PMID
Data
Article Title
Organization
Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors.

Central China Normal University
Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.

Glaxosmithkline
Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.

Merck Research Laboratories
Bicyclic [3.3.0]-Octahydrocyclopenta[c]pyrrolo Antagonists of Retinol Binding Protein 4: Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease.

Columbia University Medical Center
Effect of the tyrosinase inhibitor (S)-N-trans-feruloyloctopamine from garlic skin on tyrosinase gene expression and melanine accumulation in melanoma cells.

Gansu College of Traditional Chinese Medicine
Design, synthesis, and evaluation of nonretinoid retinol binding protein 4 antagonists for the potential treatment of atrophic age-related macular degeneration and Stargardt disease.

Albany Molecular Research
The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist.

Merck Research Laboratories
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.

Merck
Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain.

Bristol-Myers Squibb
Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: profile of clinical candidate (2R,3S,5R)-2-(2,5-difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine (23).

Merck Research Laboratories
2-Substituted 4,5-dihydrothiazole-4-carboxylic acids are novel inhibitors of metallo-ß-lactamases.

Baylor College of Medicine
Synthesis and structure-activity relationship investigation of adenosine-containing inhibitors of histone methyltransferase DOT1L.

Baylor College of Medicine
Synthesis, fluorine-18 radiolabeling, and biological evaluation of N-((E)-4-fluorobut-2-en-1-yl)-2beta-carbomethoxy-3beta-(4'-halophenyl)nortropanes: candidate radioligands for in vivo imaging of the brain dopamine transporter with positron emission tomography.

Emory University
Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes.

Merck Research Laboratories
Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.

Pfizer
Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties.

Bristol-Myers Squibb
Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.

Bristol-Myers Squibb Pharmaceutical Research Institute
Inhibition of 1-deoxy-D-xylulose-5-phosphate reductoisomerase by lipophilic phosphonates: SAR, QSAR, and crystallographic studies.

Baylor College of Medicine
Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors.

Merck Research Laboratories
Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Bristol-Myers Squibb Research and Development
Discovery of pyrrole-indoline-2-ones as Aurora kinase inhibitors with a different inhibition profile.

Development Center For Biotechnology
3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT(6) receptor modulators.

Wyeth Pharmaceuticals
α-hydroxyamide derived aminodiols as potent inhibitors of hiv protease

TBA
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.

Pfizer
Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1.

Pfizer
Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA.

Bristol-Myers Squibb Research and Development
Fragment-Based Anti-inflammatory Agent Design and Target Identification: Discovery of AF-45 as an IRAK4 Inhibitor to Treat Ulcerative Colitis and Acute Lung Injury.

Wenzhou Medical University
Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr.

Amgen
Identification of the exosomal PD-L1 inhibitor to promote the PD-1 targeting therapy of gastric cancer.

The First Affiliated Hospital of Zhengzhou University
5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors.

Erasca
Cyclization strategy leads to highly potent Bromodomain and extra-terminal (BET) Bromodomain inhibitors for the treatment of acute liver injury.

Fudan University
Design, Synthesis, and Bioevaluation of Novel MyD88 Inhibitor c17 against Acute Lung Injury Derived from the Virtual Screen.

Wenzhou Medical University
New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of the Diphenyl 6-Oxo-1,6-dihydropyridazine-3-carboxylate/carboxamide Analogue J27 for the Treatment of Acute Lung Injury and Sepsis by Targeting JNK2 and Inhibiting the JNK2-NF-κB/MAPK Pathway.

Wenzhou Medical University
Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors.

Wenzhou Medical University
Discovery of a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase: Structural activity relationship and antitumor activity both in vitro and in vivo.

Sichuan University
Identification and Characterization of a Novel Indoleamine 2,3-Dioxygenase 1 Protein Degrader for Glioblastoma.

Northwestern University Feinberg School of Medicine
Discovery of 6,7-dihydro-5H-pyrrolo[3,4-d] pyrimidine derivatives as a new class of ATR inhibitors.

Sichuan University
Discovery of a novel and potent inhibitor with differential species-specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis.

Sichuan University
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis of analogs of (1,4)-3- and 5-imino oxazepane, thiazepane, and diazepane as inhibitors of nitric oxide synthases.

Merck Research Laboratories
Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.

Bristol-Myers Squibb Pharmaceutical Research Institute
Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists.

Merck Research Laboratories
Calcitonin gene-related peptide (CGRP) receptor antagonists: Heterocyclic modification of a novel azepinone lead.

Bristol-Myers Squibb
Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.

Merck Research Laboratories
Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family.

China Pharmaceutical University
Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).

Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of 3,6-disubstutited-imidazo[1,2-a]pyridine derivatives as a new class of CLK1 inhibitors.

Sichuan University
3-cyanoindole-based inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships.

Bristol-Myers Squibb Pharmaceutical Research Institute
Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-Methoxy-4-(5-oxazolyl)phenyl moiety.

Bristol-Myers Squibb Pharmaceutical Research Institute
Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute
Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer.

China Pharmaceutical University
Synthesis and characterization of iodine-123 labeled 2beta-carbomethoxy-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane. A ligand for in vivo imaging of serotonin transporters by single-photon-emission tomography.

Emory University
Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues.

Bristol-Myers Squibb Pri
Novel inhibitors of IMPDH: a highly potent and selective quinolone-based series.

Bristol-Myers Squibb Pri
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.

Merck Research Laboratories
Synthesis and SAR of novel imidazoquinoxaline-based Lck inhibitors: improvement of cell potency.

Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195).

Pfizer
C-3 Amido-indole cannabinoid receptor modulators.

Bristol-Myers Squibb
Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck).

Bristol-Myers Squibb Pharmaceutical Research Institute
Design, synthesis and biological evaluation of imidazolopyridone derivatives as novel BRD4 inhibitors.

China Pharmaceutical University
Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists.

Bristol-Myers Squibb
Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection.

Merck Research Laboratories
Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection.

Merck Research Laboratories
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide.

China Pharmaceutical University
Design, synthesis and biological evaluation of 2,5-dimethylfuran-3-carboxylic acid derivatives as potential IDO1 inhibitors.

China Pharmaceutical University
Design, synthesis and biological evaluation of imidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD9 inhibitors.

China Pharmaceutical University
Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.

Merck Research Laboratories
Synthesis, biodistribution, and primate imaging of fluorine-18 labeled 2beta-carbo-1'-fluoro-2-propoxy-3beta-(4-chlorophenyl)tr opanes. Ligands for the imaging of dopamine transporters by positron emission tomography.

Emory University
Synthesis, biological evaluation, and molecular docking investigation of 3-amidoindoles as potent tubulin polymerization inhibitors.

Southern Medical University
Discovery of potent anti-inflammatory 4-(4,5,6,7-tetrahydrofuro[3,2-c]pyridin-2-yl) pyrimidin-2-amines for use as Janus kinase inhibitors.

Central China Normal University
Discovery of 1,8-disubstituted-[1,2,3]triazolo[4,5-c]quinoline derivatives as a new class of Hippo signaling pathway inhibitors.

Sichuan University
Development of 2-amino-4-phenylthiazole analogues to disrupt myeloid differentiation factor 88 and prevent inflammatory responses in acute lung injury.

Wenzhou Medical University
Pharmacokinetics-Driven Optimization of 7-Methylimidazo[1,5-

China Pharmaceutical University
Discovery of novel, potent, isosteviol-based antithrombotic agents.

Peking University
Design, Synthesis, and Preclinical Efficacy of Novel Nonretinoid Antagonists of Retinol-Binding Protein 4 in the Mouse Model of Hepatic Steatosis.

Albany College of Pharmacy and Health Sciences
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers.

Agios Pharmaceuticals
Discovery of the selective and efficacious inhibitors of FLT3 mutations.

China Pharmaceutical University
Discovery of caffeic acid phenethyl ester derivatives as novel myeloid differentiation protein 2 inhibitors for treatment of acute lung injury.

Wenzhou Medical University
Discovery of non-zwitterionic aryl sulfonamides as Na

Bristol-Myers Squibb Research and Development
Development of spiroguanidine-derivedα7 neuronal nicotinic receptor partial agonists.

Bristol-Myers Squibb Research and Development
TYRO3 INHIBITORS

Halia Therapeutics
IMIDAZO[1,2-A]PYRIDINE COMPOUNDS AND THEIR USE IN THERAPY

Imperial College Innovations
IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS IRAK4 INHIBITORS AND THEIR USE IN THE TREATMENT OF DISEASE

Biogen Ma
FUSED HETEROAROMATIC PYRROLIDINONES

Calithera Biosciences
PLASMA KALLIKREIN INHIBITORS

Merck Sharp & Dohme
Substituted benzene compounds

Epizyme
Compositions and methods for the prevention and/or treatment of mitochondrial disease, including Friedreich's ataxia

Stealth Biotherapeutics
[1,2,4]Triazolo derivatives as PDE1 inhibitors for the treatment of diabetes

Eli Lilly
Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors

Incyte
Substituted bridged diazepane derivatives and use thereof as TASK-1 and TASK-3 inhibitors

Bayer Pharma Aktiengesellschaft
Quinoline compounds as modulators of RAGE activity and uses thereof

TBA
Combinations comprising substituted imidazo[1,5-α]pyrazinones as PDE1 inhibitors

H. Lundbeck
Conjugate comprising a neurotensin receptor ligand and use thereof

3B Pharmaceuticals
Substituted pyrrolidines as G-protein coupled receptor 43 agonists

Epics Therapeutics
Heteroaryl compounds and uses thereof

Celgene Car
Macrocylic compounds as ROS1 kinase inhibitors

Array Biopharma
Kv1.3 inhibitors and their medical applications

4Sc
Bromodomain-inhibiting compounds and pharmaceutical composition comprising same for preventing or treating a cancer

Kainos Medicine
Apoptosis signal-regulating kinase inhibitor

Gilead Sciences
Pyridine-2-amides useful as CB2 agonists

Hoffmann-La Roche
Synthetic Triterpenoid Inhibition of Human Ghrelin O-Acyltransferase: The Involvement of a Functionally Required Cysteine Provides Mechanistic Insight into Ghrelin Acylation.

Syracuse University
Fused heterocyclic derivatives and methods of use

Amgen
Discovery of novel purine-based heterocyclic P2X7 receptor antagonists.

Gwangju Institute of Science and Technology
Benzodioxole or benzodioxepine heterocyclic compounds as phosphodiesterase inhibitors

Leo Pharma
4-(substituted anilino)-quinazoline derivatives useful as tyrosine kinase inhibitors

Qilu Pharmaceutical
Expanding the Scope of Human DNA Polymerase ¿ and ß Inhibitors.

University of Konstanz
Fused pyrrolidino-cyclopropane derivatives as selective 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors

Merck Patent
Generation of oxamic acid libraries: antimalarials and inhibitors of Plasmodium falciparum lactate dehydrogenase.

University of Mississippi
RP 73870, a gastrin/cholecystokinin-B receptor antagonist with potent anti-ulcer activity in the rat.

Rhone-Poulenc Rorer Central Research
Identification of a small-molecule inhibitor of DNA topoisomerase II by proteomic profiling.

Riken Advanced Science Institute
Inhibitors of indoleamine 2,3-dioxygenase (IDO)

Bristol-Myers Squibb
Pyridine derivatives as soft rock inhibitors

Redx Pharma
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes.

Martin-Luther-University Halle-Wittenberg