â Realizing the potential of IonWorks screening in a drug discovery ...

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New technologies facilitate an integratedapproach to ion channel drug discoveryIdea Lead development Candidate drugThroughput/capacity1000’s 100’s 10’s 1’sIonWorks(384)QPatch(48)Manual(1 – serial)FLIPR(384)OpusXpress(8)
Electrophysiology has an integralrole in iterative ion channel drug designDesignSYNTHESISFLIPRSingle pointIon channelmodulatorChemical spaceexpansionHT EPHYSElectrophysiologyIC 50 / use dependencyFLIPRretestIC 50• Functional ion channel screeningnot rate limiting• Unique opportunity in ion channeldrug discovery• HTS electrophysiology provides anideal tool to discern detailed SARDrugproperties
Page 1 and 2: Realizing the potential of IonWorks
Page 3: Groton ion channel drug discoveryCN
Page 7 and 8: Assessment of cell growth parameter
Page 9 and 10: Growth kinetics dictate experimenta
Page 11 and 12: Variables influencing assay success
Page 13 and 14: The importance of voltage control o
Page 15 and 16: Sample ion channel recordingPre-com
Page 17 and 18: Assay validation post-relocation•
Page 19 and 20: Resolution approachRe-chlorideE-hea
Page 21 and 22: I-V and inactivation curvesre-visit
Page 23 and 24: Pre- to post-addition current ampli
Page 25 and 26: Summary• Cell line husbandry and
Page 27 and 28: Back-up slides
Page 29 and 30: Kv70Single hole mode70Population pa

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