guangxi University
Identification of a novel, orally bioavailable histamine H(3) receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template.
The Schering Plough Research Institute
Synthesis and bioevaluation of 1-phenylimidazole-4-carboxylic acid derivatives as novel xanthine oxidoreductase inhibitors.
South China University of Technology
Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1.
Bristol Myers Squibb Research and Development
Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.
Genentech
Structure and Activity Studies of Disulfide-Deficient Analogues of αO-Conotoxin GeXIVA.
Hainan University
Modifications of the 4,4'-residues and SAR studies of Biphalin, a highly potent opioid receptor active peptide.
University of Arizona
Discovery of potent anti-inflammatory 4-(4,5,6,7-tetrahydrofuro[3,2-c]pyridin-2-yl) pyrimidin-2-amines for use as Janus kinase inhibitors.
Central China Normal University
Triazole Bridged Flavonoid Dimers as Potent, Nontoxic, and Highly Selective Breast Cancer Resistance Protein (BCRP/ABCG2) Inhibitors.
Hong Kong Polytechnic University
GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.
Genentech
Design, synthesis, and biological activity of novel dicoumarol glucagon-like peptide 1 conjugates.
China Pharmaceutical University
Structure-based design and synthesis of C-1- and C-4-modified analogs of zanamivir as neuraminidase inhibitors.
Chinese Academy of Sciences
Synthesis and SAR Studies of Fused Oxadiazines as γ-Secretase Modulators for Treatment of Alzheimer's Disease.
Merck Research Laboratory
Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.
Florida A and M University
Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.
Novartis Institutes For Biomedical Research
Discovery of Novel Flavonoid Dimers To Reverse Multidrug Resistance Protein 1 (MRP1, ABCC1) Mediated Drug Resistance in Cancers Using a High Throughput Platform with "Click Chemistry".
Hong Kong Polytechnic University
Single Amino Acid Substitution in α-Conotoxin TxID Reveals a Specific α3β4 Nicotinic Acetylcholine Receptor Antagonist.
Hainan University
Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300.
Wuxi Apptec
Discovery of APD371: Identification of a Highly Potent and Selective CB
Arena Pharmaceuticals
Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases.
Genomics Institute of The Novartis Research Foundation
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).
Genentech
GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2).
Genentech
Design and synthesis of novel PRMT1 inhibitors and investigation of their binding preferences using molecular modelling.
Ningxia Medical University
Rational design of conformationally constrained oxazolidinone-fused 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.
South China Agricultural University
A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.
Genentech
Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
Astrazeneca
(Hetero)aryl-methyl-thio-beta-D-galactopyranoside derivatives
Idorsia Pharmaceuticals
SULFONAMIDE DERIVATIVE, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
Jiangsu Hengrui Pharmaceuticals
SULFONAMIDE DERIVATIVES AND THEIR USE AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS
Department Of Health
SUBSTITUTED PYRAZOLO [1,5-A]PYRIMIDINE-7-AMINE COMPOUNDS AS CDK INHIBITORS AND THEIR THERAPEUTIC USE
Carrick Therapeutics
Substituted pyrazolo[4,3-d]pyrimidines and imidazo[5,1 -f][1,2,4]triazines as androgen receptor and phosphodiesterase dual inhibitors
Ildong Pharmaceutical
SALT OF DIHYDROPYRIDO[2,3-D]PYRIMIDINONE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
Nanjing Chia Tai Tianqing Pharmaceutical
Thiophene, manufacturing method thereof, and pharmaceutical application of same
Cstone Pharmaceutical (Suzhou)
Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy
Abbvie Deutschland
Aminotetraline and aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy
Abbvie Deutschland
Susceptibility of cord blood antioxidant enzymes glutathione reductase, glutathione peroxidase and glutathione S-transferase to different antibiotics: in vitro approach.
Ondokuz Mayis University
Inhibition of cysteine proteases by a natural biflavone: behavioral evaluation of fukugetin as papain and cruzain inhibitor.
Federal University of Sao Paulo
Purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition with inhibitory activity against Raf kinase, containing same as active ingredient
Medpacto
Amidopyrazole inhibitors of interleukin receptor-associated kinases
Merck Sharp & Dohme
[(pF)Phe4,Arg14,Lys15]N/OFQ-NH2 (UFP-102), a highly potent and selective agonist of the nociceptin/orphanin FQ receptor.
Section of Pharmacology