PMID
Cmpds
Data
Article Title
Organization
17
Discovery of Selective Phosphodiesterase 1 Inhibitors with Memory Enhancing Properties.

Dart Neuroscience
26
Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders.

Dart Neuroscience
11
DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-ß aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy.

Sichuan University
24
Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases andß-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.

Sichuan University
22
Design, synthesis and biological evaluation of 4'-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer's disease.

Sichuan University
16
Substituted 4-morpholine N-arylsulfonamides as¿-secretase inhibitors.

Merck Research Laboratories
51
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.

Ariad Pharmaceuticals
14
Discovery of a Novel, Potent Spirocyclic Series of¿-Secretase Inhibitors.

Merck Research Laboratories
22
Ether modifications to 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine (SA4503): effects on binding affinity and selectivity for sigma receptors and monoamine transporters.

University of Missouri
1
Targeting (cellular) lysosomal acid ceramidase by B13: design, synthesis and evaluation of novel DMG-B13 ester prodrugs.

Medical University of South Carolina
1
Synthesis and evaluation in monkey of [(18)F]4-fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([(18)F]FIMX): a promising radioligand for PET imaging of brain metabotropic glutamate receptor 1 (mGluR1).

National Institute of Mental Health
14
Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors.

Ariad Pharmaceuticals
31
Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.

Array Biopharma
9
Discovery of SCH 900229, a Potent Presenilin 1 Selective ¿-Secretase Inhibitor for the Treatment of Alzheimer's Disease.

TBA
7
Synthesis, biological evaluation and molecular docking studies of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents.

Nanjing University
26
Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors.

Takeda California
10
Neuronal nicotinic acetylcholine receptor binding affinities of boron-containing nicotine analogues.

University of Kentucky
36
Small molecule agonists of the orphan nuclear receptors steroidogenic factor-1 (SF-1, NR5A1) and liver receptor homologue-1 (LRH-1, NR5A2).

University of Southampton
19
Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.

Array Biopharma
23
Discovery and SAR of spirochromane Akt inhibitors.

Array Biopharma
49
Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV.

Takeda California
27
Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors.

Array Biopharma
25
Design, synthesis, and structure-activity relationship studies of N-arylsulfonyl morpholines as¿-secretase inhibitors.

Merck Research Lab.
18
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.

National Institute of Mental Health
51
Discovery of pyrrolopyrimidine inhibitors of Akt.

Array Biopharma
4
Design and synthesis of tricyclic sulfones as gamma-secretase inhibitors with greatly reduced Notch toxicity.

Merck Research Laboratories
53
Discovery of AK-1690: A Potent and Highly Selective STAT6 PROTAC Degrader.

University of Michigan
3
Discovery of SD-436: A Potent, Highly Selective and Efficacious STAT3 PROTAC Degrader Capable of Achieving Complete and Long-Lasting Tumor Regression.

University of Michigan
9
Molecular understanding of the therapeutic potential of melanin inhibiting natural products.

Tianjin University
4
Discovery of N-(1-(6-Oxo-1,6-dihydropyrimidine)-pyrazole) Acetamide Derivatives as Novel Noncovalent DprE1 Inhibitors against Mycobacterium tuberculosis.

Zhejiang University
14
Discovery of a brain-permeable bromodomain and extra terminal domain (BET) inhibitor with selectivity for BD1 for the treatment of multiple sclerosis.

China Pharmaceutical University
22
Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.

Schering-Plough Research Institute
29
Discovery of a Potent and Selective STAT5 PROTAC Degrader with Strong Antitumor Activity

University of Michigan
5
Synthesis and in vitro evaluation of tetrahydroisoquinolinyl benzamides as ligands for sigma receptors.

University of Missouri-Columbia
30
Discovery of 1

China Pharmaceutical University
3
Discovery of Pyxinol Amide Derivatives Bearing Amino Acid Residues as Nonsubstrate Allosteric Inhibitors of P-Glycoprotein-Mediated Multidrug Resistance.

Yantai University
52
Discovery of 2-Aminopyrimidine Derivatives as Potent Dual FLT3/CHK1 Inhibitors with Significantly Reduced hERG Inhibitory Activities.

Zhejiang University
1
Tetracyclic Steroids Bearing a Bicyclo[4.4.1] Ring System as Potent Antiosteoporosis Agents from the Deep-Sea-Derived Fungus

Third Institute of Oceanography
27
Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: impacting hERG liability via aryl modifications.

Schering-Plough Research Institute
41
Discovery of orally efficacious melanin-concentrating hormone receptor-1 antagonists as antiobesity agents. Synthesis, SAR, and biological evaluation of bicyclo[3.1.0]hexyl ureas.

Schering-Plough Research Institute
35
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.

Schering-Plough Research Institute
21
Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.

China Pharmaceutical University
13
Discovery of bicycloalkyl urea melanin concentrating hormone receptor antagonists: orally efficacious antiobesity therapeutics.

Schering-Plough Research Institute
3
Selective Discovery of GPCR Ligands within DNA-Encoded Chemical Libraries Derived from Natural Products: A Case Study on Antagonists of Angiotensin II Type I Receptor.

Northwest University
22
Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release.

University of Kentucky
52
SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction.

Schering-Plough Research Institute
21
Design and synthesis of xanthine analogues as potent and selective PDE5 inhibitors.

Schering-Plough Research Institute
2
SD-91 as A Potent and Selective STAT3 Degrader Capable of Achieving Complete and Long-Lasting Tumor Regression.

University of Michigan
3
Synthesis, structure activity relationship and in vitro anti-influenza virus activity of novel polyphenol-pentacyclic triterpene conjugates.

Peking University
11
Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein.

TBA
10
3-[(1

Peloton Therapeutics
21
Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors.

Merck Research Laboratories
27
Synthesis and pharmacological characterization of O-alkynyloximes of tropinone and N-methylpiperidinone as muscarinic agonists.

National University of Singapore
27
Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.

Sichuan University
3
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.

Sichuan University
54
Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385).

Peloton Therapeutics
27
Design, synthesis and evaluation of scutellarein-O-acetamidoalkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease.

Sichuan University
39
ISOXAZOLE-HETEROCYCLIC DERIVATIVE, PHARMACEUTICAL COMPOSITION AND USE

Shanghai Simr Biotechnology Co.
47
Psychedelics and the human receptorome.

University of Oklahoma
59
Oxoisoquinoline derivatives

Carna Biosciences
29
Cyanopyrrolidine derivatives as inhibitors for DUBs

Mission Therapeutics
66
Arginase inhibitors as therapeutics

Mars
8
Quaternized amines as sodium channel blockers

Purdue Pharma
23
Design, synthesis and SAR study of hydroxychalcone inhibitors of human ß-secretase (BACE1).

Shanghai Institute of Material Medica, Chinese Academy of Sciences
818
Flap modulators

Janssen Pharmaceutica
7
Tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidines as antagonists of serotonin 5-HT6 receptors, methods for the production and use thereof

TBA
10
The discovery of novel vascular endothelial growth factor receptor tyrosine kinases inhibitors: pharmacophore modeling, virtual screening and docking studies.

Shanghai Jiao Tong University
74
Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell line.

Brigham and Women'S Hospital