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Ion Channels Focused Library

Ion Channels Focused Library

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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
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