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Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate. | LitMetric

Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.

Bioorg Med Chem Lett

CNS Chemistry and DMPK Department, AstraZeneca Pharmaceuticals LP, Wilmington, DE 19850-5437, USA.

Published: December 2010

We determined the experimental solubility of CNS marketed drugs. Of the 98 drugs measured, greater than 90% had solubility >10 μM in pH 7.4 buffer. Only seven drugs had solubility <10 μM. Using these data, we established a solubility criterion to support CNS discovery. The implication of poor solubility with potential safety concerns and undesirable side effects are discussed.

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Source
http://dx.doi.org/10.1016/j.bmcl.2010.10.068DOI Listing

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