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Note: this service is for Research Use Only and Not intended for clinical use.
Discovering a new drug is a lengthy and often unsuccessful process. Compound screening aims at discovering specific compounds that could be promising candidates for pharmaceutical development, and screening a chemical library for compounds that could be useful in drug development. Compound screening is also conducted to identify the potential side effects caused by administration of such compounds. Compound screening makes the drug development easier and has its place in pharmaceutical research.
The study of compound screening involves in many aspects, including enantiomorphic composition, partition coefficients at selected pH, estimated dissociation constant. With extensive and significant experience in high quality screening assays, Alfa Chemistry has been involved in compound screening projects for a diversity of drugs. Our advanced techniques will help to find new uses for existing drugs and other compounds present in pharmaceutical libraries and speed up drug development without the burden of increased staff and equipment.
The pharmaceuticals obtained by chemically synthesis are often enantiomorphic. Enantiomers occupy a large proportion of drugs. The biological effects of a pair of enantiomers on humans or animals are quite different. There are pharmacokinetic differences between a pair of enantiomers, including absorption, transport and metabolism, which eventually lead to different therapeutic effects, side effects and toxic reactions. The data related enantiomorphic composition have important significance for the development of chiral drug. A nuclear magnetic resonance (NMR) method is available for the determination of the enantiomorphic compisition.
The partition coefficient, pH dependent, is very useful physicochemical parameters. The octanol/water partition coefficients (log P) and/or the octanol/buffer partition coefficient at a selected pH (log D) are key indicators of lipophilicity of a compound. Lipophilicity is a major structural factor governing both pharmaceutical kinetics and dynamics. Modern screening technology trends to more lipophilic molecules. High lipophilicity means poor aqueous solubility, which makes the development of a seemingly promising drug candidate very difficult. We apply a high-throughput microplate assay for the determination of partition coefficients, providing important lipophilicity information at the early discovery stage to help design new molecules.
As the majority of drugs are weak acids and bases, the dissociation constant (pKa) of a drug is a key physicochemical parameter, which influences lipophilicity, solubility, protein binding and permeability that in turn directly affects pharmacokinetic characteristics. Considering the importance of this parameter pKa to the drug development, estimating or measuring the pKa will be of great benefit. Nuclear magnetic resonance (NMR) spectroscopy has evolved as an important tool for drug discovery. Our experience demonstrate that NMR is an effective technique to be used as primary drug screening and estimating their dissociation constants.
Alfa Chemistry is a reliable provider of compound screening services in the areas of pre-clinical drug development programs. If you are looking for screening of compound, please contact us.
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