Compound class:
Synthetic organic
Comment: Compound 11 is a potent, selective, and brain penetrant inhibitor of dual leucine zipper kinase (DLK, MAP3K12) [2]. DLK inhibitors are being investigated for neuroprotective potential.
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 |
Compound 11 is active in an in vivo nerve injury model [2]. It inhibits JNK phosphorylation downstream of DLK signalling with an IC50 of 536 nM. Compound 11 was screened for DLK selectivity against a selected panel of 58 kinases. Those with >50% inhibition were CSF1R, Flt3, GSK3β, Kit, Src, TrkA and TrkB (see Figure 6 in [2]), but all calculated IC50 values were in the micromolar range or above. It is selective for DLK over the three JNKs (IC50s 1-5 μM) and over the three related mixed lineage kinases MLK1, MLK2 and MLK3 (IC50s all >10 μM). |
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