PMID
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Article Title
Organization
Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors.

Bristol-Myers Squibb
Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of thed-opioid receptor.

Bristol-Myers Squibb
Synthesis and pharmacological evaluation of multifunctional tacrine derivatives against several disease pathways of AD.

University of Pisa
Design and synthesis of novel 2-pyrazoline-1-ethanone derivatives as selective MAO inhibitors.

Anhui Medical University
2-Amino-1,3,4-thiadiazoles in the 7-hydroxy-N-neopentyl spiropiperidine indolinyl series as potent P2Y1 receptor antagonists.

Bristol-Myers Squibb
Synthesis and antiproliferative activity of 4-substituted-piperazine-1-carbodithioate derivatives of 2,4-diaminoquinazoline.

Capital Normal University
Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors.

Korea Institute of Science and Technology
Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.

TBA
Design and synthesis of potent, isoxazole-containing renin inhibitors.

Merck Frosst Centre For Therapeutic Research
Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor.

Merck Frosst Centre For Therapeutic Research
Structure-activity relationships and pharmacokinetic parameters of quinoline acylsulfonamides as potent and selective antagonists of the EP(4) receptor.

Merck Frosst Centre For Therapeutic Research
Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors.

Hong Kong University of Science and Technology
3,4-Diarylpiperidines as potent renin inhibitors.

Merck Frosst Center For Therapeutic Research
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of spirocyclic piperidines.

Merck Frosst Centre For Therapeutic Research
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of tertiary alcohol-bearing piperidines.

Merck Frosst Centre For Therapeutic Research
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.

Merck Frosst Centre For Therapeutic Research
Naphthalene/quinoline amides and sulfonylureas as potent and selective antagonists of the EP4 receptor.

Merck Frosst Centre For Therapeutic Research
A novel series of potent and selective EP(4) receptor ligands: facile modulation of agonism and antagonism.

Merck Frosst Canada
Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain.

Merck Frosst Canada
The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.

Merck Frosst Centre For Therapeutic Research
Design, synthesis, and evaluation of novel 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective CXCR2 chemokine receptor antagonists.

Wuxi Pharmatech
The stereochemical requirements of the novel δ-opioid selective dipeptide antagonist TMT-Tic

TBA
Opportunities and perspectives of small molecular phosphodiesterase inhibitors in neurodegenerative diseases.

Qingdao University
Discovery of Novel Mcl-1 Inhibitors with a 3-Substituted-1H-indole-1-yl Moiety Binding to the P1-P3 Pockets to Induce Apoptosis in Acute Myeloid Leukemia Cells.

Shenyang Pharmaceutical University
Discovery of Pyrido[2,3-d]pyrimidin-7-one Derivatives as Highly Potent and Efficacious Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 (ENPP1) Inhibitors for Cancer Treatment.

Shanghai Institute of Materia Medica
Targeting Myeloid Leukemia-1 in Cancer Therapy: Advances and Directions.

Shenyang Pharmaceutical University
Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500).

Repare Therapeutics, Inc.
Discovery of MK-8768, a Potent and Selective mGluR2 Negative Allosteric Modulator.

Merck
Function-oriented synthesis of Imidazo[1,2-a]pyrazine and Imidazo[1,2-b]pyridazine derivatives as potent PI3K/mTOR dual inhibitors.

East China Normal University
Solid-phase analogue synthesis of caspase-3 inhibitors via palladium-catalyzed amination of 3-bromopyrazinones.

Merck Frosst Centre For Therapeutic Research
Structure-activity relationship (SAR) studies on substituted N-(pyridin-3-yl)-2-amino-isonicotinamides as highly potent and selective glycogen synthase kinase-3 (GSK-3) inhibitors.

Bristol-Myers Squibb
The importance of indole and azaindole scaffold in the development of antitumor agents.

Qingdao University of Science and Technology
Synthesis of Novel Kidney-Type Glutaminase Allosteric Inhibitors Targeting the Critical Lys-320 Residue.

Zhejiang University
Oxetane Promise Delivered: Discovery of Long-Acting IDO1 Inhibitors Suitable for Q3W Oral or Parenteral Dosing.

Pharmaron Beijing
Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.

Merck Frosst Centre For Therapeutic Research
Utilization of Metabolite Identification and Structural Data to Guide Design of Low-Dose IDO1 Inhibitors.

Merck
Optimization of 4,6-Disubstituted Pyrido[3,2-

Shenyang Pharmaceutical University
SAR towards indoline and 3-azaindoline classes of IDO1 inhibitors.

Merck
Novel 1,3,4-oxadiazole compounds inhibit the tyrosinase and melanin level: Synthesis, in-vitro, and in-silico studies.

Kongju National University
Discovery of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold.

Merck
Design, synthesis and biological activity of novel 2,3,4,5-tetra-substituted thiophene derivatives as PI3Kα inhibitors with potent antitumor activity.

Guizhou Medical University
Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.

Shenyang Pharmaceutical University
Carbamate and

Merck
Design, synthesis and biological evaluation of new Axl kinase inhibitors containing 1,3,4-oxadiazole acetamide moiety as novel linker.

Shenyang Pharmaceutical University
Kojyl cinnamate esters are peroxisome proliferator-activated receptor α/γ dual agonists.

Seoul National University
Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors.

Merck
Synthesis and Anticancer Activity of Novel Actinonin Derivatives as HsPDF Inhibitors.

Sun Yat-Sen University
Strategic Incorporation of Polarity in Heme-Displacing Inhibitors of Indoleamine-2,3-dioxygenase-1 (IDO1).

Merck
Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.

Merck
Structure-Based Design of N-(5-Phenylthiazol-2-yl)acrylamides as Novel and Potent Glutathione S-Transferase Omega 1 Inhibitors.

Sichuan University
Discovery of 4-piperazinyl-2-aminopyrimidine derivatives as dual inhibitors of JAK2 and FLT3.

Shenyang Pharmaceutical University
Design, Synthesis, and Biological Evaluation of Imidazo[1,2-

East China Normal University
Synthesis, pharmacological evaluation, and mechanistic study of adefovir mixed phosphonate derivatives bearing cholic acid and l-amino acid moieties for the treatment of HBV.

Guizhou Medical University
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.

Korea University
Biphenyl Acid Derivatives as APJ Receptor Agonists.

Bristol-Myers Squibb
Novel Quinoline-Based P2-P4 Macrocyclic Derivatives As Pan-Genotypic HCV NS3/4a Protease Inhibitors.

Merck Research Laboratories
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.

Shanghai Pharmaceuticals Holding
Peptide HIV-1 integrase inhibitors from HIV-1 gene products.

Tokyo Medical and Dental University
Design, Synthesis, and Biological Evaluation of 4-Quinoline Carboxylic Acids as Inhibitors of Dihydroorotate Dehydrogenase.

University of Michigan
Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold.

Shenyang Pharmaceutical University
HIF-1α inhibitor, preparation method therefor, and pharmaceutical composition for preventing or treating angiogenesis-associated eye disease, containing same as active ingredient

Seoul National University
PYRIDO OXAZINE DERIVATIVES AS ALK5 INHIBITORS

Chiesi Farmaceutici
TRICYCLIC COMPOUNDS AS EGFR INHIBITORS

Qilu Pharmaceutical
SUBSTITUTED 4-([1,2,4]TRIAZOLO[1,5-a]PYRIDIN-6-YL)THIOPHENE-2-CARBOXAMIDE DERIVATIVES AND USE THEREOF

The Johns Hopkins University
Heterocyclic compounds for the inhibition of PASK

Bioenergenix
Pyridazines

Boehringer Ingelheim International
Substituted purines as TLR7 agonists

Primmune Therapeutics
Second generation GRP94-selective inhibitors

University of Kansas
Heteroaryl-substituted sulfonamide compounds and their use as therapeutic agents

Xenon Pharmaceuticals
Indolinone derivatives as inhibitors of maternal embryonic leucine zipper kinase

University Of Texas
Cyclohexene compounds and use thereof

Guangzhou Henovcom Bioscience
KV1.3 inhibitors and their medical application

4Sc
4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase

Eastern Virginia Medical School
6-(6-membered heteroaryl and aryl)isoquinolin-3-yl carboxamides and preparation and use thereof

Samumed
AMIDE DERIVATIVES

Merck Patent
Inhibitors of RET

Blueprint Medicines
2-azabicyclo[3.1.0]hexan-3-one derivatives and methods of use

Genentech
Purine inhibitors of human phosphatidylinositol 3-kinase delta

Merck Sharp & Dohme
Tetrahydroisoquinoline derived PRMT5-inhibitors

Ctxt
Imidazolonylquinolines and the use thereof as ATM kinase inhibitors

Merck Patent
Sulfonamide compounds and uses as TNAP inhibitors

Sanford-Burnham Prebys Medical Discovery Institute
Tricyclic PI3K inhibitor compounds and methods of use

Genentech
Compounds that are ERK inhibitors

Merck Sharp & Dohme
Substituted pyrimidine-5-carboxamides as spleen tyrosine kinase inhibitors

Ziarco Pharma
Sulfonamide derivative and medicinal use thereof

Ea Pharma
Synthesis and HIV-1 RT inhibitory action of novel (4/6-substituted benzo[d]thiazol -2-yl)thiazolidin-4-ones. Divergence from the non-competitive inhibition mechanism.

Aristotle University of Thessaloniki
Triazolopyridinone PDE10 inhibitors

Merck Sharp & Dohme
SF2312 is a natural phosphonate inhibitor of enolase.

University of Texas M. D. Anderson Cancer Center
Structural and Functional Analysis of the Allosteric Inhibition of IRE1a with ATP-Competitive Ligands.

University of Washington
Morpholinylbenzotriazines for use in cancer therapy

Merck Patent
Mechanism of the Flavoprotein l-Hydroxynicotine Oxidase: Kinetic Mechanism, Substrate Specificity, Reaction Product, and Roles of Active-Site Residues.

University of Texas At San Antonio
Anti-inflammatory compound having inhibitory activity against multiple tyrosine kinases and pharmaceutical composition containing same

Korea Institute of Science and Technology
Chemical compounds 542

Astrazeneca
Rosuvastatin and atorvastatin derivatives

Redx Pharma
Design, Synthesis, and Evaluation of Polyamine Deacetylase Inhibitors, and High-Resolution Crystal Structures of Their Complexes with Acetylpolyamine Amidohydrolase.

University of Pennsylvania
Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections.

F. Hoffmann-La Roche
Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates?

Istituto Di Biostrutture E Bioimmagini-Cnr
Hepatitis C virus NS3-4A serine protease inhibitors: use of a P2-P1 cyclopropyl alanine combination for improved potency.

Schering-Plough Research Institute
Novel Indolocarbazole protein kinase C inhibitors with improved biochemical and physicochemical properties.

Tumor Biology Center
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.

Sapienza University of Rome