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3
Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3).

East China University of Science and Technology
16
Design, synthesis and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives as selective c-Met inhibitors.

Shenyang Pharmaceutical University
8
Discovery of biphenyl imidazole derivatives as potent antifungal agents: Design, synthesis, and structure-activity relationship studies.

Shenyang Pharmaceutical University
29
Design, synthesis and biological evaluation of novel cholesteryl ester transfer protein inhibitors bearing a cycloalkene scaffold.

Shenyang Pharmaceutical University
16
Synthesis and biological evaluation of 4-(2-fluorophenoxy)-3,3'-bipyridine derivatives as potential c-met inhibitors.

Shenyang Pharmaceutical University
43
Synthesis and Biological Evaluation of Novels1 Receptor Ligands for Treating Neuropathic Pain: 6-Hydroxypyridazinones.

Huazhong University of Science and Technology
19
Design, synthesis and biological evaluation of N,N-3-phenyl-3-benzylaminopropanamide derivatives as novel cholesteryl ester transfer protein inhibitor.

Shenyang Pharmaceutical University
38
Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.

The University of Texas M.D. Anderson Cancer Center
12
Design, synthesis and biological evaluation of novel 4-phenoxy-6,7-disubstituted quinolines possessing (thio)semicarbazones as c-Met kinase inhibitors.

Shenyang Pharmaceutical University
66
Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors.

Qilu Pharmaceutical
4
Discovery of imidazopyridine derivatives as highly potent respiratory syncytial virus fusion inhibitors.

Roche Innovation Center Shanghai
9
Structure-activity profiles of novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolates with modified amino acids for cellular uptake by folate receptorsa and and the proton-coupled folate transporter.

Duquesne University
2
Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.

Qilu Pharmaceutical
14
Synthesis and biological evaluation of a series of benzoxazole/benzothiazole-containing 2,3-dihydrobenzo[b][1,4]dioxine derivatives as potential antidepressants.

Huazhong University of Science and Technology
12
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.

Huazhong University of Science and Technology
15
Structure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors.

Biogen Idec
23
Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1.

Biogen Idec
11
Synthesis and HMG-CoA reductase inhibition of 2-cyclopropyl-4-thiophenyl-quinoline mevalonolactones.

Institute of Pharmaceutical Industry
23
Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.

Ligand Pharmaceuticals
27
Carboxylic acid bioisosteres acylsulfonamides, acylsulfamides, and sulfonylureas as novel antagonists of the CXCR2 receptor.

Johnson & Johnson Pharmaceutical Research and Development
1
A phosphorylated prodrug for the inhibition of Pin1.

Virginia Tech
16
Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I).

Biogen Idec
1
Discovery of bacterial NAD+-dependent DNA ligase inhibitors: optimization of antibacterial activity.

AstraZeneca
22
Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists.

Glaxosmithkline
5
Design, synthesis and biological evaluation of naphthyl amide derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.

Sichuan University
5
Design, Synthesis, and Biological Evaluation of Covalently Mucoadhesive Derivatives as Nonsystemic Intestine-Targeted TGR5 Agonists.

The First Affiliated Hospital of Henan University
2
Cernuosides A and B, two sucrase inhibitors from Pulsatilla cernua.

China Pharmaceutical University
1
Design, Biological Characterization, and Discovery of Capromorelin Derivatives as Oral Growth Hormone Secretagogue Receptor Type 1a Agonist for the Treatment of Growth Hormone Deficiency.

Changchun Genescience Pharma
47
Design, synthesis and biological evaluation of arylpropylamine derivatives as potential multi-target antidepressants.

Nanjing Tech University
17
Design, Synthesis, and Biological Evaluation of 3-Amino-pyrazine-2-carboxamide Derivatives as Novel FGFR Inhibitors.

The Second Affiliated Hospital
33
Design and synthesis of 1H-benzo[d]imidazole selective HDAC6 inhibitors with potential therapy for multiple myeloma.

Sichuan University
2
Discovery of first-in-class highly selective TRPV1 antagonists with dual analgesic and hypoglycemic effects.

The First Affiliated Hospital of Zhengzhou University
50
Discovery of (2S)-N-(6-Cyano-5-(trifluoromethyl)pyridin-3-yl)-3-(6-(4-cyanophenyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)-2-hydroxy-2-methylpropanamide as a Highly Potent and Selective Topical Androgen Receptor Antagonist for Androgenetic Alopecia Treatment.

China Pharmaceutical University
4
Design and biological evaluation of dual tubulin/HDAC inhibitors based on millepachine for treatment of prostate cancer.

China Pharmaceutical University
2
Recent updates on 1,2,3-triazole-containing hybrids with in vivo therapeutic potential against cancers: A mini-review.

Wuhan University of Science and Technology
4
Discovery of Novel Potent Covalent Glutathione Peroxidase 4 Inhibitors as Highly Selective Ferroptosis Inducers for the Treatment of Triple-Negative Breast Cancer.

China Pharmaceutical University
1
Discovery of carboxyl-containing heteroaryldihydropyrimidine derivatives as novel HBV capsid assembly modulators with significantly improved metabolic stability.

Shandong University
3
Optimization of BAX trigger site activator BTSA1 with improved antitumor potency and in vitro ADMET properties.

Shenyang Pharmaceutical University
1
Structure-Based Ligand Discovery Targeting the Transmembrane Domain of Frizzled Receptor FZD7.

Shanghaitech University
3
Discovery of Novel

China Pharmaceutical University
28
Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.

Guangzhou Institutes of Biomedicine and Health
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
14
Discovery and preclinical evaluations of WX-0593, a novel ALK inhibitor targeting crizotinib-resistant mutations.

Wuxi Apptec
6
Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists.

Johnson & Johnson Pharmaceutical Research and Development
23
Rational Remodeling of Atypical Scaffolds for the Design of Photoswitchable Cannabinoid Receptor Tools.

Shanghaitech University
2
Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents.

Shenyang Pharmaceutical University
10
Discovery of Pyrazolo[3,4-

Bytedance Ai Lab
43
Structure-Based Design of Dual-Acting Compounds Targeting Adenosine A

Shanghaitech University
44
Discovery of AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma.

AstraZeneca
3
Design, synthesis and biological activities of benzo[d]imidazo[1,2-a]imidazole derivatives as TRPM2-specfic inhibitors.

Peking University
5
Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.

Shenyang Pharmaceutical University
17
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.

Peking University
24
Elucidation of Distinct Modular Assemblies of Smoothened Receptor by Bitopic Ligand Measurement.

Shanghaitech University
15
Design, synthesis and evaluation of heteroaryldihydropyrimidine analogues bearing spiro ring as hepatitis B virus capsid protein inhibitors.

Shandong University
28
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.

Vrije Universiteit Brussel
5
Design, synthesis and biological activities of piperidine-spirooxadiazole derivatives as α7 nicotinic receptor antagonists.

Peking University
48
Discovery of 5-Benzylidene-2-phenyl-1,3-dioxane-4,6-diones as Highly Potent and Selective SIRT1 Inhibitors.

Chinese Academy of Sciences
12
Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists.

Henan University
14
Discovery of a novel potent GPR40 full agonist.

Janssen Research & Developmen
60
Discovery of AB680: A Potent and Selective Inhibitor of CD73.

Arcus Biosciences
3
4-Aryl Pyrrolidines as Novel Orally Efficacious Antimalarial Agents. Part 2: 2-Aryl-

Saint Louis University
2
Design, synthesis and evaluation of biphenyl imidazole analogues as potent antifungal agents.

Shenyang Pharmaceutical University
14
Strategies for the development of highly selective cytochrome P450 inhibitors: Several CYP targets in current research.

Shenyang Pharmaceutical University
14
Colocalization Strategy Unveils an Underside Binding Site in the Transmembrane Domain of Smoothened Receptor.

Shanghaitech University
54
Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands.

Shanghaitech University
86
Discovery of Potent and Selective Non-Nucleotide Small Molecule Inhibitors of CD73.

Arcus Biosciences
9
Design, synthesis and biological evaluation of benzamide derivatives as novel NTCP inhibitors that induce apoptosis in HepG2 cells.

Southwest Jiaotong University
10
4-Aryl Pyrrolidines as a Novel Class of Orally Efficacious Antimalarial Agents. Part 1: Evaluation of 4-Aryl- N-benzylpyrrolidine-3-carboxamides.

Saint Louis University
19
Design, synthesis and biological evaluation of novel isoindolinone derivatives as potent histone deacetylase inhibitors.

Northwest A&F University
10
Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.

Janssen Research & Development
2
Benzofuran derivatives and their anti-tubercular, anti-bacterial activities.

Huanghuai University
5
Discovery of novel pyruvate dehydrogenase kinases inhibitors by screening of an in-house small molecule library for anti-lung cancer therapeutics.

Shaanxi Province Tuberculosis Prevention and Treatment Institute
30
Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4).

Glaxosmithkline
17
Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).

Amgen
13
Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer.

Qilu Pharmaceutical
61
6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CB

Janssen Research & Development
50
Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.

Shandong University
25
Synthesis and biological evaluation of novel 1-(aryl-aldehyde-oxime)uracil derivatives as a new class of thymidine phosphorylase inhibitors.

Yunnan University
6
Terpenoids with vasorelaxant effects from the Chinese liverwort Scapania carinthiaca.

Shandong University
7
Design, synthesis and evaluation of benzoheterocycle analogues as potent antifungal agents targeting CYP51.

Shenyang Pharmaceutical University
19
Reverse Hydroxamate Inhibitors of Bone Morphogenetic Protein 1.

Glaxosmithkline Pharmaceuticals
2
Docking based design of diastereoisomeric MTCA as GPIIb/IIIa receptor inhibitor.

Capital Medical University
3
Design, Synthesis, and Evaluation of Tetrahydropyrrolo[1,2-

Wuxi Apptec (Shanghai)
7
Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents.

Shenyang Pharmaceutical University
23
Design and Synthesis of Soluble and Cell-Permeable PI3Kδ Inhibitors for Long-Acting Inhaled Administration.

AstraZeneca
48
4-[[(7-aminopyrazolo[1,5-a]pyrimidin-5-yl)amino methyl]piperidin-3-ol compounds and their therapeutic use

Carrick Therapeutics
45
AZETIDINE DERIVATIVES AND USE THEREOF AS DIPEPTIDYL PEPTIDASE 1 INHIBITORS

Chiesi Farmaceutici
119
KINASE INHIBITORS, PREPARATION METHODS AND USES THEREOF

Inventisbio
14
MULTICYCLIC COMPOUNDS

Slap Pharmaceuticals
20
MST1 kinase inhibitor and use thereof

Tarapeutics Science Inc.
12
COMPOUNDS CONTAINING A GEM-DIFLUORIDE GROUP AND PREPARATION METHOD AND USE THEREOF

Cgenetech (Suzhou, China) Co.
31
NOVEL ERGOLINES AND METHODS OF TREATING MOOD DISORDERS

Gilgamesh Pharmaceuticals
27
CONFORMATIONALLY-CONSTRAINED INHIBITORS OF 3C OR 3C-LIKE PROTEASES

Kansas State University Research Foundation
29
COMPOUND USED AS KINASE INHIBITOR AND USE THEREOF

Tyk Medicines
18
5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof

Cancer Research Technology
573
2-Acylamidomethyl and sulfonylamidomethyl benzoxazine carbamates for inhibition of RORgamma activity and the treatment of disease

Lycera
53
Aromatic heterocyclic compounds and their application in pharmaceuticals

Sunshine Lake Pharma
492
AMPK-activating heterocyclic compounds and methods for using the same

Rigel Pharmaceuticals
35
Piperazine compound capable of inhibiting prostaglandin D synthase

Taiho Pharmaceutical
2
Pharmacological characterization of two novel and potent 5-HT4 receptor agonists, RS 67333 and RS 67506, in vitro and in vivo.

Syntex Discovery Research
31
Aza-peptidyl Michael Acceptors. A New Class of Potent and Selective Inhibitors of Asparaginyl Endopeptidases (Legumains) from Evolutionarily Diverse Pathogens.

Georgia Institute of Technology
55
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.

Vernalis (R&D)
3
Structural basis for Chk1 inhibition by UCN-01.

Glaxosmithkline
45
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.

Pharmacia Italia