Hit to Lead - PharmaCore Labs (PCL) Co., Ltd




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Hit to Lead

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Hit to Lead

Time2020-04-23 17:02:21 Hits869

•Qualify your hits with biophysical characterization of the mechanism of action.

•Drive SAR to increase potency and reduce off-target and toxic effects.

•Prioritize your hits using in vivo screening tools with medium-throughput.

Cell-based activity screening

Following biochemical screening, cell-based activity testing of compounds accounts for parameters influencing the potency of compounds such as the need to cross the membrane

and physiologic levels of ATP, co-factors, and pH.

Cellular phosphorylation, methylation and deacetylation assays allow compound screening on endogenous enyzmes whereas the NanoBRETTM technology enables investigation of target engagement in the cellular setup.

In additon, cell-based activity assays are available for targeting GPCRs and ion channels for both primary and secondary screening.

Four biophysical platforms are available for characterization of the compound-target interaction on a molecular level

In vivo screening of compounds

The In Vivo Hollow Fiber Model enables an early potency evaluation in the physiological environment of a body with medium throughput.

Up to 14 compounds can be tested in parallel with group sizes of 3 animals on three tumor cell lines simultaneously

Structure – Activity – Relationship

The partnership with our MedChem partners‘ specialists enable our clients to access medicinal chemistry expertise during the various phases of the drug discovery process. Reaction Biology has the means to test improvements of the changes in the chemical structure in regards of potency, functional effects, selectivity, pharmacodynamic/ pharmacokinetic profile, toxicity and bioavailability.

We have worked with our MedChem partners in numerous projects over the course of the last 10 years and can provide seamless interaction to drive fast SAR cycles.


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