Burger line Burger line Burger line
Logo Logo Logo
Burger line Burger line Burger line
Sign in
Sign in

Ion Channels Focused Library

Preferred format:
Desirable size of the custom library selection:
  • Mg
  • uMol


A unique collection of small molecule compounds selected for Ion Channels protein targets
  • Therapeutically relevant 57 ion channels (119 protein sub-families/units targets in total)
  • Recent literature data from 509 research papers and patents published since 2014
  • The most recent (2019 and 2020) X-Ray and Cryo-EM structures from PDB
  • Comprehensive Ion Channels Platform Library : 26,000 compounds

Ion channels are pore-forming proteins that allow the flow of ions across membranes
Physiologically the Ion Channels are regulated by
– voltage, e.g. most Na, K, Ca and some Cl channels are “voltage-gated ion channels”
– intracellular and/or extracellular mediators, e.g. some K and Cl channels, TRP channels, GABA(A) and P2X receptors are “ligand-gated ion channels”
Ion channels are well recognized as important therapeutic targets for diseases of
– the central nervous system (CNS), e.g. sleep disorders, anxiety, epilepsy, pain
– the peripheral nervous system, e.g. anticonvulsant, analgesic, anti-inflammatory
– the cardiovascular system, e.g. ischemia, hypoxic conditions, stroke


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
0
Cart Subtotal:
Go to cart
You will be able to Pay Online or Request a Quote

We use "cookies*  to ensure the functionality of our website, recognise your browser or device, learn more about your interests, and provide you with essential features and services and for additional purposes, including:

Recognising you when you sign-in to use our services. This allows us to provide you with product recommendations, display personalised content, and provide other customised features and services.
Keeping track of your specified preferences. You may set your preferences through Your Account..
Keeping track of items stored in your shopping basket and personal cabinet.
Conducting research and diagnostics to improve ChemDiv’s content, products, and services.
Delivering content, including ads, relevant to your interests on ChemDiv’s site
Reporting. This allows us to measure and analyse the performance of our services.

By  cookies you give consent to the processing of your personal data, including transfer to third parties. Further information can be found in our privacy policy.

Accept all cookies