PMID

Data

Article Title

Organization

Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.

Glaxosmithkline

Synthesis and optimization of novela-phenylglycinamides as selective TRPM8 antagonists.

Kissei Pharmaceutical

Identification of orally-bioavailable antagonists of the TRPV4 ion-channel.

Renovis

Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain.

Pfizer

Effect of acyclic monoterpene alcohols and their derivatives on TRP channels.

Sapienza University of Rome

Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist.

Raqualia Pharma

Discovery, optimization, and biological evaluation of 5-(2-(trifluoromethyl)phenyl)indazoles as a novel class of transient receptor potential A1 (TRPA1) antagonists.

Genomics Institute of The Novartis Research Foundation

Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists.

Amgen

Serendipity in drug-discovery: a new series of 2-(benzyloxy)benzamides as TRPM8 antagonists.

Pfizer

Synthesis and pharmacological evaluation of novel N-aryl-3,4-dihydro-1'H-spiro[chromene-2,4'-piperidine]-1'-carboxamides as TRPM8 antagonists.

Glenmark Pharmaceuticals

Ion channels as therapeutic targets: a drug discovery perspective.

Pfizer

Design and optimization of benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonists.

Janssen Pharmaceutica

Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists.

Abbott Laboratories

Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents.

Ferrara University

Discovery of vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia.

Janssen Pharmaceutica

Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.

Amgen

5-benzyloxytryptamine as an antagonist of TRPM8.

Renovis

TRPM8 voltage sensor mutants reveal a mechanism for integrating thermal and chemical stimuli.

Ku Leuven

Discovery of (S)-N-(3-isopropylphenyl)-2-(5-phenylthiazol-2-yl)pyrrolidine-1-carboxamide as potent and brain-penetrant TRPV1 antagonist.

Henan University

The discovery of (1R, 3R)-1-(3-chloro-5-fluorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-6-carbonitrile, a potent and selective agonist of human transient receptor potential cation channel subfamily m member 5 (TRPM5) and evaluation of as a potential gastrointestinal prokinetic agent.

Turning Point Therapeutics

Phytocannabinoid Pharmacology: Medicinal Properties of

Scientus Pharma

Design, synthesis and biological evaluation of new thiazole scaffolds as potential TRPM8 antagonists.

Dipartimento Di Scienze Fisiche E Chimiche Universit£

The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.

Peking University

From High-Throughput Screening to Target Validation: Benzo[

Aptuit, An Evotec

Structural and in Vitro Functional Characterization of a Menthyl TRPM8 Antagonist Indicates Species-Dependent Regulation.

Marshall University

Identification of N-acyl-N-indanyl-?-phenylglycinamides as selective TRPM8 antagonists designed to mitigate the risk of adverse effects.

Kissei Pharmaceutical

Exploration of TRPM8 Binding Sites by ?-Carboline-Based Antagonists and Their In Vitro Characterization and In Vivo Analgesic Activities.

University of Salerno

Onydecalins, Fungal Polyketides with Anti- Histoplasma and Anti-TRP Activity.

University of Utah

Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model.

TBA

N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.

University of Hull

Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity.

University of Salerno

Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine.

TBA

Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4).

TBA

Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors.

Peking University

Identification of a Novel TRPM8 Agonist from Nutmeg: A Promising Cooling Compound.

Kao

Discovery and development of a novel class of phenoxyacetyl amides as highly potent TRPM8 agonists for use as cooling agents.

Senomyx

Discovery of a Potent (4 R,5 S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling.

Pharmaron-Beijing