Compound class:
Synthetic organic
Comment: Compound 6j is a preclinical, orally available and selective inhibitor of discoidin domain receptor 1 (DDR1) [5]. The compound has a favourable pharmacokinetic profile.
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 |
In a kinase screening panel, 6j exhibited binding affinity values (Kd) of 18, 22, and 100nM for the TRKC, TRKB and TRKA enzymes repectively [5]. These were the highest affinity values detected apart from DDR1. |
Selectivity at catalytic receptors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
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