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

Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 1.

Shionogi

Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 2.

Shionogi

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

Renovis

Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).

Glaxosmithkline

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

Raqualia Pharma

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

Glaxosmithkline

Ion channels as therapeutic targets: a drug discovery perspective.

Pfizer

TRPV4 Antagonists: Potential Treatment for Congestive Heart Failure, Bladder Dysfunctions, and Pain.

Therachem Research Medilab (India)

Optimization of a Novel Series of TRPV4 Antagonists with In Vivo Activity in a Model of Pulmonary Edema.

Glaxosmithkline

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

Modulation of the transient receptor potential vanilloid channel TRPV4 by 4alpha-phorbol esters: a structure-activity study.

Ku Leuven

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

Amgen

Research progress and challenges of TRPV1 channel modulators as a prospective therapy for diabetic neuropathic pain.

The First Affiliated Hospital of Zhengzhou University

Discovery and pharmacological characterization of a novel benzimidazole TRPV4 antagonist with cyanocyclobutyl moiety.

Beijing Institute of Pharmacology and Toxicology

-Guided Rational Drug Design and Synthesis of Novel 4-(Thiophen-2-yl)butanamides as Potent and Selective TRPV1 Agonists.

Magna Gracia 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

Identification, Synthesis, and Characterization of a Major Circulating Human Metabolite of TRPV4 Antagonist GSK2798745.

Glaxosmithkline

From High-Throughput Screening to Target Validation: Benzo[

Aptuit, An Evotec

Modulation of TRPV4 and BKCa for treatment of brain diseases.

Kunming University of Science and Technology

Design and Optimization of an Acyclic Amine Series of TRPV4 Antagonists by Electronic Modulation of Hydrogen Bond Interactions.

Glaxosmithkline

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

Kissei Pharmaceutical

Cannabitwinol, a Dimeric Phytocannabinoid from Hemp,

University of Naples Federico Ii

Recent advances in TRPV4 agonists and antagonists.

Glaxosmithkline

Tetrahydroisoquinoline-Derived Urea and 2,5-Diketopiperazine Derivatives as Selective Antagonists of the Transient Receptor Potential Melastatin 8 (TRPM8) Channel Receptor and Antiprostate Cancer Agents.

National Research Council

Discovery of Novel Transient Receptor Potential Vanilloid 4 (TRPV4) Agonists as Regulators of Chondrogenic Differentiation: Identification of Quinazolin-4(3 H)-ones and in Vivo Studies on a Surgically Induced Rat Model of Osteoarthritis.

Asahi Kasei Medical

Discovery of a novel orally active TRPV4 inhibitor: Part 1. Optimization from an HTS hit.

Astellas Pharma

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

Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.

University of Nebraska Medical Center

Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4).

Glaxosmithkline

Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4).

Glaxosmithkline

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

Iodine-mediated cyclization of cannabigerol (CBG) expands the cannabinoid biological and chemical space.

University of Naples Federico II

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

TBA

Iodine-Promoted Aromatization of p-Menthane-Type Phytocannabinoids.

University of Eastern Piedmont

Pharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain.

Shionogi

Bicyclic fused pyridine compounds as inhibitors of TAM kinases

Array Biopharma

Diacylglycerol acyl transferase 2 inhibitor

Pfizer

Isoquinolones as BTK inhibitors

Boehringer Ingelheim International

Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics

Galderma Research & Development

Characterization of isoprenaline- and salmeterol-stimulated interactions between beta2-adrenoceptors and beta-arrestin 2 using beta-galactosidase complementation in C2C12 cells.

Institute of Cell Signaling