Compound class:
Synthetic organic
Comment: Inhibitor 1 inhibits the ORAI1 protein component of the CRAC channel [1]. The chemical structure represents a novel ORAI1-specific chemotype that is suitable for the development of more refined CRAC channel inhibitors.
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Bioactivity Comments |
Ca2+ influx mediated by constitutively opened CRAC channels is inhibited by inhibitor 1 with an IC50 of 200 nM, and 30 μM of the compound maximally inhibits the calcium level by ~80% [1]. |
Selectivity at ion channels | ||||||||||||||||||||||||||||||||||
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