Compound class:
Synthetic organic
Comment: JR14a is reported as an antagonist of the Complement C3a receptor (C3aR) [1]. It is orally active, and elicits anti-inflammatory effects in vitro and in vivo. It is a more potent antagonist than SB290157.
![]() 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. ✖ |
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Bioactivity Comments |
JR14a exhibits selectivity for human C3aR compared to C5aR [1]. It is a potent inhibitor of C3a-induced mast cell degranulation in vitro (IC50 8 nM for inhibition of β-hexosaminidase release from LAD2 human mast cells). |
Selectivity at GPCRs | ||||||||||||||||||||||||||||||||||
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