Biology and Screening
The value of compounds is in their biological properties – and knowing them. Our biology and screening group enables us to rapidly generate those data that are essential and critical to advance your project. We can develop and execute both cellular and cell-free screens to client targets using most common readouts. Some of the screens developed by our group have been transferred to clients’ laboratories to screen the clients compound library. A particular strength of the group are functional assays for inhibitors of peptidyl-prolyl cis/trans isomerases such as FK506 binding proteins, cyclophilins, and similar proteins (PPIases).
Assay Development and Screening
The biology group at Selcia Discovery supports ongoing medicinal chemistry projects. In addition, the group provides an extensive range of assay development and screening services tailored to customer requirements.
- Binding assay
- Enzyme inhibition assays, including kinetic assays for PPIase inhibition
- Reporter gene assays
- Cell-based functional assays
- Membrane protein arrays
- As well as running a client’s existing assay protocol, we can develop, optimise and apply novel methodologies, tailored to our client’s needs
- Available assay readouts: UV/visual absorbance, fluorescence (fluorescence intensity, fluorescence polarisation, TR-FRET) and luminescence
Our chemists have proven success in developing our own fluorophores to fine-tune tool-ligand affinities for optimising our fluorescence-based assays.
ADME/PK capabilities
Acting primarily as a support for medicinal chemistry, we provide a comprehensive range of ADME, PK and bioanalytical services generating robust and reliable data. High quality drug candidates are not possible without high quality data. Whilst all in vitro assays are performed in the Selcia laboratories, in vivo studies are carried out by trusted partner companies upon whose quality and delivery we can rely.
Selcia is currently expanding its capabilities by developing an assay that detects a compounds potential to form chemically reactive metabolites. The bio-activation of a drug is one key factor responsible for idiosyncratic toxicity. This type of toxicity is commonly only recognised after the launch of a drug with usually enormous financial consequences. Early recognition of this potential liability in drug discovery can reduce the risk of developing candidates causing idiosyncratic drug reactions.
- Physiochemical properties (Log D, Solubility, chemical stability)
- Metabolic stability (in microsomes and plasma)
- Distribution studies (plasma protein binding and PAMPA)
- Cytochrome P450 inhibition (drug-drug Interactions, e.g. CYP3A4)
- Metabolite Identification
- In vivo pharmacokinetics
Please do not hesitate to get in touch for more information about our services.