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.
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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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