PMID
Cmpds
Data
Article Title
Organization
29
Adamantyl Antiestrogens with Novel Side Chains Reveal a Spectrum of Activities in Suppressing Estrogen Receptor Mediated Activities in Breast Cancer Cells.

The Scripps Research Institute
2
Conformationally restricted phenothiazine neuroleptics. 1. 3-(Dimethylamino)-1,2,3,4-tetrahydroazepino[3,2,1-kl]phenothiazine.

TBA
25
Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors.

Korea Institute of Science and Technology
28
Synthesis and biological evaluation of novel 4-hydroxytamoxifen analogs as estrogen-related receptor gamma inverse agonists.

Daegu-Gyeongbuk Medical Innovation Foundation
1
The discovery and the structural basis of an imidazo[4,5-b]pyridine-based p21-activated kinase 4 inhibitor.

Soongsil University
1
Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development.

Merck Research Laboratories
39
Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series.

Arena Pharmaceuticals
32
Design and synthesis of new tricyclic indoles as potent modulators of the S1P1 receptor.

Arena Pharmaceuticals
37
Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists.

Arena Pharmaceuticals
11
(7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists.

Arena Pharmaceuticals
19
Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.

Arena Pharmaceuticals
12
Anti-tyrosinase, antioxidant, and antibacterial activities of novel 5-hydroxy-4-acetyl-2,3-dihydronaphtho[1,2-b]furans.

Yeungnam University
38
IV. Discovery of CXCR3 antagonists substituted with heterocycles as amide surrogates: improved PK, hERG and metabolic profiles.

Merck Research Laboratories
4
Design, synthesis, functional and structural characterization of an inhibitor of N-acetylneuraminate-9-phosphate phosphatase: observation of extensive dynamics in an enzyme/inhibitor complex.

Bristol Myers Squibb
6
Discovery of non-LBD inhibitor for androgen receptor by structure-guide design.

Korea Research Institute of Chemical Technology
12
Reversal of P-glycoprotein-mediated MDR by 5,7,3',4',5'-pentamethoxyflavone and SAR.

Chosun University
7
Brominated aromatic furanones and related esters from the ascidian Synoicum sp.

Seoul National University
30
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.

Merck Research Laboratories
34
Dipeptidyl peptidase-4 inhibitor withß-amino amide scaffold: synthesis, SAR and biological evaluation.

Dong-A Pharm.
20
Synthesis and biological evaluation of cyclic sulfamide derivatives as 11ß-hydroxysteroid dehydrogenase 1 inhibitors.

TBA
13
Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases.

Bristol Myers Squibb
4
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.

University Of California
37
Synthesis of potent leukotriene A(4) hydrolase inhibitors. Identification of 3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid.

Pfizer
71
Structure-activity relationship studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase.

Searle Research and Development
32
4-arylphthalazin-1(2H)-one derivatives as potent antagonists of the melanin concentrating hormone receptor 1 (MCH-R1).

Korea Research Institute of Chemical Technology
40
III. Identification of novel CXCR3 chemokine receptor antagonists with a pyrazinyl-piperazinyl-piperidine scaffold.

Merck Research Laboratories
27
Discovery of DA-1229: a potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes.

Dong-A Pharm.
2
Discovery of new inhibitor for PDE3 by virtual screening.

Korea Research Institute of Chemical Technology
57
II. SAR studies of pyridyl-piperazinyl-piperidine derivatives as CXCR3 chemokine antagonists.

Ligand Pharmaceuticals
18
Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Bristol Myers Squibb
32
Novel TNF-a converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases.

Merck Research Laboratories
36
Biaryl substituted hydantoin compounds as TACE inhibitors.

Merck Research Laboratories
18
Synthesis and evaluation of tricyclic derivatives containing a non-aromatic amide as inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).

Jeil Pharmaceutical
34
Discovery and SAR of hydantoin TACE inhibitors.

Merck Research Laboratories
15
Discovery of cyclicsulfonamide derivatives as 11beta-hydroxysteroid dehydrogenase 1 inhibitors.

Korea University
16
Synthesis and bioactivities of heterocyclic lipids as PAF antagonists. 2

TBA
25
Synthesis and bioactivities of heterocyclic lipids as PAF antagonists. 1

TBA
34
Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.

Yuhan Research Institute
8
Effect of novel N-cyano-tetrahydro-pyridazine compounds, a class of cathepsin K inhibitors, on the bone resorptive activity of mature osteoclasts.

Korea Research Institute of Chemical Technology
36
Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA.

Bristol Myers Squibb
14
Design and synthesis of 4-quinolinone 2-carboxamides as calpain inhibitors.

Kyung Hee University
39
Identification of a novel potent CDK inhibitor degrading cyclinK with a superb activity to reverse trastuzumab-resistance in HER2-positive breast cancer in vivo.

Hanyang University
15
Macrocyclization strategy for improving candidate profiles in medicinal chemistry.

Gachon University
30
Synthesis and structure-activity relationship of novel indene N-oxide derivatives as potent peroxisome proliferator activated receptor gamma (PPARgamma) agonists.

Korea Research Institute of Chemical Technology
23
Discovery of CRN04894: A Novel Potent Selective MC2R Antagonist.

Crinetics Pharmaceuticals
5
Oxazolidinones as versatile scaffolds in medicinal chemistry.

University College London
39
Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Bristol Myers Squibb
30
Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist.

Crinetics Pharmaceuticals
16
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.

Pharmaceutical Research Institute
18
N-Benzylbenzamides: a new class of potent tyrosinase inhibitors.

Seoul National University
45
Pyrrolopyridazine MEK inhibitors.

Pharmaceutical Research Institute
25
New dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Bristol Myers Squibb
16
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).

Pharmaceutical Research Institute
11
Synthesis and anti-inflammatory effects of novel pimarane diterpenoid analogs.

Seoul National University
16
Discovery of diarylacrylonitriles as a novel series of small molecule sortase A inhibitors.

Seoul National University
48
Rational design of an indolebutanoic acid derivative as a novel aldose reductase inhibitor based on docking and 3D QSAR studies of phenethylamine derivatives.

Yonsei University
15
Discovery of a Hydroxypyridinone APJ Receptor Agonist as a Clinical Candidate.

Bristol Myers Squibb
18
Synthesis of imidazopyridines and purines as potent inhibitors of leukotriene A4 hydrolase.

Pfizer
26
Pyrrolidine and piperidine analogues of SC-57461A as potent, orally active inhibitors of leukotriene A(4) hydrolase.

Pharmacia
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
6
Recent applications of hydantoin and thiohydantoin in medicinal chemistry.

College of Pharmacy and Gachon Institute of Pharmaceutical Science
31
Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity.

Bristol Myers Squibb
14
Discovery of BR102375, a new class of non-TZD PPARγ full agonist for the treatment of type 2 diabetes.

Boryung Pharmaceuticals
36
Discovery of Potent, Selective, and Orally Bioavailable Estrogen-Related Receptor-γ Inverse Agonists To Restore the Sodium Iodide Symporter Function in Anaplastic Thyroid Cancer.

Daegu-Gyeongbuk Medical Innovation Foundation
43
Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase.

Bristol Myers Squibb
11
Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase.

Bristol Myers Squibb
5
Design, synthesis, and biological evaluation of novel pyrrolo[1,2-a]pyrazine derivatives.

Yonsei University
24
Identification of BR101549 as a lead candidate of non-TZD PPARγ agonist for the treatment of type 2 diabetes: Proof-of-concept evaluation and SAR.

Boryung Pharmaceuticals
16
Identification of Reversible Small Molecule Inhibitors of Endothelial Lipase (EL) That Demonstrate HDL-C Increase In Vivo.

TBA
29
Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.

Merck Research Laboratories
7
Meroterpenoids from a Tropical Dysidea sp. Sponge.

Seoul National University
23
Synthesis and evaluation of 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives as glycogen synthase kinase-3 (GSK-3) inhibitors.

Jeil Pharmaceutical
19
Chalcones, inhibitors for topoisomerase I and cathepsin B and L, as potential anti-cancer agents.

Cha University
48
Discovery of (2S)-1-[4-(2-{6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl)sulfanyl]-9H-purin-9-yl}ethyl)piperidin-1-yl]-2-hydroxypropan-1-one (MPC-3100), a purine-based Hsp90 inhibitor.

Myrexis
41
Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors.

University of Pisa
13
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.

Boryung Pharmaceuticals
18
Design, synthesis, and biological evaluation of a series of resorcinol-based N-benzyl benzamide derivatives as potent Hsp90 inhibitors.

Keimyung University
41
Novel Hypoxia-Inducible Factor 1α (HIF-1α) Inhibitors for Angiogenesis-Related Ocular Diseases: Discovery of a Novel Scaffold via Ring-Truncation Strategy.

Seoul National University
12
Selective inhibition of monoamine oxidase A by hispidol.

Sunchon National University
13
Development of a prodrug of hydantoin based TACE inhibitor.

Merck
6
Plasma-induced dimerization of phloridzin as a new class of anti-adipogenic agents.

Daegu University
1
Discovery of an Orally Bioavailable Benzofuran Analogue That Serves as aβ-Amyloid Aggregation Inhibitor for the Potential Treatment of Alzheimer's Disease.

Medifron Dbt
30
Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors.

Merck
7
Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors.

Ulsan National Institutes of Science and Technology (Unist)
2
Methods of treating disorders using CSFIR inhibitors

Deciphera Pharmaceuticals
105
C-LINKED INHIBITORS OF ENL/AF9 YEATS

Bridge Medicines
500
Lactams as CBL-B inhibitors selective over C-CBL

Genentech
76
Pyridinyl sulfonamide derivatives, pharmaceutical compositions and uses thereof

Boehringer Ingelheim International
13
Substituted pyrazolo[1,5-a]pyridine compound, composition containing the same and use thereof

Shenzhen Targetrx
42
Peptide derivatives and uses thereof

Nosopharm
5
Targeted drug rescue with novel compositions, combinations, and methods thereof

Exciva
70
PDE9 inhibitor and use thereof

Nanjing Transthera Biosciences
133
Heterocyclic compounds as kinase inhibitors

Nuvation Bio
47
4,5,6-trisubstituted indazole derivatives, and preparation method and pharmaceutical use thereof

Yangtze River Pharmaceutical Group
812
Substituted isoindolin-1-ones and 2,3-dihydro-1h-pyrrolo[3,4-c]pyridin-1-ones as HPK1 antagonists

Nimbus Saturn
50
Therapeutic agent for FGFR inhibitor-resistant cancer

Taiho Pharmaceutical
89
OXA-Diazaspiro compounds having activity against pain

Esteve Pharmaceuticals
378
Substituted 7-azabicycles and their use as orexin receptor modulators

Janssen Pharmaceutica
45
Substituted pyrrolopyrimidines as HDM2 inhibitors

Merck Sharp & Dohme
20
Cycloalkyl acid derivative, preparation method thereof, and pharmaceutical application thereof

Shanghai Hengrui Pharmaceutical
3
N-sulfonyl homoserine lactone derivatives, preparation method and use thereof

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
8
Protein kinase inhibitors (variants), use thereof in treating oncological diseases and a pharmaceutical composition based thereon

Obshchestvo S Ogranichennoy Otvetstvennostyou “Fusion Pharma”
36
Epoxyeicosatrienoic acid analogs and methods of making and using the same

The Medical College of Wisconsin
8
Carbonic anhydrase inhibitors: Inhibition of human erythrocyte isozymes I and II with a series of phenolic acids.

Ataturk University
25
Dual-site binding of bivalent 4-aminopyridine- and 4-aminoquinoline-based AChE inhibitors: contribution of the hydrophobic alkylene tether to monomer and dimer affinities.

Hong Kong University of Science and Technology
11
Identification of 7-phenylaminothieno- [3,2-b]pyridine-6-carbonitriles as a new class of Src kinase inhibitors.

Wyeth Research
23
Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins.

Hebrew University of Jerusalem
19
Tyrphostins. 6. Dimeric benzylidenemalononitrile tyrophostins: potent inhibitors of EGF receptor tyrosine kinase in vitro.

Hebrew University of Jerusalem