Ligand id: 7453

Name: crofelemer

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View more information in the IUPHAR Pharmacology Education Project: crofelemer

View interactive charts of activity data from GtoPdb and ChEMBL (where available) across species

Bioactivity Comments
Studies in mouse models report that crofelemer has an inhibitory effect on intestinal cAMP-mediated (active) Cl- and fluid secretion [1]. Patch-clamp analysis of cells stably expressing hCFTR or hANO1, and cAMP and calcium signaling measurements in human colorectal cancer cells (T84 cells) confirm the activity of crofelemer at the proposed human Cl- channels.
Selectivity at ion channels
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Affinity Units Concentration range (M) Reference
CaCC Hs Inhibitor Inhibition 5.2 pIC50 - 2
pIC50 5.2 (IC50 6.5x10-6 M) [2]
CFTR Hs Inhibitor Inhibition 5.2 pIC50 - 2
pIC50 5.2 (IC50 7x10-6 M) [2]