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

N-(2-Alkyleneimino-3-phenylpropyl)acetamide Compounds and Their Use against Pain and Pruritus via Inhibition of TRPA1 Channels.

Temple University

Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.

Amgen

TRPA1 channels as targets for resveratrol and related stilbenoids.

Sapienza University of Rome

a-Aryl pyrrolidine sulfonamides as TRPA1 antagonists.

Genentech

Structure-Activity Relationship Study on Isothiocyanates: Comparison of TRPA1-Activating Ability between Allyl Isothiocyanate and Specific Flavor Components of Wasabi, Horseradish, and White Mustard.

University of Shizuoka

Development of novel azabenzofuran TRPA1 antagonists as in vivo tools.

Amgen

Discovery of a series of aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamides as TRPA1 antagonists.

Astrazeneca

Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives.

University of Shizuoka

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

Discovery of a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine and a 1-aryloxyisoquinoline series of TRPA1 antagonists.

Astrazeneca

Activation and inhibition of thermosensitive TRP channels by voacangine, an alkaloid present in Voacanga africana, an African tree.

University of Shizuoka

3-Ylidenephthalides as a new class of transient receptor potential channel TRPA1 and TRPM8 modulators.

Sapienza University of Rome

The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore.

Glaxosmithkline

Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: modulation at the N-portion and distal phenyl ring.

Sapienza University of Rome

Ion channels as therapeutic targets: a drug discovery perspective.

Pfizer

Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds.

Sapienza University of Rome

N-1-Alkyl-2-oxo-2-aryl amides as novel antagonists of the TRPA1 receptor.

Astrazeneca

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

Ferrara University

Noxious compounds activate TRPA1 ion channels through covalent modification of cysteines.

The Scripps Research Institute

7-Substituted-pyrrolo[3,2-d]pyrimidine-2,4-dione derivatives as antagonists of the transient receptor potential ankyrin 1 (TRPA1) channel: a promising approach for treating pain and inflammation.

University of Ferrara

Tricyclic 3,4-dihydropyrimidine-2-thione derivatives as potent TRPA1 antagonists.

Janssen Pharmaceutica

Design and pharmacological evaluation of PF-4840154, a non-electrophilic reference agonist of the TrpA1 channel.

Pfizer

Analogues of morphanthridine and the tear gas dibenz[b,f][1,4]oxazepine (CR) as extremely potent activators of the human transient receptor potential ankyrin 1 (TRPA1) channel.

Johnson & Johnson Pharmaceutical Research & Development

Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands.

Sapienza University of Rome

Oxime derivatives related to AP18: Agonists and antagonists of the TRPA1 receptor.

Renovis

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

Novel Tetrazole Derivatives as TRPA1 Inhibitors for Treating Idiopathic Lung Disease or Cough.

Smith, Gambrell & Russell

Tetrazole Derivatives as TRPA1 Inhibitors for Treating Idiopathic Lung Disease or Cough.

Smith, Gambrell & Russell

Phytocannabinoid Pharmacology: Medicinal Properties of

Scientus Pharma

Photosensitive and Photoswitchable TRPA1 Agonists Optically Control Pain through Channel Desensitization.

Qingdao University Medical College

Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists May Provide a Superior Treatment for Pain and Migraine.

Therachem Research Medilab

A Retrospective Look at the Impact of Binding Site Environment on the Optimization of TRPA1 Antagonists.

Genentech

From High-Throughput Screening to Target Validation: Benzo[

Aptuit, An Evotec

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

Kissei Pharmaceutical

Discovery of natural TRPA1 activators through pharmacophore-based virtual screening and a biological assay.

Kyoto University Shogoin-Kawaharacho

Identification of a new class of non-electrophilic TRPA1 agonists by a structure-based virtual screening approach.

Kyoto University

Plumbagin, Juglone, and Boropinal as Novel TRPA1 Agonists.

Universit£T Leipzig

Medicinal properties of terpenes found in Cannabis sativa and Humulus lupulus.

Univerisity of Eastern Finland (Uef)

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

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

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

Kao

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

Discovery of a Series of Indazole TRPA1 Antagonists.

Pfizer

Synthesis of resveratrol derivatives as new analgesic drugs through desensitization of the TRPA1 receptor.

Hyogo University of Health Sciences

A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic.

University of British Columbia

Ethylene biosynthesis: processing of a substrate analog supports a radical mechanism for the ethylene-forming enzyme.

Duke University

Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.

The Institute For Diabetes Discovery