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Potent and selective inhibitors of CDPK1 from and based on a 5-aminopyrazole-4-carboxamide scaffold. | LitMetric

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Article Abstract

5-Aminopyrazole-4-carboxamide was used as an alternative scaffold to substitute for the pyrazolopyrimidine of a known "bumped kinase inhibitor" to create selective inhibitors of calcium-dependent protein kinase-1 from both and . Compounds with low nanomolar inhibitory potencies against the target enzymes were obtained. The most selective inhibitors also exhibited submicromolar activities in cell proliferation assays and were shown to be non-toxic to mammalian cells.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3908674PMC
http://dx.doi.org/10.1021/ml400315sDOI Listing

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