Synonyms: compound 1 [PMID: 24794745]
Compound class:
Synthetic organic
Comment: This is a DAG-indololactone class compound that was developed as an activator of RAS guanyl releasing proteins (RasGRP) that can discriminate between RasGRPs and protein kinase C (PKC) isoforms [1].
![]() 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 |
RasGRP activator 1 binds to RasGRP3 with a Ki of 0.33 nM which is equipotent with its binding to RasGRP1 [1]. It is approximately 100-fold selective for the RasGRPs compared to PKCs α and ε. |
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Selectivity at other protein targets | ||||||||||||||||||||||||||||||||||
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