evolocumab   Click here for help

GtoPdb Ligand ID: 7343

Synonyms: AMG-145 | AMG145 | Repatha®
Approved drug
evolocumab is an approved drug (EMA & FDA (2015))
Compound class: Antibody
Comment: Evolocumab is a clinically approved anti-PCSK9 (proprotein convertase subtilisin/kexin type 9) monoclonal antibody. Peptide sequences for this antibody are available from its IMGT/mAb-DB link. The development and discovery of this antibody is described in patent US8030457, where SEQ IDs 23 and 49 comprising clone 21B12 light and heavy chain variable regions respectively, match the peptide sequences in the INN record for evolocumab.
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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
Pending publication, affinity data for evolocumab is derived from patent US8030457.
Selectivity at enzymes
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
proprotein convertase subtilisin/kexin type 9 Primary target of this compound Hs Antibody Binding 9.7 pKd - 3
⤷ pKd 9.7 (Kd 1.9x10-10 M) [3]
Description: Dissociation equilibrium constant for wild-type hPCSK9, measured using proprietary BIACore® technology.
Ligand mentioned in the following text fields
S8: Subtilisin overview