223 articles for Y Zhu
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Cmpds
Data
Article Title
Organization
28
Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.
Merck Research Laboratories
5
Synthesis and anticancer activity of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives bearing chromone moiety.
Jiangxi Science & Technology Normal University
32
Functionalized N,N-Diphenylamines as Potent and Selective EPAC2 Inhibitors.
University of Texas Medical Branch
5
Synthesis, antitumor evaluation and molecular docking studies of [1,2,4]triazolo[4,3-b][1,2,4,5]tetrazine derivatives.
Taizhou Vocational & Technical College
45
3D-QSAR-aided design, synthesis, in vitro and in vivo evaluation of dipeptidyl boronic acid proteasome inhibitors and mechanism studies.
Nanjing Forestry University
28
Differentiation of ROMK potency from hERG potency in the phenacetyl piperazine series through heterocycle incorporation.
Merck Research Laboratories
9
Design, synthesis and docking studies of novel dipeptidyl boronic acid proteasome inhibitors constructed fromaa- anda -amino acids.
China Pharmaceutical University
13
Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer.
Bristol Myers Squibb
4
Design, synthesis, and docking studies of afatinib analogs bearing cinnamamide moiety as potent EGFR inhibitors.
Jiangxi Science & Technology Normal University
19
Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes.
Merck Research Laboratories
31
Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation.
Merck Research Laboratories
36
Structure-Activity Relationship Studies of Substituted 2-(Isoxazol-3-yl)-2-oxo-N'-phenyl-acetohydrazonoyl Cyanide Analogues: Identification of Potent Exchange Proteins Directly Activated by cAMP (EPAC) Antagonists.
University of Texas Medical Branch
38
Synthesis and evaluation of N-acyl-substituted 1,2-benzisothiazol-3-one derivatives as caspase-3 inhibitors.
TBA
26
Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties.
Bristol Myers Squibb
33
Discovery of a novel sub-class of ROMK channel inhibitors typified by 5-(2-(4-(2-(4-(1H-Tetrazol-1-yl)phenyl)acetyl)piperazin-1-yl)ethyl)isobenzofuran-1(3H)-one.
Merck Research Laboratories
71
Design of substituted imidazolidinylpiperidinylbenzoic acids as chemokine receptor 5 antagonists: potent inhibitors of R5 HIV-1 replication.
Sanofi
37
Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics.
TBA
18
Design, synthesis and biological evaluation ofß-carboline derivatives as novel inhibitors targeting B-Raf kinase.
China Pharmaceutical University
20
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.
Pfizer
28
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.
Wyeth Research
29
Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Merck Research Laboratories
31
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
Wyeth Research
31
Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines.
Wyeth Research
16
Synthesis and progesterone receptor antagonist activities of 6-aryl benzimidazolones and benzothiazolones.
Wyeth-Ayerst Research
37
Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
Genzyme
3
Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies.
Bristol Myers Squibb
3
Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors.
Novartis Institutes For Biomedical Research
27
Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
Genzyme
19
Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication.
Genzyme
10
Synthesis, biological assay in vitro and molecular docking studies of new imidazopyrazinone derivatives as potential dipeptidyl peptidase IV inhibitors.
East China University of Science and Technology
19
5-Aryl indanones and derivatives as non-steroidal progesterone receptor modulators.
Wyeth Research
31
Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and beta-secretase.
Chinese Academy of Sciences
52
4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Merck Research Laboratories
40
Structure-Guided Optimization of 2-Aminoquinazoline Hematopoietic Progenitor Kinase 1 Inhibitors for Improved Oral Bioavailability and Synergistic Antitumor Immunity.
China Pharmaceutical University
20
Discovery of Potent PDEδ/NAMPT Dual Inhibitors: Preclinical Evaluation in KRAS Mutant Pancreatic Cancer Cells.
Shanghai University
1
Design and Synthesis of Hederagenin Derivatives for the Treatment of Sepsis by Targeting TAK1 and Regulating the TAK1-NF-κB/MAPK Signaling.
Yantai University
43
Development of Novel PRMT7 Inhibitors for the Treatment of Prostate Cancer.
China Pharmaceutical University
22
Discovery of Nirmatrelvir (PF-07321332): A Potent, Orally Active Inhibitor of the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS CoV-2) Main Protease.
Pfizer
2
Opto-Epigenetic Regulation of Histone Arginine Asymmetric Dimethylation via Type I Protein Arginine Methyltransferase Inhibition.
The University of Hong Kong
8
Chemical Space Profiling of SARS-CoV-2 PLpro Using DNA-Encoded Focused Libraries.
Shanghai Institute of Materia Medica
12
Design, synthesis, and evaluation of a novel TRAIL-activated HDAC6 inhibitor for the treatment of pulmonary fibrosis.
Sichuan University
1
Discovery of Novel Small-Molecule Inhibitors Disrupting the MTDH-SND1 Protein-Protein Interaction.
China Pharmaceutical University
31
Discovery of N-Phenyl-5-propyl-1H-pyrazole-3-carboxamide, with Selective Inhibition and Degradation of HDAC6 for the Treatment of Acute Liver Injury.
Anhui Medical University
2
Discovery of SZJK-0421: A Novel Potent, Low Toxicity, Selective Second Generation of CRM1 Inhibitor for the Treatment of Both Hematological and Solid Tumors.
Nanjing Normal University
33
Design and synthesis of 1H-benzo[d]imidazole selective HDAC6 inhibitors with potential therapy for multiple myeloma.
Sichuan University
1
Design, synthesis, and biological evaluation of a series of new anthraquinone derivatives as anti-ZIKV agents.
Sun Yat-sen University
11
Azetidine ring, salicylic acid, and salicylic acid bioisosteres as determinants of the binding characteristics of novel potent compounds to Stat3.
Cedars-Sinai Medical Center
13
A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19.
Pfizer
13
Discovery and preclinical evaluations of TQB3616, a novel CDK4-biased inhibitor.
WuXi AppTec
24
Discovery of Urea Derivatives of Celastrol as Selective Peroxiredoxin 1 Inhibitors against Colorectal Cancer Cells.
Shanghai Jiao Tong University
2
Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting C797S Mutation.
China Pharmaceutical University
45
Discovery of potent and selective c-Met inhibitors for MET-amplified hepatocellular carcinoma treatment.
China Pharmaceutical University
5
A novel scaffold long-acting selective estrogen receptor antagonist and degrader with superior preclinical profile against ER+ breast cancer.
Yantai University
9
Anti-Helicobacter pylori and thrombin inhibitory components from Chinese dragon's blood, Dracaena cochinchinensis.
Chinese Academy of Sciences
6
Targeted regulated cell death with small molecule compounds in colorectal cancer: Current perspectives of targeted therapy and molecular mechanisms.
Sichuan University
86
Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2.
BeiGene(Beiing) Co., Ltd.
11
5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.
Wyeth Research
26
Design, synthesis and biological evaluation of a new class of 7H-pyrrolo[2,3-d]pyrimidine derivatives as Mps1 inhibitors for the treatment of breast cancer.
Sichuan University
3
Design, Synthesis, and Antitumor Activity of Potent and Selective EGFR L858R/T790M Inhibitors and Identification of a Combination Therapy to Overcome Acquired Resistance in Models of Non-small-cell Lung Cancer.
Sichuan University
49
Discovery of Novel Fourth-Generation EGFR Inhibitors to Overcome C797S-Mediated Resistance.
China Pharmaceutical University
19
Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors.
Wyeth Research
29
Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series.
Pharmaceutical Research Institute
21
Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).
Bristol Myers Squibb
34
Design and Synthesis of 1,3,5-Triazines or Pyrimidines Containing Dithiocarbamate Moiety as PI3Kα Selective Inhibitors.
Shenyang Pharmaceutical University
27
Optimization of potent, selective and orally bioavailable biphenyl scaffold as FABP4 inhibitors for anti-inflammation.
Fudan University
22
Identification and immunological evaluation of novel TLR2 agonists through structural optimization of Diprovocim.
Fudan University
23
Discovery of CRN04894: A Novel Potent Selective MC2R Antagonist.
Crinetics Pharmaceuticals
49
Discovery of Potent and Wild-Type-Sparing Fourth-Generation EGFR Inhibitors for Treatment of Osimertinib-Resistance NSCLC.
China Pharmaceutical University
53
Discovery and optimization of dihydropteridone derivatives as novel PLK1 and BRD4 dual inhibitor for the treatment of cancer.
Shenyang Pharmaceutical University
27
Recent advances of β-catenin small molecule inhibitors for cancer therapy: Current development and future perspectives.
Sichuan University
5
Review and prospects of targeted therapies for Spleen tyrosine kinase (SYK).
China Pharmaceutical University
9
Discovery of a Novel Covalent EZH2 Inhibitor Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer.
Sichuan University
73
Discovery of Novel Indazole Chemotypes as Isoform-Selective JNK3 Inhibitors for the Treatment of Parkinson's Disease.
Sichuan University
13
Research progress of indole compounds with potential antidiabetic activity.
Xi'An Jiaotong University
2
Design, synthesis, and biological evaluation of novel 2'-methyl-2'-fluoro-6-methyl-7-alkynyl-7-deazapurine nucleoside analogs as anti-Zika virus agents.
Guangzhou Institutes of Biomedicine and Health
26
SAR studies of 6-(arylamino)-4,4-disubstituted-1-methyl-1,4-dihydro-benzo[d][1,3]oxazin-2-ones as progesterone receptor antagonists.
Wyeth Research
18
Novel 2, 5-diketopiperazine derivatives as potent selective histone deacetylase 6 inhibitors: Rational design, synthesis and antiproliferative activity.
Northwest A&F University
33
Discovery of a Potent FLT3 Inhibitor (LT-850-166) with the Capacity of Overcoming a Variety of FLT3 Mutations.
China Pharmaceutical University
30
Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist.
Crinetics Pharmaceuticals
23
Discovery of pyrrolo[2,3-d]pyrimidine-based molecules as a Wee1 inhibitor template.
Capital Medical University
13
Design, synthesis and biological evaluations of novel farnesoid X receptor (FXR) agonists.
Shandong University
25
Design and synthesis of butynyloxyphenyl beta-sulfone piperidine hydroxamates as TACE inhibitors.
Wyeth Research
32
Design and synthesis of HDAC inhibitors to enhance the therapeutic effect of diffuse large B-cell lymphoma by improving metabolic stability and pharmacokinetic characteristics.
China Pharmaceutical University
49
Design, synthesis and biological evaluation of 7-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-2,3-dihydro-1H-inden-1-one derivatives as potent FAK inhibitors for the treatment of ovarian cancer.
Sichuan University-University of Oxford Huaxi Joint Centre For Gastrointestinal Cancer
8
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.
China Pharmaceutical University
40
Discovery of Novel Phosphoinositide-3-Kinase α Inhibitors with High Selectivity, Excellent Bioavailability, and Long-Acting Efficacy for Gastric Cancer.
China Pharmaceutical University
1
Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD).
Wuxi Apptec
35
Discovery of small-molecule inhibitors of RUVBL1/2 ATPase.
California Institute of Technology
16
Discovery and optimization of betulinic acid derivatives as novel potent CD73 inhibitors.
The Second Military Medical University
22
Unraveling the Design and Discovery of c-Jun N-Terminal Kinase Inhibitors and Their Therapeutic Potential in Human Diseases.
National Clinical Research Center For Geriatrics
15
Design, synthesis and biological evaluation of novel osimertinib derivatives as reversible EGFR kinase inhibitors.
College of Pharmacy of Liaoning University
11
Design and synthesis of highly TRAIL expression HDAC inhibitors based on ONC201 to promote apoptosis of colorectal cancer.
China Pharmaceutical University
7
Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal progesterone receptor agonist tanaproget.
Women'S Health Research Institute
25
Discovery and computational studies of 2-phenyl-benzoxazole acetamide derivatives as promising P2Y
Soochow University
4
Discovery of non-substrate, environmentally sensitive turn-on fluorescent probes for imaging HDAC8 in tumor cells and tissue slices.
Nanjing University of Chinese Medicine
24
SAR studies of 6-aryl-1,3-dihydrobenzimidazol-2-ones as progesterone receptor antagonists.
Wyeth Research
4
Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent.
Wuxi Apptec
4
Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
Wuxi Apptec
43
Discovery of 4-(3-aminopyrrolidinyl)-3-aryl-5-(benzimidazol-2-yl)-pyridines as potent and selective SST5 agonists for the treatment of congenital hyperinsulinism.
Crinetics Pharmaceuticals
12
Natural products from mangrove sediments-derived microbes: Structural diversity, bioactivities, biosynthesis, and total synthesis.
Chinese Academy of Sciences
19
Discovery of a new class of valosine containing protein (VCP/P97) inhibitors for the treatment of colorectal cancer.
Nanjing Normal University
25
Design and synthesis of dual inhibitors targeting snail and histone deacetylase for the treatment of solid tumour cancer.
China Pharmaceutical University
45
Discovery of novel and orally bioavailable CDK 4/6 inhibitors with high kinome selectivity, low toxicity and long-acting stability for the treatment of multiple myeloma.
China Pharmaceutical University
25
Potent Hydrazide-Based HDAC Inhibitors with a Superior Pharmacokinetic Profile for Efficient Treatment of Acute Myeloid Leukemia In Vivo.
Ocean University of China
17
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.
Bristol Myers Squibb
22
Design and Synthesis of EZH2-Based PROTACs to Degrade the PRC2 Complex for Targeting the Noncatalytic Activity of EZH2.
Sichuan University
1
In Pursuit of an Allosteric Human Tropomyosin Kinase A (
Veterinary Medicine Research & Development
26
Discovery of novel tripeptide propylene oxide proteasome inhibitors for the treatment of multiple myeloma.
Nanjing Normal University
23
Discovery of novel pyrimidine molecules containing boronic acid as VCP/p97 Inhibitors.
Nanjing Normal University
37
Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors.
Fudan University
34
Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity.
China Pharmaceutical University
33
Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists.
Wyeth Research
25
Discovery and Evaluation of Pyrazolo[3,4-
Hubei Bio-Pharmaceutical Industrial Technological Institute
31
New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles.
Wyeth Research
22
Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.
Bristol Myers Squibb
76
Discovery of Novel Azetidine Amides as Potent Small-Molecule STAT3 Inhibitors.
University of Hawaii Cancer Center
26
Design, syntheses and evaluations of novel indole derivatives as orally selective estrogen receptor degraders (SERD).
Luoxin Pharmaceutical (Shanghai) Co.
4
Discovery of natural product ellagic acid as a potent CD73 and CD39 dual inhibitor.
Ningxia Medical University
61
Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development.
TBA
24
Discovery and optimization of a potent and selective indazolamine series of IRAK4 inhibitors.
Zhejiang Hisun Pharmaceutical
17
The discovery of quinoline derivatives, as NF-κB inducing kinase (NIK) inhibitors with anti-inflammatory effects in vitro, low toxicities against T cell growth.
China Pharmaceutical University
45
The optimization of a novel selective antagonist for human M
Shanghai Jiao Tong University School of Medicine
37
Discovery of substituted 3H-pyrido[2,3-d]pyrimidin-4-ones as potent, biased, and orally bioavailable sst2 agonist.
Crinetics Pharmaceuticals
23
Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.
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
17
Optimization of substituted N-3-benzylimidazoquinazolinone sulfonamides as potent and selective PDE5 inhibitors.
Bristol Myers Squibb
11
(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor.
AstraZeneca
13
Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure.
Merck Research Laboratories
5
N-3-substituted imidazoquinazolinones: potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.
Bristol Myers Squibb
3
Unravel a neuroactive sHA sulfation pattern with neurogenesis activity by a library of defined oligosaccharides.
Peking University
28
Preparation and biological evaluation of soluble tetrapeptide epoxyketone proteasome inhibitors.
Nanjing Forestry University
15
SAR study of celastrol analogs targeting Nur77-mediated inflammatory pathway.
Xiamen University
15
Discovery of novel phenoxybenzamide analogues as Raf/HDAC dual inhibitors.
China Pharmaceutical University
19
Design, synthesis and biological evaluation of novel isoindolinone derivatives as potent histone deacetylase inhibitors.
Northwest A&F University
41
Discovery of aryl-substituted indole and indoline derivatives as RORγt agonists.
Fudan University
49
Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies.
Merck
25
6-Substituted 2,4-diaminopyrido[3,2-d]pyrimidine analogues of piritrexim as inhibitors of dihydrofolate reductase from rat liver, Pneumocystis carinii, and Toxoplasma gondii and as antitumor agents.
Duquesne University
17
Discovery of a new class of valosine containing protein (VCP/P97) inhibitors for the treatment of non-small cell lung cancer.
Nanjing Normal University
49
Nonclassical 2,4-diamino-8-deazafolate analogues as inhibitors of dihydrofolate reductases from rat liver, Pneumocystis carinii, and Toxoplasma gondii.
Duquesne University
18
Synthetic approaches and application of representative clinically approved fluorine-enriched anti-cancer medications.
Shengjing Hospital of China Medical University
35
Thioxo-dihydroquinazolin-one Compounds as Novel Inhibitors of Myeloperoxidase.
Emory University
30
Design and bio-evaluation of indole derivatives as potent Kv1.5 inhibitors.
China Pharmaceutical University
4
Mechanistic insights into a Ca2+-dependent family of alpha-mannosidases in a human gut symbiont.
Newcastle University
2
Enzymatic therapeutic index of acyclovir. Viral versus human polymerase gamma specificity.
The University of Texas
35
Structure-Based Design of 1-Heteroaryl-1,3-propanediamine Derivatives as a Novel Series of CC-Chemokine Receptor 5 Antagonists.
University of Chinese Academy of Sciences
26
Design, synthesis, in vitro and in vivo evaluation, and structure-activity relationship (SAR) discussion of novel dipeptidyl boronic acid proteasome inhibitors as orally available anti-cancer agents for the treatment of multiple myeloma and mechanism studies.
Nanjing Forestry University
17
Ridaifen-F conjugated with cell-penetrating peptides inhibits intracellular proteasome activities and induces drug-resistant cell death.
Nagahama Institute of Bio-Science and Technology
20
Multipotent AChE and BACE-1 inhibitors for the treatment of Alzheimer's disease: Design, synthesis and bio-analysis of 7-amino-1,4-dihydro-2H-isoquilin-3-one derivates.
Central South University
27
Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold.
Nanjing University of Chinese Medicine
24
Structure-activity relationships of 2-substituted phenyl-N-phenyl-2-oxoacetohydrazonoyl cyanides as novel antagonists of exchange proteins directly activated by cAMP (EPACs).
University of Texas Medical Branch
18
Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis.
Shenyang Pharmaceutical University
4
Structure-Activity Relationship Studies with Tetrahydroquinoline Analogs as EPAC Inhibitors.
Institute For Research In Cancer and Allied Diseases
17
Design, synthesis and biological evaluation of dual acetylcholinesterase and phosphodiesterase 5A inhibitors in treatment for Alzheimer's disease.
Central South University
19
Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants.
Nanjing Normal University
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
31
Identification of novel 2-(benzo[d]isoxazol-3-yl)-2-oxo-N-phenylacetohydrazonoyl cyanide analoguesas potent EPAC antagonists.
University of Texas Medical Branch
8
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Moe) and Hubei Provinc
16
BROMODOMAIN AND EXTRA-TERMINAL (BET) SUBFAMILY BROMODOMAIN 1 (BD1) SELECTIVE INHIBITORS AND METHODS USING SAME
Baylor College of Medicine
7
ANTIBODY-DRUG CONJUGATE PRECURSORS COMPRISING A CYCLIC DINUCLEOTIDE
Takeda Pharmaceutical
3
AMIDO PYRIDO[3,4-B]INDOLE-1,4-DIONE COMPOUNDS FOR TREATMENT OF PORPHYRIAS
Portal Therapeutics
84
SUBSTITUTED HYDANTOIN COMPOUNDS, METHODS FOR PREPARATION THEREOF AND USE THEREOF IN THE TREATMENT AND/OR PREVENTION OF A CORONA VIRUS DISEASE
Individual
4
HIGH PURITY COPPER RADIOPHARMACEUTICAL COMPOSITIONS AND DIAGNOSTIC AND THERAPEUTIC USES THEREOF
Nuclidium
31
CYCLIN-DEPENDENT KINASE INHIBITING COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS
G1 Therapeutics
10
PROTEIN-PROTEIN INTERACTION MODULATORS OF AURORA KINASE A AND THEIR USE IN THE PREVENTION AND/OR TREATMENT OF CANCER
Eberhard Karls Universitat Tubingen
57
Oxopyridine derivatives useful as aminocarboxymuconate semialdehyde decarboxylase (ACMSD) inhibitors
Orsobio
780
Tetrahydro-imidazo quinoline compositions as CBP/P300 inhibitors
Forma Therapeutics
107
Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
Incyte
56
1,3-dihydroxy-phenyl derivatives useful as immunomodulators
Bristol-Meyers Squibb
409
NOVEL DERIVATIVES HAVING 2,3-DIHYDRO-1H-INDENE OR 2,3-DIHYDROBENZOFURAN MOIETY OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
Yuhan
104
Methyl- and trifluromethyl-substituted pyrrolopyridine modulators of RORC2 and methods of use thereof
Pfizer
95
4-cyano-benzyl carbamimidoylcarbamate derivatives and their use as AOC3 inhibitors
Boehringer Ingelheim International
8
Combination Alzheimer therapy using anti-N3pGlu Abeta antibodies + a BACE inhibitor
Eli Lilly
8
Protein kinase inhibitors (variants), use thereof in treating oncological diseases and a pharmaceutical composition based thereon
Obshchestvo S Ogranichennoy Otvetstvennostyou “Fusion Pharma”
3
Isoxazolo-quinazolines as modulators of protein kinase activity
Nerviano Medical Sciences
5
Plasmodium falciparum UvrD activities are downregulated by DNA-interacting compounds and its dsRNA inhibits malaria parasite growth.
International Centre For Genetic Engineering and Biotechnology
12
Functional reversal of (-)-Stepholidine analogues by replacement of benzazepine substructure using the ring-expansion strategy.
Fudan University
12
Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism.
Pfizer
7
Design, Synthesis, and Evaluation of Polyamine Deacetylase Inhibitors, and High-Resolution Crystal Structures of Their Complexes with Acetylpolyamine Amidohydrolase.
University of Pennsylvania
19
Synthesis and molecular modelling studies of novel sulphonamide derivatives as dengue virus 2 protease inhibitors.
Birla Institute of Technology
30
Substituted bicyclic 1-carboxylic-acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin C
Boehringer Ingelheim International
176
Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof
Acetylon Pharmaceuticals
21
Synthesis and characterization of new piperazine-type inhibitors for mitochondrial NADH-ubiquinone oxidoreductase (complex I).
Kyoto University
4
Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing antagonistic activity.
Banyu Pharmaceutical
5
Characterization of the binding site for a novel class of noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonists.
Pfizer
1
Human serotonin 5-HT7 receptor: cloning and pharmacological characterisation of two receptor variants.
Organon
5
9-Dihydroxy-2,3,7,11b-tetrahydro-1H-naph[1,2,3-de]isoquinoline: a potent full dopamine D1 agonist containing a rigid-beta-phenyldopamine pharmacophore.
Purdue University
7
Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo.
Yamanouchi Pharmaceutical