P2pal18S   Click here for help

GtoPdb Ligand ID: 6659

Synonyms: P2pal-18S
Comment: Pepducins are membrane tethered mimics of intracellular loops of the target receptor. They are designed to interact with regions of the target receptor identified as being involved in signal transduction. Pepducins are able to modify receptor activity by flipping across the lipid membrane and where they are able to interact with the targeted portions of the native receptor. P2pal18S is an intracellualr loop 3 pepducin that acts as an antagonist at the PAR2 receptor [1].
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Selectivity at GPCRs
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
PAR2 Hs Antagonist Antagonist 5.4 pIC50 -
pIC50 5.4 (IC50 4x10-6 M)
Description: Measuring antagonism of calcium flux induced by PAR2 agonist SLIGRL.