isunakinra   Click here for help

GtoPdb Ligand ID: 9704

Synonyms: EBI-005
Immunopharmacology Ligand
Compound class: Peptide
Comment: Isunakinra (EBI-005) is a fusion protein containing domains from IL-1β and IL-1 receptor antagonist (IL-1Ra or anakinra) [3]. It potently blocks IL-1R1 signalling, with higher affinity than anakinra. It was developed as a topical therapy for inflammatory diseases of the ocular surface.
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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 affinity value presented below is calculated from the published affinity of anakinra for the IL1R1 [1], and the statement that 'EBI-005 has 500 times higher affinity than anakinra' in Kovalchin et al. (2017) [3].
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
Interleukin-1 receptor, type I Primary target of this compound Hs Inhibitor Inhibition 10.5 pKd - 3
⤷ pKd 10.5 (Kd 3x10-11 M) [3]