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Booklet: InCELL Pulse™ Target Engagement Kinase Reference Set

Posted: 7 February 2017 | | No comments yet

Monitoring cellular drug permeability and target engagement enables assessment of compound efficacy and confirmation of mode of action. InCELL Pulse target engagement assays provide the ability to confirm compound cell entry and target engagement while overcoming limitations of current target engagement assays…

Monitoring cellular drug permeability and target engagement enables assessment of compound efficacy and confirmation of mode of action. InCELL Pulse target engagement assays provide the ability to confirm compound cell entry and target engagement while overcoming limitations of current target engagement assays. These simple binding assays require no target-specific chemical tracer or antibody reagents and provide a convenient solution when functional assays are difficult or unavailable. Additionally, these assays are designed for screening inhibitors, validating hits identified in biochemical assays, measuring cellular EC50 values, and ranking compounds – all in the cellular environment.

InCELL Pulse has been successfully applied to rapidly measure quantitative cellular target engagement potency values for inhibitors of diverse protein classes, including kinases, methyltransferases, and hydrolases. This reference set booklet demonstrates the broad utility for InCELL Pulse across the human kinome, where we have validated assays for kinases from seven of the eight phylogenetic groups.

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