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Ion Channels Focused Library

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  • Mg
  • uMol


ChemDiv’s focused library of small molecules targeting a variety of ion channels comprises 26,421 compounds.

Our library presents a unique collection of small molecule compounds carefully selected for targeting ion channel protein targets, which are critical components in various therapeutic areas. This collection encompasses an impressive range of 57 ion channels, further broken down into 119 protein sub-families/units, making it highly relevant for a multitude of research applications.

The library contents are backed by recent publication references, with data compiled from more than 500 research papers and patents published since 2014, ensuring that all compounds in the library are at the forefront of current scientific knowledge. Moreover, it incorporates the most recent structural data dated 2019 and 2020, including X-Ray and Cryo-EM structures from the Protein Data Bank, providing valuable insights into the molecular architecture of these targets. As a comprehensive Ion Channels Platform Library, it totally boasts more than 26 thousand compounds, offering a rich resource for researchers and pharmaceutical companies in the pursuit of discovering and developing new ion channels targeting therapeutics. This library not only aids in the advancement of drug discovery but also contributes to a deeper understanding of ion channel functions and their roles in various diseases.

Ion channels are pore-forming proteins that facilitate the flow of ions across cellular membranes. Physiologically, ion channels are regulated by various mechanisms:

Voltage: Most Na, K, Ca, and some Cl channels belong to the 'voltage-gated ion channels,' activated by changes in the cell's electrical potential.

Intracellular and/or extracellular mediators: Some K and Cl channels, transient receptor potential (TRP) channels, GABA(A) receptors, and P2X receptors are 'ligand-gated ion channels,' activated by binding specific molecules.

Ion channels are widely recognized as crucial therapeutic targets for diseases affecting:

●      The central nervous system (CNS), such as sleep disorders, anxiety, epilepsy, and neuropathic pain.

●      The peripheral nervous system, when the ion channel-targeted drugs are used as anticonvulsant, analgesic, and anti-inflammatory treatments.

●      The cardiovascular system, including conditions like coronary heart disease, hypoxic conditions, and stroke.

As gatekeepers of cellular ionic homeostasis, ion channels regulate critical functions in both excitable and non-excitable cells, impacting everything from neuronal signaling and muscle contraction to hormone secretion and immune responses. This makes them key targets for therapeutic intervention in diverse medical fields, including neurology, cardiology, and pain management. The modulation of ion channel activity can rectify aberrant signaling pathways, offering therapeutic solutions for conditions like epilepsy, cardiac arrhythmias, chronic pain, and mood disorders. Furthermore, the specificity and diversity of ion channels, combined with advances in understanding their structural and functional dynamics, have opened up new opportunities for targeted drug design. As a result, ion channels remain a highly attractive and dynamic area in drug discovery, with ongoing research continually revealing novel aspects of their potential as therapeutic targets.


1. J Med Chem 2018(61)8:3641-3659. Discovery of a Potent (4 R5 S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling. Chen H Volgraf M Do S Kolesnikov A Shore DG Verma VA Villemure E Wang L Chen Y Hu B Lu AJ Wu G Xu X Yuen PW Zhang Y Erickson SD Dahl M Brotherton-Pleiss C Tay S Ly JQ Murray LJ Chen J Amm D Lange W Hackos DH Reese RM Shields SD Lyssikatos JP Safina BS Estrada AA.

2. J Med Chem 2018(61)3:695-710. Targeting Acidic Mammalian chitinase Is Effective in Animal Model of Asthma. Mazur M Olczak J Olejniczak S […] Cousido-Siah A Fadel F

Golebiowski A.

3. J Med Chem 2018(61)1:224-250. Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity. Li B Ni S Mao F Chen F Liu Y Wei H Chen W Zhu J Lan L Li J.

4. J Med Chem 2018(61)3:1355-1374. 3-((R)-4-(((R)-6-(2-Bromo-4-fluorophenyl)-5-(ethoxycarbonyl)-2-(thiazol-2-yl)-36-dihydropyrimidin-4-yl)methyl)morpholin-2-yl)propanoic Acid (HEC72702) a Novel Hepatitis B Virus Capsid Inhibitor Based on Clinical Candidate GLS4. Ren Q Liu X Yan G Nie B Zou Z Li J Chen Y Wei Y Huang J Luo Z Gu B Goldmann S Zhang J Zhang Y.

5. J Med Chem 2018(61)1:207-223. A Dipolar Cycloaddition Reaction To Access 6-Methyl-4567-tetrahydro-1H-[123]triazolo[45-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate. Chrovian CC Soyode-Johnson A Peterson AA Gelin CF Deng X Dvorak CA Carruthers NI Lord B Fraser I Aluisio L Coe KJ Scott B Koudriakova T Schoetens F Sepassi K Gallacher DJ Bhattacharya A Letavic MA.

6. J Med Chem 2018(61)1:84-97. Phenotypic Optimization of Urea-Thiophene Carboxamides To Yield Potent Well Tolerated and Orally Active Protective Agents against Aminoglycoside-Induced Hearing Loss. Chowdhury S Owens KN Herr RJ Jiang Q Chen X Johnson G Groppi VE Raible DW Rubel EW Simon JA.

7. J Med Chem 2018(61)8:3685-3696. Discovery of a Novel Small-Molecule Modulator of C-X-C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis. Menhaji-Klotz E

Hesp KD Londregan AT Kalgutkar AS Piotrowski DW Boehm M Song K Ryder T Beaumont K Jones RM Atkinson K Brown JA Litchfield J Xiao J Canterbury DP Burford K Thuma BA Limberakis C Jiao W Bagley SW Agarwal S Crowell D Pazdziorko S Ward J Price DA Clerin V.

8. J Med Chem 2018(61)1:251-264. 7-Phenoxy-Substituted 34-Dihydro-2H-124-benzothiadiazine 11-Dioxides as Positive Allosteric Modulators of Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency. Goffin E Drapier T Larsen AP Geubelle P Ptak CP Laulumaa S Rovinskaja K Gilissen J Tullio P Olsen LFrydenvang K Pirotte B Hanson J Oswald RE Kastrup JS Francotte P.

9. J Med Chem 2017(60)22:9239-9250. Structure-Based Design and Discovery of New M2 Receptor Agonists. Fish I Stößel A Eitel K Valant C Albold S Huebner H Möller D Clark MJSunahara RK Christopoulos A Shoichet BK Gmeiner P.

10. ACS Med Chem Lett 2017(8)1:133-137. Development of 4-Heteroarylamino-1'-azaspiro[oxazole-53'-bicyclo[2.2.2]octanes] as Nicotinic Receptor Agonists. Hill MD Fang H King
HD Iwuagwu CI McDonald IM Cook J Zusi FC Mate RA Knox RJ Post-Munson D Easton A Miller R Lentz K Clarke W Benitex Y Lodge N Zaczek R Denton R Morgan D Bristow L

Macor JE Olson R.

11. J Med Chem 2017(60)16:7029-7042. Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-13-thiazol--ylbenzenesulfonamide

(PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7. Swain NA Batchelor D […] Storer RI Stupple PA West CW.

12. 25-disubstituted-pyridyl nicotinic ligands and methods of use thereof 2016 US-9303017-B2

13. Substituted pyrazoles as N-type calcium channel blockers 2016 US-9434693-B2

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