Ligand id: 9250

Name: erenumab

Bioactivity Comments
In functional in vitro cell-based assays AMG-334 abolishes CGRP-stimulated cAMP production (IC50 2.3nM), and is 5000-fold selective for the CGRP receptor over other human calcitonin family receptors [7]. AMG-334 has affinity for the cynomolgus monkey CGRP receptor similar to that for the human receptor, but has drastically reduced affinity for the dog, rabbit and rat receptors, excluding these latter species from providing preclinical testing models.
Selectivity at GPCRs
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
CGRP receptor Hs Antibody Antagonist 10.7 pKi - 7
pKi 10.7 (Ki 2x10-11 M) [7]
Description: Displacement binding of [(125)I]-CGRP at the human CGRP receptor