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patritumab deruxtecan   Click here for help

GtoPdb Ligand ID: 14121

Synonyms: HER3-DXd | MK-1022 | U3-1402
Immunopharmacology Ligand
Compound class: Antibody
Comment: Patritumab deruxtecan (MK-1022; HER3-DXd) is an anti-Erb-B2 receptor tyrosine kinase 3 (ERBB3; HER3) antibody-drug conjugate. The conjugate is a camptothecin derivative that inhibits topoisomerase I activity to kill tumour cells [5]. HER3 is a key dimerisation partner for HER receptors. Antibody binding induces rapid receptor internalisation and inhibits HER signalling.
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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
The parental mAb patritumab is cross-reactive with human, cynomolgus, rat and mouse HER3 [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
erb-b2 receptor tyrosine kinase 3 Hs Antibody Binding 8.5 – 9.0 pKd - 1
⤷ pKd 8.5 – 9.0 (Kd 3x10-9 – 1x10-9 M) [1]
Description: Binding affinity of unconjugated mAb U3-1287 (AMG888) for HER3