PMID
Cmpds
Data
Article Title
Organization
49
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERa+ Breast Cancer.

Novartis Institutes For Biomedical Research
18
Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight.

Novartis Institutes For Biomedical Research
1
The discovery and the structural basis of an imidazo[4,5-b]pyridine-based p21-activated kinase 4 inhibitor.

Soongsil University
70
Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.

Seoul National University
46
Discovery of novel 2,5-dioxoimidazolidine-based P2X(7) receptor antagonists as constrained analogues of KN62.

Gwangju Institute of Science and Technology (Gist)
28
Synthesis and optimization of picolinamide derivatives as a novel class of 11 -hydroxysteroid dehydrogenase type 1 (11 -HSD1) inhibitors.

Seoul National University
25
Synthesis and biological evaluation of picolinamides as potent inhibitors of 11 -hydroxysteroid dehydrogenase type 1 (11 -HSD1).

Seoul National University
20
Novel thienopyrimidinones as mGluR1 antagonists.

Yonsei University
18
Discovery of MK-7655, a -lactamase inhibitor for combination with Primaxin .

Merck Research Labs
26
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase

Genomics Institute of The Novartis Research Foundation
30
Virtual medicinal chemistry: in silico pre-docking functional group transformation for discovery of novel inhibitors of botulinum toxin serotype A light chain.

Panthera Biopharma
41
Discovery of novel 2-hydroxydiarylamide derivatives as TMPRSS4 inhibitors.

Korea Research Institute of Bioscience and Biotechnology
7
Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors.

TBA
2
Chemical modulators working at pharmacological interface of target proteins.

Korea University College of Pharmacy Sejong-Ro
30
Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptord agonists as potent anti-obesity agents in vivo.

Seoul National University
16
Antidotes to anthrax lethal factor intoxication. Part 3: Evaluation of core structures and further modifications to the C2-side chain.

Panthera Biopharma
9
Inhibition of protein tyrosine phosphatase 1B by diterpenoids isolated from Acanthopanax koreanum.

Korea Research Institute of Bioscience and Biotechnology
8
Deoxyribosyl analogues of methionyl and isoleucyl sulfamate adenylates as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases.

Seoul National University
24
Vanilloid and isovanilloid analogues as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases.

Seoul National University
24
Ester and hydroxamate analogues of methionyl and isoleucyl adenylates as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases.

Seoul National University
17
A novel class of inhibitors for steroid 5alpha-reductase: synthesis and evaluation of umbelliferone derivatives.

Seoul National University
15
Side chain SAR of bicyclicß-lactamase inhibitors (BLIs). 2. N-Alkylated and open chain analogs of MK-8712.

Merck Research Labs
14
Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors.

Korea Institute of Science and Technology
39
Antidotes to anthrax lethal factor intoxication. Part 2: structural modifications leading to improved in vivo efficacy.

Panthera Biopharma
8
Sulfonamide derivatives of styrylheterocycles as a potent inhibitor of COX-2-mediated prostaglandin E2 production.

Seoul National University
32
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.

Novartis Institutes For Biomedical Research
29
Antidotes to anthrax lethal factor intoxication. Part 1: Discovery of potent lethal factor inhibitors with in vivo efficacy.

Panthera Biopharma
10
B-Raf kinase inhibitors: hit enrichment through scaffold hopping.

Wyeth Research
31
Novel benzofuran-3-one indole inhibitors of PI3 kinase-alpha and the mammalian target of rapamycin: hit to lead studies.

Wyeth Research
24
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.

Wyeth Research
36
SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.

Bristol Myers Squibb
31
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.

Wyeth Research
12
Side chain SAR of bicyclic beta-lactamase inhibitors (BLIs). 1. Discovery of a class C BLI for combination with imipinem.

Merck Research Labs
26
Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies.

Wyeth Research
35
Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.

Wyeth Research
12
Rational design of selective thrombin inhibitors

TBA
5
Design, synthesis, and characterization of dipeptide isostere containing
cis-epoxide for the irreversible inactivation of HIV protease

TBA
19
4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.

Wyeth Research
2
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.

The Scripps Research Institute
13
T-type Ca2+ channel blockers suppress the growth of human cancer cells.

Kyung Hee University
1
Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR).

Albert Einstein College of Medicine
1
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.

Genomics Institute of The Novartis Research Foundation
15
Discovery of Diphenyl Ether Derivatives as Novel BKCa Channel Activators: Structure-Activity Relationship, Cryo-EM Complex Structures, and In Vivo Animal Studies.

Gwangju Institute of Science and Technology
24
Discovery of INCB159020, an Orally Bioavailable KRAS G12D Inhibitor.

Incyte
3
Synthesis of 1-Hydroxy(and 1-Alkoxy, 1-Acyloxy)-1H-indoles and evaluations of their suppressive activities against tumor growth through inhibiting lactate dehydrogenase A.

Pusan National University
22
Synthesis and antibacterial activities of baulamycin A inspired derivatives.

Korea University
38
Discovery of Triazolopyrimidine Derivatives as Selective P2X3 Receptor Antagonists Binding to an Unprecedented Allosteric Site as Evidenced by Cryo-Electron Microscopy.

Gwangju Institute of Science and Technology
7
Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity.

Seoul National University
18
Discovery of (4-Pyrazolyl)-2-aminopyrimidines as Potent and Selective Inhibitors of Cyclin-Dependent Kinase 2.

Incyte
2
Discovery and Binding Mechanism of Pyrazoloisoquinoline-Based Novel β-Arrestin Inverse Agonists of the Kappa-Opioid Receptor.

Gwangju Institute of Science and Technology (GIST)
28
Discovery of Orally Bioavailable Phthalazinone Analogues as an ENPP1 Inhibitor for STING-Mediated Cancer Immunotherapy.

Ajou University
23
Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones.

Lg Life Sciences
1
Perspective for Discovery of Small Molecule IL-6 Inhibitors through Study of Structure-Activity Relationships and Molecular Docking.

Dongguk University
1
Discovery of 2-aminoquinolone acid derivatives as potent inhibitors of SARS-CoV-2.

Seoul National University
28
Synthesis and biological evaluation of N-(3-fluorobenzyl)-4-(1-(methyl-d

Sungkyunkwan University
4
Pharmacophore-based virtual screening: the discovery of novel methionyl-tRNA synthetase inhibitors.

Seoul National University
65
Discovery of Novel Sphingosine-1-Phosphate-1 Receptor Agonists for the Treatment of Multiple Sclerosis.

Korea Institute of Science & Technology (Kist)
7
Protein tyrosine phosphatase 1B inhibitors from Morus root bark.

Korea Research Institute of Bioscience and Biotechnology (Kribb)
24
Discovery of 5,7-Dihydro-6

Incyte
16
Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain.

Merck Research Laboratories
3
Synthesis of 15R-PGD2: a potential DP2 receptor agonist.

Florida Institute of Technology
2
Identification of a Target Site for Covalent Inhibition of Protein Phosphohistidine Phosphatase 1.

Ulsan National Institute of Science and Technology (UNIST)
18
Discovery of benzodioxane analogues as lead candidates of AIMP2-DX2 inhibitors.

Institut Pasteur Korea
27
Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers.

Merck Research Laboratories
15
Novel diarylsulfonylurea derivatives as potent antimitotic agents.

Lg Life Sciences
17
Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains.

Merck Research Laboratories
17
Estrogen receptor ligands. Part 7: Dihydrobenzoxathiin SERAMs with bicyclic amine side chains.

Merck Research Laboratories
1
Optimization and Evaluation of Novel Antifungal Agents for the Treatment of Fungal Infection.

Korea Institute of Science & Technology (Kist)
3
Computational Design of Potent D-Peptide Inhibitors of SARS-CoV-2.

University of Toronto
37
A Novel, Selective c-Abl Inhibitor, Compound 5, Prevents Neurodegeneration in Parkinson's Disease.

Johns Hopkins University School of Medicine
32
Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.

Merck Research Laboratories
16
Discovery of diarylacrylonitriles as a novel series of small molecule sortase A inhibitors.

Seoul National University
16
Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs.

Merck Research Laboratories
12
Estrogen receptor ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptor alpha modulators.

Merck Research Laboratories
42
Identification of Thieno[3,2-

Yonsei University College of Medicine
2
Discovery of novel potent migrastatic Thiazolo[5,4-b]pyridines targeting Lysyl-tRNA synthetase (KRS) for treatment of Cancer metastasis.

Cha University
18
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.

Genomics Institute of The Novartis Research Foundation
10
Discovery of 6-substituted thieno[2,3-d]pyrimidine analogs as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis in folate receptor expressing human tumors.

Wayne State University School of Medicine
65
Development and optimization of halogenated vinyl sulfones as Nrf2 activators for the treatment of Parkinson's disease.

Korea Institute of Science & Technology (Kist)
3
Discovery of Leucyladenylate Sulfamates as Novel Leucyl-tRNA Synthetase (LRS)-Targeted Mammalian Target of Rapamycin Complex 1 (mTORC1) Inhibitors.

Seoul National University
45
Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.

Daegu-Gyeongbuk Medical Innovation Foundation
22
Discovery of 2-((R)-4-(2-Fluoro-4-(methylsulfonyl)phenyl)-2-methylpiperazin-1-yl)-N-((1R,2s,3S,5S,7S)-5-hydroxyadamantan-2-yl)pyrimidine-4-carboxamide (SKI2852): A Highly Potent, Selective, and Orally Bioavailable Inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1).

Sk Chemicals
13
Design, synthesis, and discovery of novel trans-stilbene analogues as potent and selective human cytochrome P450 1B1 inhibitors.

Seoul National University
30
Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma.

Ontario Institute For Cancer Research
4
Dual Binding to Orthosteric and Allosteric Sites Enhances the Anticancer Activity of a TRAP1-Targeting Drug.

Ulsan National Institutes of Science and Technology (Unist)
57
Potent Suppressive Effects of 1-Piperidinylimidazole Based Novel P2X7 Receptor Antagonists on Cancer Cell Migration and Invasion.

Gwangju Institute of Science and Technology (Gist)
8
Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.

Pusan National University
4
2-Aminophenylpyrimidines as Novel Inhibitors of Aminoacyl-tRNA Synthetase Interacting Multifunctional Protein 2 (AIMP2)-DX2 for Lung Cancer Treatment.

Cha University
12
Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.

Janssen Research and Development
13
Benzylamine-based selective and orally bioavailable inhibitors of thrombin.

Biotech Research Institute
3
Synthesis and Structure-Activity Relationships of Arylsulfonamides as AIMP2-DX2 Inhibitors for the Development of a Novel Anticancer Therapy.

Dongguk University-Seoul
10
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.

Biotech Research Institute
54
Optimization of Vinyl Sulfone Derivatives as Potent Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Activators for Parkinson's Disease Therapy.

Korea Institute of Science & Technology (Kist)
4
Adaptable Small Ligand of CYP1 Enzymes for Use in Understanding the Structural Features Determining Isoform Selectivity.

Seoul National University
1
Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors.

Korea Research Institute of Chemical Technology
10
Bis(indole) alkaloids as sortase A inhibitors from the sponge Spongosorites sp.

Seoul National University
24
Small molecule inhibitors of anthrax edema factor.

Hawaii Biotech
48
Synthesis and evaluation of biaryl derivatives for structural characterization of selective monoamine oxidase B inhibitors toward Parkinson's disease therapy.

Yonsei University
2
Dehydrodiconiferyl Alcohol Inhibits Osteoclast Differentiation and Ovariectomy-Induced Bone Loss through Acting as an Estrogen Receptor Agonist.

Seoul National University
43
Discovery and evaluation of 3,5-disubstituted indole derivatives as Pim kinase inhibitors.

Keimyung University
2
Discovery of simplified leucyladenylate sulfamates as novel leucyl-tRNA synthetase (LRS)-targeted mammalian target of rapamycin complex 1 (mTORC1) inhibitors.

Seoul National University
46
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.

Novartis Institutes For Biomedical Research
9
Autotaxin inhibitors and uses thereof

Df 2024 IP Acquisition
19
Compounds useful for inhibiting RAF dimers

Albert Einstein College of Medicine
66
NOVEL COMPOUND AND USE THEREOF FOR INHIBITING CHECKPOINT KINASE 2

Arum Therapeutics
12
Nitrile derivative that acts as inhibitor of dipeptidyl peptidase 1 and use thereof

Haisco Pharmaceuticals
48
Heteroaryl-substituted sulfonamide compounds and their use as therapeutic agents

Xenon Pharmaceuticals
27
Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds

Eli Lilly
76
Pyrazolopyridine compounds and uses thereof

Incyte
87
Spirocyclic compounds

Recurium Ip Holdings
182
Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors

Forma Therapeutics
274
PRMT5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof

Epizyme
589
Sulfone amide linked benzothiazole inhibitors of endothelial lipase

Bristol Myers Squibb
54
Indazole compounds and uses thereof

Incyte
122
Pyrrolidine compounds

Hoffmann-La Roche
2
Spectroscopic and Computational Investigations of Ligand Binding to IspH: Discovery of Non-diphosphate Inhibitors.

University of Illinois
28
Transformation of the Non-Selective Aminocyclohexanol-Based Hsp90 Inhibitor into a Grp94-Seletive Scaffold.

The University of Kansas
27
Structure-activity relationship studies of benzyl-, phenethyl-, and pyridyl-substituted tetrahydroacridin-9-amines as multitargeting agents to treat Alzheimer's disease.

University of Waterloo
217
Pharmaceutical compounds

Astex Therapeutics
211
Substituted pyrimidines for the treatment of diseases such as cancer

Boehringer Ingelheim International
15
Organophosphorous Compounds and Uses Thereof

Jal Therapeutics
6
Kinetics Studies on the Inhibition Mechanism of Pancreatic ±-Amylase by Glycoconjugated 1H-1,2,3-Triazoles: A New Class of Inhibitors with Hypoglycemiant Activity.

Yonsei University
7
Creating an a7 Nicotinic Acetylcholine Recognition Domain from the Acetylcholine-binding Protein

Uc San Diego
10
Comparison of [Dmt1]DALDA and DAMGO in binding and G protein activation at mu, delta, and kappa opioid receptors.

Cornell University
9
DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters.

Suntory Institute For Bioorganic Research
5
Cloning and pharmacologic characterization of a thromboxane A2 receptor from K562 (human chronic myelogenous leukemia) cells.

University of Cincinnati
8
Design, synthesis, and biological evaluation of new 5-HT4 receptor agonists: application as amyloid cascade modulators and potential therapeutic utility in Alzheimer's disease.

Cnrs
11
Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists.

Acadia Pharmaceuticals