CFZ533   Click here for help

GtoPdb Ligand ID: 9802

Synonyms: CFZ-533 | iscalimab (proposed INN) | NVP-CFZ533 | OM11-62MF
Immunopharmacology Ligand
Compound class: Antibody
Comment: CFZ533 is an anti-CD40 monoclonal antibody that is designed exhibit no agonist activity and is non-depleting (no ADCC activity for an improved safety profile, particularly in non-oncologic indications). It is claimed in Novartis' patent WO2012065950 [1] as mAb1 (based on peptide sequence alignments between the INN record for iscalimab and patented sequences retrieved from a BLAST search). Blocking CD40-mediated inflammatory responses is a well advanced mechanism being expoited for potential to treat autoimmune and inflammatory disorders and/or for preventing/reducing graft rejection following organ transplant.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
Bioactivity Comments
CFZ533 (mAb1) shows no agonist activity in an in vitro assay using isolated human PBMCs, blocks CD40 ligand-mediated PBMC proliferation (IC50 58 ng/ml), inhibits CD40L-mediated TNF-α release from human monocyte derived dendritic cells (IC50 40 ng/ml), and has ADCC activity of < 1% (measuring specific lysis) [1].
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
CD40 Primary target of this compound Hs Antibody Binding 9.2 pKd - 1
⤷ pKd 9.2 (Kd 6.9x10-10 M) [1]
Description: Measured using a Biacore assay.