abatacept   Click here for help

GtoPdb Ligand ID: 6891

Synonyms: BMS-188667 | CTLA4-IgG4m | Orencia® | RG-1046 | RG-2077
Approved drug Immunopharmacology Ligand
abatacept is an approved drug (FDA (2005), EMA (2005))
Compound class: Peptide or derivative
Comment: Abatacept is a recombinant protein fusing the extracellular domain of human cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4) to the modified Fc (hinge, CH2, and CH3 domains) portion of human immunoglobulin G1 (IgG1) [3]. In essence, abatacept is a CTLA-4 mimetic, that enhances CTLA-4's inhibitory signal to T cells, thereby down-modulating T cell mediated inflammation.
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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

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View more information in the IUPHAR Pharmacology Education Project: abatacept

Bioactivity Comments
In a cell based CD80/86 inhibition assay abatacept inhibits IL-2 release with an IC50 of 22.6 nM [2].
Selectivity at other protein targets
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
CD80 Primary target of this compound Hs Fusion protein Inhibition ~7.9 pKd - 3,5
⤷ pKd ~7.9 (Kd ~1.2x10-8 M) [3,5]
Description: Measuring binding of 125I-labeled B7Ig fusion protein to immobilized abatacept.
CD86 Primary target of this compound Hs Fusion protein Inhibition ~7.9 pKd - 3,5
⤷ pKd ~7.9 (Kd ~1.2x10-8 M) [3,5]
Description: Measuring binding of 125I-labeled B7Ig fusion protein to immobilized abatacept.