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Compound class: Synthetic organic
Comment: Compound 11 is a potent, selective, and brain penetrant inhibitor of dual leucine zipper kinase (DLK, MAP3K12) . DLK inhibitors are being investigated for neuroprotective potential.
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.✖
1. Patel S, Freedman S, Chapman KL, Emms F, Fletcher AE, Knowles M, Marwood R, Mcallister G, Myers J, Curtis N et al.. (1997)
Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor.
J Pharmacol Exp Ther, 283 (2): 636-47. [PMID:9353380]
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Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).
J Med Chem, 58 (20): 8182-99. [PMID:26431428]