PMID
Cmpds
Data
Article Title
Organization
11
MARK inhibitors: Declaring a No-Go decision on a chemical series based on extensive DMPK experimentation.

Merck
26
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.

Merck
31
Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia.

Broad Institute
33
Potent benzoazepinone¿-secretase modulators with improved bioavailability.

Merck Research Laboratories
36
Discovery of bisamide-heterocycles as inhibitors of scavenger receptor BI (SR-BI)-mediated lipid uptake.

Marquette University
52
Benzo-fused lactams from a diversity-oriented synthesis (DOS) library as inhibitors of scavenger receptor BI (SR-BI)-mediated lipid uptake.

Marquette University
14
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.

Broad Institute of Mit and Harvard
14
Discovery of N-{N-[(3-cyanobenzene) sulfonyl]-4(R)-(3,3-difluoropiperidin-1-yl)-(l)-prolyl}-4-[(3',5'-dichloro-isonicotinoyl) amino]-(l)-phenylalanine (MK-0617), a highly potent and orally active VLA-4 antagonist.

Merck Research Laboratories
9
Influence of acid surrogates toward potency of VLA-4 antagonist.

Merck Research Laboratories
29
A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells.

TBA
35
Triazoloamides as potent¿-secretase modulators with reduced hERG liability.

Merck Research Laboratories
21
Optimization of Potent Inhibitors of P. falciparum Dihydroorotate Dehydrogenase for the Treatment of Malaria.

TBA
34
Identification and synthesis of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to the alpha 2 delta-1 subunit of voltage gated calcium channel.

Merck Research Laboratories
17
Triazoles as¿-secretase modulators.

Merck Research Laboratories
18
Quinazolinones as¿-secretase modulators.

Merck Research Laboratories
19
Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists.

Merck Research Laboratories
39
3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors.

Merck Research Laboratories
3
The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent.

Merck Research Laboratories
41
Expedited SAR study of high-affinity ligands to the alpha(2)delta subunit of voltage-gated calcium channels: Generation of a focused library using a solution-phase Sn2Ar coupling methodology.

Merck Research Laboratories
22
Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.

Merck Research Laboratories
2
Water soluble prodrug of a COX-2 selective inhibitor suitable for intravenous administration in models of cerebral ischemia.

Merck Research Laboratories
2
Novel approach to pro-drugs of lactones: water soluble imidate and ortho-ester derivatives of a furanone-based COX-2 selective inhibitor.

Merck Research Laboratories
60
Expedited SAR study of an mGluR5 antagonists: generation of a focused library using a solution-phase Suzuki coupling methodology.

Merck Research Laboratories
18
Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.

TBA
18
5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity.

Merck Research Laboratories
25
N-Acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the alpha2delta subunit of voltage gated calcium channels.

Merck Research Laboratories
37
Synthesis and biological evaluation of 6-aryl-6H-pyrrolo[3,4-d]pyridazine derivatives: high-affinity ligands to the alpha 2 delta subunit of voltage gated calcium channels.

Merck Research Laboratories
22
Discovery of novel triazolobenzazepinones as γ-secretase modulators with central Aβ42 lowering in rodents and rhesus monkeys.

Merck Research Laboratories Boston
29
Development of selective tight-binding inhibitors of leukotriene A4 hydrolase.

Scripps Research Institute
4
Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction.

The State University of New Jersey
22
Lead optimization of 4,4-biaryl piperidine amides as γ-secretase inhibitors.

Merck Research Laboratories
7
Purine derivatives as potent gamma-secretase modulators.

Merck Research Laboratories
8
Piperazinyl pyrimidine derivatives as potent gamma-secretase modulators.

Merck Research Laboratories
11
Fluorinated piperidine acetic acids as gamma-secretase modulators.

Merck Research Laboratories
23
Substituted 1,4-methanopyrido[1′,2′:4,5]pyrazino[1,2-a]pyrimidines for treating viral infections

Gilead Sciences
116
Spiro-condensed pyrrolidine derivatives as deubiquitylating enzymes (DUB) inhibitors

Mission Therapeutics
1
Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile.

Broad Institute
7
Substituted 2-[2-(phenyl) ethylamino] alkaneamide derivatives and their use as sodium and/or calcium channel modulators

Newron Pharmaceuticals
9
Ligand structure-activity requirements and phospholipid dependence for the binding of phorbol esters to protein kinase D.

University of Pittsburgh
5
Rofecoxib [Vioxx, MK-0966; 4-(4'-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles.

Merck Frosst Centre For Therapeutic Research
36
NOVEL PYRIDAZINES

Boehringer Ingelheim International