abrilumab   Click here for help

GtoPdb Ligand ID: 11531

Synonyms: AMG 181 | AMG-181 | MEDI-7183 | MEDI7183
Immunopharmacology Ligand
Compound class: Antibody
Comment: Abrilumab (AMG-181, MEDI-7183) is a fully human IgG2κ monoclonal antibody which selectively targets α4β7 integrin heterodimers [1] that was developed by MedImmune. It was designed for the treatment of inflammatory bowel diseases (ulcerative colitis [2], and Crohn's disease).
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Bioactivity Comments
Abrilumab is selective for α4β7 heterodimers and does not bind to α4β1 or αEβ7 integrins [1]. It does not disrupt VCAM-1-mediated T cell adhesion in the vascular endothelium.
Selectivity at catalytic receptors
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
integrin, alpha 4 subunit (antigen CD49D, alpha 4 subunit of VLA-4 receptor) Hs Antibody Inhibition 11.1 pKd - 1
pKd 11.1 (Kd 9x10-12 M) [1]
Description: Binding affinity for α4β7 receptors expressed on the surface of HuT78 cells.