crotedumab   Click here for help

GtoPdb Ligand ID: 9614

Synonyms: REGN-1193 | REGN1193
Compound class: Antibody
Comment: Crotedumab (REGN1193) is a fully human IgG4 monoclonal antibody that functionally antagonises activity of the glucagon receptor (GCGR) in vitro [1]. REGN1193 was investigated as a potential therapy for type 2 diabetes mellitus.
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.
This mAb is no longer included in Regeneron's development pipeline (access their pipeline webpage here).
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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
REGN1193 cross-reacts with mouse, rat, monkey, and human GCGRs, which facilitates effective preclinical assessment of efficacy and safety [1]. REGN1193 inhibits glucagon-induced hGCGR signalling (cAMP) with an IC50 of 0.65 nM in a cell-based luciferase reporter system [1]. The antibody reduces blood glucose levels in diabetic ob/ob mice.
Selectivity at GPCRs
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
glucagon receptor Rn Antibody Antagonist 10.8 pKd - 1
⤷ pKd 10.8 (Kd 1.5x10-11 M) [1]
glucagon receptor Mm Antibody Antagonist 10.1 – 10.5 pKd - 1
⤷ pKd 10.1 – 10.5 (Kd 8.99x10-11 – 3.05x10-11 M) [1]
glucagon receptor Monkey Antibody Antagonist 9.4 – 10.5 pKd - 1
⤷ pKd 9.4 – 10.5 (Kd 3.86x10-10 – 3.03x10-11 M) [1]
glucagon receptor Primary target of this compound Hs Antibody Antagonist 9.8 – 10.0 pKd - 1
⤷ pKd 9.8 – 10.0 (Kd 1.62x10-10 – 1.09x10-10 M) [1]