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Synonyms: compound 4 [PMID: 32251410]
Compound class: Synthetic organic
Comment: DCLK1-IN-1 is reported as a selective inhibitor of the serine/threonine kinases, doublecortin-like kinase 1 and 2 [1-2]. It was discovered using chemoproteomic profiling and structure-based design, and is an in vivo suitable tool for investigating and characterizing the physiological and pathophysiological roles of these kinases, particularly the role of DCLK1 in cancer and type II immunity in the gut (via epithelial tuft cells). DCLK1-IN-1 shares a chemical scaffold with LRRK2-IN-1 (an LRRK2 inhibitor) and XMD8-92 (an ERK5 inhibitor) which both exhibit off-target activity towards DCLK1. These latter tool compounds also inhibit the bromodomains of the oncology target BRD4. DCLK1-IN-1 was designed to reduce off-target effects and increase DCLK1 selectivity.
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.✖