UORSY DCLK1 modulators

DCLK1 kinase is a homologue of DCX kinase, a microtubule-associated protein, crucial for neuronal migration and developing of nervous system. The N terminus of DCLK1 encodes a MT-binding domain with high homology to DCX, the C terminus of DCLK1 is unique and encodes a domain similar to Ca2+/calmodulin-dependent kinases (CaMKs).1 DCLK is a PSD component and plays role in synaptic functions. Understanding its’ importance, we have created a library of DCLK1 modulators.

All in-stock compounds, possessing activity towards DCLK1 was chosen basing on the similarity approach and then clusterized. 4 clusters were obtained and a pharmacophore model for each cluster was built.2,3 Additionally, exclusion of pharmacophore’s volume due to bound ligand was performed.  As a result, we obtained library, which contains 2286 compounds.

     

Physicochemical profiles of UORSY DCLK1 modulators:

300<MW<500; 2<HbA<9; 0<HbD<3; 0<logP<6; RotBonds≤8; TPSA<145.

UORSY DCLK1 modulators are available as powders, dry films or DMSO solutions. All compounds have a minimum purity of 90% assessed by 1H NMR; analytical data is provided.

For more information, please contact us at screenlibs@uorsy.com

1Shin, E. et. al, Nat. Commun. 2013, 4, 1440.
2Lindvall, M. et. al, ACS Med. Chem. Lett. 2011, 2, 720–723.
3Zheng, Y. et. al, Bioorg. Med. Chem. Lett. 2013, 23, 3523–3530.

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