PMID
Data
Article Title
Organization
Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening.

Korea Research Institute of Chemical Technology
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives.

Glaxosmithkline
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives.

Glaxosmithkline
Structure-activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers.

Dongguk University-Seoul
Discovery ofa-mangostin as a novel competitive inhibitor against mutant isocitrate dehydrogenase-1.

Dongguk University
Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3.

Pfizer
Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists.

Chung-Ang University
Bioactive benzofuran derivatives: moracins A-Z in medicinal chemistry.

Dongguk University-Seoul
Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression.

Yonsei University
Synthesis and structure-activity relationship study of chemical probes as hypoxia induced factor-1a/malate dehydrogenase 2 inhibitors.

Dongguk University-Seoul
Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-ß type I receptor kinase as cancer immunotherapeutic/antifibrotic agent.

Ewha Womans University
SAR based design of nicotinamides as a novel class of androgen receptor antagonists for prostate cancer.

Chonnam National University
Synthesis of a novel series of 2-alkylthio substituted naphthoquinones as potent acyl-CoA: cholesterol acyltransferase (ACAT) inhibitors.

Dongguk University-Seoul
Fragment-based discovery of novel and selective mPGES-1 inhibitors Part 1: identification of sulfonamido-1,2,3-triazole-4,5-dicarboxylic acid.

Kyung Hee University
Identification of novel mPGES-1 inhibitors through screening of a chemical library.

Kookmin University
Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors.

Dongguk University-Seoul
Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors.

Dongguk University-Seoul
Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1a inhibitors.

Dongguk University-Seoul
Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).

Glaxosmithkline
Synthesis and pharmacological evaluation of carbamic acid 1-phenyl-3-(4-phenyl-piperazine-1-yl)-propyl ester derivatives as new analgesic agents.

Sk Biopharmaceuticals
Discovery and characterization of small molecule inhibitors of the BET family bromodomains.

Glaxosmithkline
Synthesis and structure-activity relationship of aminopyridines with substituted benzoxazoles as c-Met kinase inhibitors.

Korea Research Institute of Chemical Technology
Design and synthesis of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2-yl)-1H-quinolin-2-ones as VEGFR-2 kinase inhibitors.

Korea Research Institute of Chemical Technology
Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide.

Lg Life Sciences
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.

National Institute of Diabetes and Digestive and Kidney Diseases
Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists.

National Institute of Diabetes
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.

National Institute of Diabetes and Digestive and Kidney Diseases
Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1.

Life Science R & D, Lgci
Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications.

Niddk
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.

TBA
HIF-1a inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.

Dongguk University-Seoul
Structure and property based design, synthesis and biological evaluation of¿-lactam based HDAC inhibitors.

Yonsei University
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.

Konkuk University
Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.

S*Bio
A novel class of highly potent multidrug resistance reversal agents: disubstituted adamantyl derivatives.

Chung-Ang University
Structure-based virtual screening of Src kinase inhibitors.

Konkuk University
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.

University of Cambridge
A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.

GlaxoSmithKline R&D
Discovery of a novel BLT2 antagonist for the treatment of inflammatory airway diseases.

Korea University
DW71177: A novel [1,2,4]triazolo[4,3-a]quinoxaline-based potent and BD1-Selective BET inhibitor for the treatment of acute myeloid leukemia.

Korea Research Institute of Chemical Technology
Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.

Molecular Cancer Research Center
Novel cudraisoflavone J derivatives as potent neuroprotective agents for the treatment of Parkinson's disease via the activation of Nrf2/HO-1 signaling.

Dongguk University-Seoul
Examination of acylated 4-aminopiperidine-4-carboxylic acid residues in the phosphotyrosyl+1 position of Grb2 SH2 domain-binding tripeptides.

National Cancer Institute-Frederick
Perspective for Discovery of Small Molecule IL-6 Inhibitors through Study of Structure-Activity Relationships and Molecular Docking.

Dongguk University
3-Substituted-(5-arylfuran-2-ylcarbonyl)guanidines as NHE-1 inhibitors.

Korea Research Institute of Chemical Technology
Novel allosteric glutaminase 1 inhibitors with macrocyclic structure activity relationship analysis.

Yonsei University College of Medicine
Synthesis of tripeptides as potent Yersinia protein tyrosine phosphatase inhibitors.

Nih
4-Substituted (benzo[b]thiophene-2-carbonyl)guanidines as novel Na+/H+ exchanger isoform-1 (NHE-1) inhibitors.

Korea Research Institute of Chemical Technology
(5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1.

Korea Research Institute of Chemical Technology
Macrocyclization in the design of non-phosphorus-containing Grb2 SH2 domain-binding ligands.

National Cancer Institute-Frederick
Synthesis of a 5-methylindolyl-containing macrocycle that displays ultrapotent Grb2 SH2 domain-binding affinity.

National Cancer Institute-Frederick
Acylsulfonamide-containing PTP1B inhibitors designed to mimic an enzyme-bound water of hydration.

Nih
Tripeptide inhibitors of Yersinia protein-tyrosine phosphatase.

National Cancer Institute-Frederick
Utilization of a beta-aminophosphotyrosyl mimetic in the design and synthesis of macrocyclic Grb2 SH2 domain-binding peptides.

National Cancer Institute-Frederick
Macrocyclization in the design of Grb2 SH2 domain-binding ligands exhibiting high potency in whole-cell systems.

National Cancer Institute-Frederick
Development of a Polo-like Kinase-1 Polo-Box Domain Inhibitor as a Tumor Growth Suppressor in Mice Models.

Korea Basic Science Institute (Kbsi)
Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.

University of Oxford
Synthesis and purine receptor affinity of 6-oxopurine nucleosides and nucleotides containing (N)-methanocarba-pseudoribose rings.

Niddk
Elucidation of Mechanism for Ligand Efficacy at Leukotriene B

Incerebro
Sulfonamide-based 4-anilinoquinoline derivatives as novel dual Aurora kinase (AURKA/B) inhibitors: Synthesis, biological evaluation and in silico insights.

Jouf University
Noncovalent thrombin inhibitors incorporating an imidazolylethynyl P1.

Lg Chemical
Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.

Biotech Research Institute
Thrombin inhibitors based on a propargylglycine template.

Biotech Research Institute
Benzylamine-based selective and orally bioavailable inhibitors of thrombin.

Biotech Research Institute
Potent and efficacious thienylamidine-incorporated thrombin inhibitors.

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

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

Biotech Research Institute
Solid phase synthesis of benzylamine-derived sulfonamide library.

Biotech Research Institute
Development and structure-activity relationship study of SHP2 inhibitor containing 3,4,6-trihydroxy-5-oxo-5H-benzo[7]annulene.

Chungnam University
Maximizing ER-α Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927.

Seragon Pharmaceuticals
Hypoxia-inducible factor-1 inhibitory benzofurans and chalcone-derived diels-alder adducts from Morus species.

Korean Research Institute of Biosciences and Biotechnology
Phenanthroquinolizidine alkaloids from the roots of Boehmeria pannosa potently inhibit hypoxia-inducible factor-1 in AGS human gastric cancer cells.

Korea Research Institute of Bioscience and Biotechnology
Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors.

Korea Research Institute of Bioscience and Biotechnology
Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1.

Korean Research Institute of Biosciences and Biotechnology
Structure-activity relationship studies of a series of novel delta-lactam-based histone deacetylase inhibitors.

Kribb
(Aryloxyacetylamino)benzoic acid analogues: A new class of hypoxia-inducible factor-1 inhibitors.

Korea Research Institute of Bioscience and Biotechnology
Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel delta-lactam-based histone deacetylase (HDAC) inhibitors.

Korea Research Institute of Bioscience and Biotechnology
First macrocyclic 3

Taibah University
Rational approach to highly potent and selective apoptosis signal-regulating kinase 1 (ASK1) inhibitors.

Pfizer
Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer.

TBA
Discovery of novel [1,2,4]triazolo[4,3-a]quinoxaline aminophenyl derivatives as BET inhibitors for cancer treatment.

Korea Research Institute of Chemical Technology
Methyl 3-(3-(4-(2,4,4-Trimethylpentan-2-yl)phenoxy)-propanamido)benzoate as a Novel and Dual Malate Dehydrogenase (MDH) 1/2 Inhibitor Targeting Cancer Metabolism.

Dongguk University
THERAPEUTIC MEDICINE FOR HEART DISEASE OR SKELETAL MUSCLE DISEASE

Shionogi
Deuterated 1-piperazino-3-phenyl indanes for treatment of schizophrenia

H. Lundbeck
SMALL MOLECULE INHIBITION OF DEUBIQUITINATING ENZYME JOSEPHIN DOMAIN CONTAINING 1 (JOSD1) AS A TARGETED THERAPY FOR LEUKEMIAS WITH MUTANT JANUS KINASE 2 (JAK2)

Dana-Farber Cancer Institute
SIGMA-1 RECEPTOR ANTAGONISTS AND THEIR APPLICATIONS

Humanwell Pharmaceutical US
PYRIDINE DERIVATIVES AS MODULATORS OF SORTILIN ACTIVITY

Insusense
MASP-2 inhibitors and methods of use

Omeros
Ethynyl derivatives

Hoffmann-La Roche
6-aryl-7-substituted-3-(1H-pyrazol-5-yl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines as inhibitors of the STAT3 pathway with anti-proliferative activity

University of Pittsburgh
CXCR7 antagonists

Chemocentryx
Substituted isoindolin-1-ones and 2,3-dihydro-1h-pyrrolo[3,4-c]pyridin-1-ones as HPK1 antagonists

Nimbus Saturn
Methods to treat lymphoplasmacytic lymphoma

Dana-Farber Cancer Institute
Pyrrolo[2,3-d]pyrimidine compound or salt thereof

Taiho Pharmaceutical
Methods, assays and compounds for treating bacterial infections by inhibiting methylthioinosine phosphorylase

Albert Einstein College of Medicine
Inhibition of memapsin 1 cleavage in the treatment of diabetes

Oklahoma Medical Research Foundation
Bicyclic aryl and heteroaryl sodium channel inhibitors

Amgen
Vanilloid receptor ligands, pharmaceutical compositions containing them, process for making them, and use thereof for treating pain and other conditions

Gruenenthal
Substituted 3-arylsulfonyl-pyrazolo[1,5-A]pyrimidines, serotonin 5-HT6 receptor antagonists and methods for the production and use thereof

TBA
Photoaffinity labeling of the Ah receptor.

University of Wisconsin
Spiro[9,10-dihydroanthracene]-9,3'-pyrrolidine-a structurally unique tetracyclic 5-HT2A receptor antagonist.

Virginia Commonwealth University
Inactivation of a novel neuropeptide Y/peptide YY receptor gene in primate species.

Yamanouchi Pharmaceutical
Characterization and distribution of putative 5-ht7 receptors in guinea-pig brain.

Syntex Discovery Research
Specific benzodiazepine receptors in rat brain characterized by high-affinity (3H)diazepam binding.

TBA
Affinity reagents that target a specific inactive form of protein kinases.

University of Washington