imaprelimab   Click here for help

GtoPdb Ligand ID: 9805

Synonyms: PRX-003 | PRX003
Immunopharmacology Ligand
Compound class: Antibody
Comment: Imaprelimab (PRX-003) is an anti-MCAM mAb developed as a novel therapy for psoriasis. In patients with autoimmune diseases, a subset of MCAM+ve T cells (which have an effector memory T-helper 17 phenotype) produce high levels of pro-inflammatory IL-17 [1,3]. Pharmacological disruption of MCAM function is thought to be a valid mechanism for the treatment of autoimmune inflammation. Peptide sequence alignments identify imaprelimab as one of the preferred antibodies claimed in patent WO2014039975 [2] (SEQ IDs 119 and 123 match the sequences submitted to the WHO for INN imaprelimab). These peptide sequences map to the construct identified as h2120VH5/L3.
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Bioactivity Comments
The affinity constant for antibody h2120VH5/L3 binding to human MCAM provided in WO2014039975 [2] appears to be quoted in μg/ml. Based on an average molecular weight of ~150kDa for an antibody the Kd of 1.3 μg/ml provided, converts to ~8.7nM..
Selectivity at other protein targets
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
melanoma cell adhesion molecule Primary target of this compound Hs Antibody Binding 8.1 pKd - 2
pKd 8.1 (Kd 8.7x10-9 M) [2]