Bioorganic & Medicinal Chemistry Letters 2010-12-15

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

Yun W Alelyunas, James R Empfield, Dennis McCarthy, Russell C Spreen, Khanh Bui, Luciana Pelosi-Kilby, Cindy Shen

Index: Bioorg. Med. Chem. Lett. 20 , 7312-6, (2010)

Full Text: HTML

Abstract

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.Copyright © 2010 Elsevier Ltd. All rights reserved.

Related Compounds

Related Articles:

Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.

2011-01-15

[Bioorg. Med. Chem. Lett. 21 , 710-4, (2011)]

Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.

2010-01-01

[Chem. Res. Toxicol. 23 , 171-83, (2010)]

The Japanese toxicogenomics project: application of toxicogenomics.

2010-02-01

[Mol. Nutr. Food. Res. 54 , 218-27, (2010)]

Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).

2005-05-05

[J. Med. Chem. 48 , 3269-79, (2005)]

Chemical genetics reveals a complex functional ground state of neural stem cells.

2007-05-01

[Nat. Chem. Biol. 3(5) , 268-273, (2007)]

More Articles...