Functional ion channel assays

Automated drug screening on HEK cells

ChanPharm offers a large collection of functional ion channel assays for selectivity profiling. Our functional assays utilize automated electrophysiology platforms and manual patch clamp. According to our clients’ needs, the respective portfolio of ion channels can be adapted either to a certain therapeutic area or to a certain risk assessment.

The company possesses a wide range of mammalian cell lines expressing voltage- and ligand-gated ion channels such as GABAA receptors and others. ChanPharm’s portfolio includes sodium, calcium, potassium channels and ligand-gated channels.

Automated drug screening on HEK cells

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Screening and lead optimization

Our ion channel screening platforms enable the discovery of small molecules (or natural products) in compound libraries and the optimization of client’s lead structures within short time.

The screening platform is complimented by ion channel profiling services using standard or custom-designed assay protocols. Our service enables accurate ranking of potent ion channel modulators.

Automated drug screening on Xenopus oocytes.

 

Optimization of your assay protocols

Pulse protocols that are utilized during a certain screening assay matter. The length of a test pulse leading to activation (opening) and inactivation (channel closure during maintained depolarization) can have major effects on apparent affinities and thus influence the outcome of a screening study.

Serum shift assay on ion channels

Prediction of in vivo effects from in vitro  ion channel inhibition may be distorted for drugs strongly binding to plasma proteins. The complication arises from the fact that only the free (unbound) drug is able to block an ion channel. Hence, unlike in the in vivo condition where drugs are present in both free and protein-bound forms ion channel assays are commonly performed in the absence of serum protein.

ChanPharm therefore executes patch clamp evaluation of drug potencies in the absence and in the presence of human serum.

Accounting for state-dependent drug action

Our team will discuss and optimize these assay parameters with you. This ensures maximal sensitivity and relates the settings to an in vivo like situation. Our flexible service allows you to screen against the complete panel of ion channels relevant for a certain diseases or, alternatively, against a selected set of targets that matter to you.