- Advanced search
- Immuno Portal
- Malaria Portal
Compound class: Synthetic organic
Comment: DDR-IN-1 is a potent and selective discoidin domain receptor tyrosine kinase 1 (DDR1) inhibitor . DDR1-IN-1 binds to DDR1 in the 'DFG-out' conformation and inhibits DDR1 autophosphorylation. It was a preclinical lead compound.
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.✖
|In cells, DDR1-IN-1 inhibits basal DDR1 autophosphorylation with an EC50 of 86nM, but does not have a significant antiproliferative effect on DDR1 deregulated cancer cell lines below 10μM .
KinomeScan assessment revealed DDR1-IN-1 binding to ABL, KIT, and PDGFRβ, but this did not translate to enzyme inhibition.
|Selectivity at catalytic receptors|
|Key to terms and symbols||Click column headers to sort|