131 articles for H Zhao
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Cmpds
Data
Article Title
Organization
38
SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.
Abbvie
1
Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis.
Peking Union Medical College
7
Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer.
University of Illinois College of Pharmacy
14
Enriching screening libraries with bioactive fragment space.
Beijing University of Technology
13
The"Gatekeeper" Residue Influences the Mode of Binding of Acetyl Indoles to Bromodomains.
University of Z£Rich
1
Three stories on Eph kinase inhibitors: From in silico discovery to in vivo validation.
University of Z£Rich
18
Selective Human Estrogen Receptor Partial Agonists (ShERPAs) for Tamoxifen-Resistant Breast Cancer.
University of Illinois At Chicago
16
Discovery of novel N-aryl piperazine CXCR4 antagonists.
Emory Institute For Drug Development
57
Identification of Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K).
Glaxosmithkline
12
Ionic derivatives of betulinic acid exhibit antiviral activity against herpes simplex virus type-2 (HSV-2), but not HIV-1 reverse transcriptase.
Mercer University
16
Pyrrolo[3,2-b]quinoxaline derivatives as types I1/2 and II Eph tyrosine kinase inhibitors: structure-based design, synthesis, and in vivo validation.
University of Z£Rich
23
Discovery of a new chemical series of BRD4(1) inhibitors using protein-ligand docking and structure-guided design.
AMRI
1
Current kinase inhibitors cover a tiny fraction of fragment space.
University of Zurich
1
Structural Analysis of the Binding of Type I, I1/2, and II Inhibitors to Eph Tyrosine Kinases.
University of Zurich
7
Design, synthesis, anticancer activity and docking studies of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as mTOR inhibitors.
TBA
2
Discovery of BRD4 bromodomain inhibitors by fragment-based high-throughput docking.
University of Zurich
78
The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist.
Merck Research Laboratories
3
Discovery of dual ZAP70 and Syk kinases inhibitors by docking into a rare C-helix-out conformation of Syk.
University of Zurich
7
Discovery of ZAP70 inhibitors by high-throughput docking into a conformation of its kinase domain generated by molecular dynamics.
University of Zurich
2
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
Amgen
4
Discovery of a novel chemotype of tyrosine kinase inhibitors by fragment-based docking and molecular dynamics.
TBA
14
Discovery of novel EGFR tyrosine kinase inhibitors by structure-based virtual screening.
East China University of Science and Technology
12
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c
Cephalon
13
Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells.
Amgen
3
Synthesis of a potent and selective (18)F-labeled delta-opioid receptor antagonist derived from the Dmt-Tic pharmacophore for positron emission tomography imaging.
Stanford University School of Medicine
21
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
50
Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors.
Abbott Laboratories
36
Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors.
Abbott Laboratories
32
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
Neurogen
1
Structural basis for the interaction between casein kinase 1 delta and a potent and selective inhibitor.
Amgen
13
Synthesis and biological evaluation of quinazoline and quinoline bearing 2,2,6,6-tetramethylpiperidine-N-oxyl as potential epidermal growth factor receptor(EGFR) tyrosine kinase inhibitors and EPR bio-probe agents.
East China University of Science and Technology
18
Synthesis and biological evaluation of 4-[3-chloro-4-(3-fluorobenzyloxy)anilino]-6-(3-substituted-phenoxy)pyrimidines as dual EGFR/ErbB-2 kinase inhibitors.
East China University of Science and Technology
2
Identification and initial SAR of silybin: an Hsp90 inhibitor.
The University of Kansas
27
Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.
Amgen
14
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.
Amgen
18
Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors.
Abbott Laboratories
71
Design, Synthesis, and Biological Evaluation of Chiral-Proline Derivatives as Novel HSP90 Inhibitors.
Dezhou University
36
Harnessing the Magic Methyl Effect: Discovery of CLPP-2068 as a Novel HsClpP Activator for the Treatment of Diffuse Large B-Cell Lymphoma.
Shanghai Institute of Materia Medica
53
Discovery of Bis-imidazolecarboxamide Derivatives as Novel, Potent, and Selective TNIK Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis.
Insilico Medicine AI Ltd.
1
Discovery of naphthoquinone-furo-piperidone derivatives as dual targeting agents of STAT3 and NQO1 for the treatment of breast cancer.
Zhejiang University
3
Design, Synthesis, and Biological Evaluation of 2-Arylaminopyrimidine Derivatives as Dual Cathepsin L and JAK Inhibitors for the Treatment of Acute Lung Injury.
Zhejiang University
15
Discovery of YK-029A, a novel mutant EGFR inhibitor targeting both T790 M and exon 20 insertion mutations, as a treatment for NSCLC.
Puhe Biopharma
39
Discovery of benzofuran-2-carboxylic acid derivatives as lymphoid tyrosine phosphatase (LYP) inhibitors for cancer immunotherapy.
Shandong University
2
Natural Product-Inspired Discovery of Naphthoquinone-Furo-Piperidine Derivatives as Novel STAT3 Inhibitors for the Treatment of Triple-Negative Breast Cancer.
Zhejiang University
47
Discovery of Potent and Selective PI3Kδ Inhibitors for the Treatment of Acute Myeloid Leukemia.
Zhejiang University
26
Coumarin-based inhibitors of human NAD(P)H:quinone oxidoreductase-1. Identification, structure-activity, off-target effects and in vitro human pancreatic cancer toxicity.
University of Manchester
20
Design, Synthesis and Antitumor Activity of a Novel Class of SHP2 Allosteric Inhibitors with a Furanyl Amide-Based Scaffold.
Shandong University
15
Proline-derived quinoline formamide compounds as human urate transporter 1 inhibitors with potent uric acid-lowering activities.
Peking Union Medical College
32
Discovery of Highly Selective and Orally Bioavailable PI3Kδ Inhibitors with Anti-Inflammatory Activity for Treatment of Acute Lung Injury.
Zhejiang University
8
Discovery of novel non-nucleoside inhibitors with high potency and selectivity for DNA methyltransferase 3A.
Zhejiang University
20
2,6-diazaspiro[3.4]octan-7-one derivatives as potent sigma-1 receptor antagonists that enhanced the antinociceptive effect of morphine and rescued morphine tolerance.
Xuzhou Medical University
18
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
Amgen
3
The Role of Allylic Strain for Conformational Control in Medicinal Chemistry.
AstraZeneca
13
Hemodynamic effects of potent and selective JNK inhibitors in anesthetized rats: implication for targeting protein kinases in metabolic diseases.
Abbott Laboratories
55
Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond.
Abbott Laboratories
34
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
1
Novel CRBN-Recruiting Proteolysis-Targeting Chimeras as Degraders of Stimulator of Interferon Genes with In Vivo Anti-Inflammatory Efficacy.
Southern Medical University
1
Discovery of Thieno[2,3-d]pyrimidine-based KRAS G12D inhibitors as potential anticancer agents via combinatorial virtual screening.
Southern Medical University
58
Optimization of 2,4-diaminopyrimidines as GHS-R antagonists: side chain exploration.
Abbott Laboratories
3
Design, Synthesis, and Biological Evaluation of Pyrrole-2-carboxamide Derivatives as Mycobacterial Membrane Protein Large 3 Inhibitors for Treating Drug-Resistant Tuberculosis.
Peking Union Medical College and Chinese Academy of Medical Sciences
1
Telocinobufagin Has Antitumor Effects in Non-Small-Cell Lung Cancer by Inhibiting STAT3 Signaling.
Wenzhou Medical University
1
Discovery of novel Quinazoline-based KRAS G12C inhibitors as potential anticancer agents.
Sun Yat-Sen University
33
Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists.
Abbott Laboratories
6
Discovery of tetralin carboxamide growth hormone secretagogue receptor antagonists via scaffold manipulation.
Abbott Laboratories
25
Novel isoxazole carboxamides as growth hormone secretagogue receptor (GHS-R) antagonists.
Abbott Laboratories
25
Discovery of DNA-Targeting HDAC Inhibitors with Potent Antitumor Efficacy In Vivo That Trigger Antitumor Immunity.
Shandong University
2
Design, synthesis and structure-activity relationship studies of 4-indole-2-arylaminopyrimidine derivatives as anti-inflammatory agents for acute lung injury.
Zhejiang University
25
Discovery of hydrazide-containing oseltamivir analogues as potent inhibitors of influenza A neuraminidase.
Shenyang Pharmaceutical University
1
Identification of Novel Tricyclic Benzo[1,3]oxazinyloxazolidinones as Potent Antibacterial Agents with Excellent Pharmacokinetic Profiles against Drug-Resistant Pathogens.
Peking Union Medical College
31
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.
Neurogen
6
Fragment screening and assembly: a highly efficient approach to a selective and cell active protein tyrosine phosphatase 1B inhibitor.
Abbott Laboratories
13
Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: a novel series of mixed dopamine D2/D4 receptor antagonist.
Neurogen
8
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
Peking Union Medical College and Chinese Academy of Medical Sciences
25
Synthesis and Pin1 inhibitory activity of thiazole derivatives.
Peking Union Medical College
35
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation.
Neurogen
85
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships.
Neurogen
19
Utilization of a peptide lead for the discovery of a novel PTP1B-binding motif.
National Cancer Institute-Frederick
23
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.
University of Illinois At Chicago
19
Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives: a novel series of mixed dopamine D2/D4 receptor antagonists.
Neurogen
11
Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.
Chinese Academy of Sciences
27
Chicoric acid analogues as HIV-1 integrase inhibitors.
National Cancer Institute-Bethesda
10
Monocarboxylic-based phosphotyrosyl mimetics in the design of GRB2 SH2 domain inhibitors.
National Cancer Institute-Bethesda
19
Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer.
University of Illinois At Chicago
45
Salicylhydrazine-containing inhibitors of HIV-1 integrase: implication for a selective chelation in the integrase active site.
National Cancer Institute-Bethesda
18
Hydrazide-containing inhibitors of HIV-1 integrase.
National Cancer Institute-Bethesda
12
Discovery of HIV-1 integrase inhibitors by pharmacophore searching.
National Cancer Institute-Bethesda
3
Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.
Wuyi University
11
3D-QSAR Assisted Design, Synthesis and Evaluation of Novobiocin Analogues.
The University of Kansas
23
Synthesis and biological evaluation of 2,4,5-substituted pyrimidines as a new class of tubulin polymerization inhibitors.
Chinese Academy of Sciences
24
Synthesis and SAR of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as potent and selective CDK4/6 inhibitors.
Jiangnan University
21
Synthesis and biological evaluation of novel 5,6-dihydropyrimido[4,5-f]quinazoline derivatives as potent CDK2 inhibitors.
Jiangnan University
13
Stabilized β-Hairpin Peptide Inhibits Insulin Degrading Enzyme.
Peking University Shenzhen Graduate School
33
Discovery of Novel Aminotetralines and Aminochromanes as Selective and Competitive Glycine Transporter 1 (GlyT1) Inhibitors.
Abbvie Deutschland
32
De Novo Design, Synthesis, and Biological Evaluation of 3,4-Disubstituted Pyrrolidine Sulfonamides as Potent and Selective Glycine Transporter 1 Competitive Inhibitors.
Abbvie
21
Discovery of dimethyl pent-4-ynoic acid derivatives, as potent and orally bioavailable DGAT1 inhibitors that suppress body weight in diet-induced mouse obesity model.
Wuxi Apptec (Shanghai)
49
Discovery of Tetrahydroisoquinoline-Containing CXCR4 Antagonists with Improved in Vitro ADMET Properties.
Emory University
26
Discovery of novel quinazoline-2,4(1H,3H)-dione derivatives as potent PARP-2 selective inhibitors.
Peking Union Medical College
3
Structural Basis of Inhibition of ERα-Coactivator Interaction by High-Affinity N-Terminus Isoaspartic Acid Tethered Helical Peptides.
Shenzhen Graduate School of Peking University
14
Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping.
Wuxi Apptec (Shanghai)
13
Beta-lactamase inhibitors, formulations, and uses thereof
University of South Florida
9
Phosphonate derivatives and methods of use thereof in the treatment of Alzheimer's disease
University of Kansas
122
2,4-diaminopyrimidine derivatives as histamine H4 modulators
Janssen Pharmaceutica
35
Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy
Abbvie Deutschland
259
Benzoxazole- and tetrahydrobenzoxazole-substituted pyridazinones as GPR119 agonists
Boehringer Ingelheim International
117
Pyrimidine derivatives, preparation thereof, and pharmaceutical use thereof as akt(pkb) phosphorylation inhibitors
Sanofi
31
Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Roche Bioscience
15
Cloning and expressional characterization of a novel galanin receptor. Identification of different pharmacophores within galanin for the three galanin receptor subtypes.
Schering-Plough Research Institute
30
Pyrazolo[3,4-c]pyridazines as novel and selective inhibitors of cyclin-dependent kinases.
Universidad San Pablo Ceu
29
Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.
Avenida De La Industria
14
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases.
Bristol Myers Squibb
22
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues.
Bristol Myers Squibb
12
Design of benzoic acid inhibitors of influenza neuraminidase containing a cyclic substitution for the N-acetyl grouping.
University of Alabama At Birmingham