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Compound class:
Antibody
Comment: CR3022 is a monoclonal antibody that binds Spike protein (S) of SARS-CoV and SARS-CoV-2 [2-3,5]. It was developed from a single chain Fv phage display library derived from lymphocytes from the convalescent plasma of a SARS-CoV patient, and reconstructed into IgG1 format [2]. CR3022 does not compete for binding with antibodies that bind to the ACE2 RBD of S, and acts allosterically to reduce binding to ACE2 [1]. Cryo-EM analysis shows that CR3022 Fab disrupts S conformation, so as to promote conversion to the fusion-incompetent post-fusion state, thus incapacitating the virus's ACE2-dependent infection mechanism [1]. Elucidating the protein-protein interactions that determine SARS-CoV-2/ACE2 binding and viral infection will help to identify ways in which this crucial interaction might the targeted for therapeutic development [4].
Ligand Activity Visualisation ChartsThese 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. ✖ |
| Bioactivity Comments |
| CR3022 binds SARS-CoV spike protein with reported Kd values between <0.1-19 nM [1,5]. Variation in binding affinity values is the result of different assay formats, and whether they use full CR3022 IgG or CR3022 Fab. Tighter binding to SARS-CoV is proposed to be due to the presence of a glycan in its epitope that is not present in SARS-CoV-2. |
| Selectivity at other protein targets | ||||||||||||||||||||||||||||||||||
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