PMID

Data

Article Title

Organization

Discovery of diamide compounds as diacylglycerol acyltransferase 1 (DGAT1) inhibitors.

Novartis Institutes For Biomedical Research

Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3.

Pfizer

Discovery and optimization of adamantane carboxylic acid derivatives as potent diacylglycerol acyltransferase 1 inhibitors for the potential treatment of obesity and diabetes.

Korea Research Institute Of Chemical Technology

Discovery of a Novel Series of N-Phenylindoline-5-sulfonamide Derivatives as Potent, Selective, and Orally Bioavailable Acyl CoA:Monoacylglycerol Acyltransferase-2 Inhibitors.

Takeda Pharmaceutical

Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.

Merck Research Laboratories

Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors.

Merck Research Laboratories

Discovery of novel quinoline carboxylic acid series as DGAT1 inhibitors.

Merck Research Laboratories

Synthesis and evaluation of cyclohexane carboxylic acid head group containing isoxazole and thiazole analogs as DGAT1 inhibitors.

Vit University

Discovery of 6-phenylpyrimido[4,5-b][1,4]oxazines as potent and selective acyl CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitors with in vivo efficacy in rodents.

Amgen

Identification of 2-aminooxazole amides as acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) inhibitors through scaffold hopping strategy.

Merck Research Laboratories

Defining the key pharmacophore elements of PF-04620110: discovery of a potent, orally-active, neutral DGAT-1 inhibitor.

Pfizer

Synthesis and biological evaluation of aminobenzimidazole derivatives with a phenylcyclohexyl acetic acid group as anti-obesity and anti-diabetic agents.

Korea Research Institute Of Chemical Technology

Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety.

Merck Research Laboratories

Evaluation of thiazole containing biaryl analogs as diacylglycerol acyltransferase 1 (DGAT1) inhibitors.

Piramal Enterprises

Identification and design of a novel series of MGAT2 inhibitors.

Astrazeneca

Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors.

Merck Research Laboratories

Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).

Astrazeneca

Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of acyl-CoA:diacylglycerol acyltransferase 1.

Abbott Laboratories

Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides.

TBA

Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.

Astrazeneca

Thiadiazoles as new inhibitors of diacylglycerol acyltransferase type 1.

Sanofi-Aventis R&D

Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1.

TBA

Design and synthesis of potent carboxylic acid DGAT1 inhibitors with high cell permeability.

Prosidion

Discovery and optimization of 2-phenyloxazole derivatives as diacylglycerol acyltransferase-1 inhibitors.

Roche Research Center

Design and synthesis of potent, orally-active DGAT-1 inhibitors containing a dioxino[2,3-d]pyrimidine core.

Pfizer

Exploration of pyridine containing heteroaryl analogs of biaryl ureas as DGAT1 inhibitors.

Piramal Life Sciences

Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes.

Hoffmann-La Roche

5-amino-pyrazoles as potent and selective p38a inhibitors.

Bristol-Myers Squibb Research And Development

Discovery of pyrrolopyridazines as novel DGAT1 inhibitors.

Amgen

Novel acyl coenzyme A (CoA): diacylglycerol acyltransferase-1 inhibitors: synthesis and biological activities of diacylethylenediamine derivatives.

Takeda Pharmaceutical

Synthesis and multiparametric evaluation of thiadiazoles and oxadiazoles as diacylglycerol acyltransferase type 1 inhibitors.

Sanofi-Aventis R&D

Discovery and Pharmacology of a Novel Class of Diacylglycerol Acyltransferase 2 Inhibitors.

Merck

Practical application of ligand efficiency metrics in lead optimisation.

Astrazeneca

Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1.

Glaxosmithkline

Discovery of dimethyl pent-4-ynoic acid derivatives, as potent and orally bioavailable DGAT1 inhibitors that suppress body weight in diet-induced mouse obesity model.

Wuxi Apptec (Shanghai)

Embarking on a Chemical Space Odyssey.

University Of Leeds

Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors.

Merck

Discovery of a low-systemic-exposure DGAT-1 inhibitor with a picolinoylpyrrolidine-2-carboxylic acid moiety.

Xinxiang Medical University

Discovery of an Orally Bioavailable Benzimidazole Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitor That Suppresses Body Weight Gain in Diet-Induced Obese Dogs and Postprandial Triglycerides in Humans.

Novartis Institutes For Biomedical Research

Unsaturated phosphinic analogues of gamma-aminobutyric acid as GABA(C) receptor antagonists.

University Of Sydney

Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility.

The Scripps Research Institute

Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds.

Scripps Florida

Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes.

Boehringer Ingelheim Pharmaceuticals