PMID
Cmpds
Data
Article Title
Organization
21
Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound.

Epizyme
54
A selective prostaglandin E2 receptor subtype 2 (EP2) antagonist increases the macrophage-mediated clearance of amyloid-beta plaques.

Amgen
26
Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction.

Amgen
26
C5-Alkyl-2-methylurea-Substituted Pyridines as a New Class of Glucokinase Activators.

Amgen
47
Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres.

Amgen
23
Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction.

Amgen
46
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.

Amgen
39
Discovery of thieno[3,2-d]pyrimidine-6-carboxamides as potent inhibitors of SIRT1, SIRT2, and SIRT3.

Sirtris A Gsk
10
Structure-based design of novel inhibitors of the MDM2-p53 interaction.

Amgen
4
Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes.

Sirtris Pharmaceuticals
34
Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors.

Neurocrine Bioscience
7
Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa.

Daiichi Asubio Medical Research Laboratories
25
Synthesis and Na+/H+ exchanger inhibitory activity of benzoylguanidine derivatives.

China Pharmaceutical University
8
Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor.

Lanzhou University
33
Discovery of AB801, a Potent and Selective Inhibitor of AXL Receptor Tyrosine Kinase for Use in Cancer Therapy.

Arcus Biosciences, Inc.
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
15
Design, Biological Characterization, and Discovery of Novel Cyclohexenyl Derivatives as Kinesin KIF18A Inhibitors for the Treatment of Ovarian Cancer.

Changchun Genescience Pharma
7
Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.

TBA
52
Discovery of novel, potent, and orally bioavailable HDACs inhibitors with LSD1 inhibitory activity for the treatment of solid tumors.

Xinxiang Medical University
23
Progress in 11β-HSD1 inhibitors for the treatment of metabolic diseases: A comprehensive guide to their chemical structure diversity in drug development.

Hong Kong Baptist University
28
Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads.

Agios Pharmaceuticals
12
A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors.

Merck Research Laboratories
25
Synthesis, SAR exploration, and X-ray crystal structures of factor XIa inhibitors containing an alpha-ketothiazole arginine.

Daiichi Asubio Medical Research Laboratories
53
Design, Synthesis, and Structure-Activity Relationship Optimization of Pyrazolopyrimidine Amide Inhibitors of Phosphoinositide 3-Kinase γ (PI3Kγ).

Arcus Biosciences
10
Peptide-based long-acting co-agonists of GLP-1 and cholecystokinin 1 receptors as novel anti-diabesity agents.

Jiangsu Normal University
5
A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells.

Merck Research Laboratories
10
Discovery of Pyridone-Substituted Triazolopyrimidine Dual A

Fudan University
26
3-(2-aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl-uracils as orally bioavailable antagonists of the human gonadotropin releasing hormone receptor.

Neurocrine Biosciences
45
Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous

Agios Pharmaceuticals
16
Discovery of a novel bicycloproline P2 bearing peptidyl alpha-ketoamide LY514962 as HCV protease inhibitor.

Eli Lilly
32
Discovery of Potent and Selective Methylenephosphonic Acid CD73 Inhibitors.

Arcus Biosciences
13
Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus.

Merck Research Laboratories
64
Discovery of Potent and Selective 7-Azaindole Isoindolinone-Based PI3Kγ Inhibitors.

Arcus Biosciences
14
Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains.

Merck Research Laboratories
5
Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.

Merck Research Laboratories
77
Stapled and

Jiangsu Normal University
18
A combinatorial library of indinavir analogues and its in vitro and in vivo studies.

Merck Research Laboratories
16
Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666.

Epizyme
39
Discovery of Potent and Selective PI3Kγ Inhibitors.

Arcus Biosciences
60
Discovery of AB680: A Potent and Selective Inhibitor of CD73.

Arcus Biosciences
7
C15-methoxyphenylated 18-deoxy-herbimycin A analogues, their in vitro anticancer activity and heat shock protein 90 binding affinity.

Peking Union Medical College
27
Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394.

Amgen
25
5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties.

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

Arcus Biosciences
7
Structure-based modification of carbonyl-diphenylpyrimidines (Car-DPPYs) as a novel focal adhesion kinase (FAK) inhibitor against various stubborn cancer cells.

The First Affiliated Hospital of Dalian Medical University
14
Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma.

Agios Pharmaceuticals
8
Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integrase.

Merck Research Laboratories
11
A potent and orally active HIV-1 integrase inhibitor.

Merck Research Laboratories
11
Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.

Merck Research Laboratories
8
AMINO HETEROARYL COMPOUNDS AND COMPOSITIONS

Anrui Biomedical Technology (Guangzhou) Co.
20
Method of increasing platelet counts of a subject

Korea Basic Science Institute
155
Imidazo[4,5-c]pyridine and pyrrolo[2,3-c]pyridine derivatives as SSAO inhibitors

Proximagen
171
Compounds for the treatment of pain

Alkermes
19
Azetidine derivatives

Vernalis (R&D)
10
[5,6]—fused bicyclic antidiabetic compounds

Merck Sharp & Dohme
72
N2-(2-methoxyphenyl)pyrimidine derivative, method for preparing same, and pharmaceutical composition for cancer prevention or treatment containing same as active ingredient

Korea Research Institute of Chemical Technology
66
Cyclobutane containing carboxylic acid GPR120 modulators

Bristol Myers Squibb
111
Cyclopropanamine compound and use thereof

Takeda Pharmaceutical
123
Substituted thiazole or oxazole P2X7 receptor antagonists

Axxam
82
Bisarylsulfonamides useful in the treatment of inflammation and cancer

Kancera
140
Inhibitors of the renal outer medullary potassium channel

Merck Sharp & Dohme
373
Unsaturated nitrogen heterocyclic compounds useful as PDE10 inhibitors

Amgen
12
Novel inhibitor of bacterial sphingomyelinase, SMY-540, developed based on three-dimensional structure analysis.

Tokushima Bunri University
6
Development of Potent, Selective SRPK1 Inhibitors as Potential Topical Therapeutics for Neovascular Eye Disease.

Exonate
1
Electrostatic Interactions as Mediators in the Allosteric Activation of Protein Kinase A RIa.

University of California San Diego
1
Pyrazole compounds

Eli Lilly
49
Inhibitors of the Renal Outer Medullary Potassium channel

Merck Sharp & Dohme
163
CHROMAN DERIVATIVES AS ESTROGEN RECEPTOR DEGRADERS

University Of Michigan
16
Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors.

Sunesis Pharmaceuticals