What are you offering?

CELLinib96: We offer a representative screening service on 96 protein kinases spread across the kinome as a 1-shot assay at your desired compound concentration to help you make your drug discovery project faster by considering off-target effects in the kinome!

CELLinibEC50: We offer to determine your EC50 as a 10-point dose-response on over 350+ kinases and mutants as well as for BRDs, HDACs and E3s to accurately determine your target engagement in living cells!

CELLKinib: We offer a half-life determination using a previously determined 10xEC50 as a parameter for a wash-out experiment to help with your decisions based on binding kinetics!

Why should I choose you?

We set up the comprehensive screen as a requirement for the characterization of chemical probes for the SGC Frankfurt – lead by the two most respected experts in the field of protein kinase inhibitor development (Prof. Dr. Stefan Knapp) and chemical probe quality (Dr. Susanne Müller-Knapp). We have been perfoming these screens for ~5 years. Feel free to have a look at the projects we have contributed to in that time.

What are your requirements for a test compound?

Please have a look at our requirements for each service. Typically we need a 100 µL stock at 1000x your desired concentration in 100% DMSO for the 1-shot assay or a 10 mM stock for EC50 determination and half-life assessment. Please be aware that we will test your sample as it comes – and cannot guarantee a usable profile or curve if your compound excites or emits light at our wavelength (450 nm and 610 nm, respectively) or is unsoluble or cytotoxic.

How does the ordering work?

Please have a look on how to get a quote here and if you have any questions, please contact us. The normal process would be to get in contact with us to find out what you need. After that we will set up a project plan to fullfill your NanoBRET needs.

What is the typical turnaround time?

CELLinib96: We will have quarterly screens. Once we start the screen, a typical turnaround time is 4 weeks.

CELLinibEC50: Once you provide us with your sample a typical turnaround time is 2 weeks.

CELLkinib: Once you provided us with your sample a typical turnaround time is 2 weeks.

What does the data look like from the 1-shot profiling?

You will get an Excel-file with the data for both technical replicates and an average and SD calculated. In the file there will also be a kinome tree representation. Please have a look at the service and/or download example data here.

How can I access my compound data and profiles?

We will send you generated data and profiles via the Email you provide us upon ordering.

Do you need to know what my compound looks like?

We don’t require your compounds structural information. You do not need to disclose any information about your compound to us. However, please make sure your compounds meets our sample requirements! Also, please be aware that we will test your sample as it comes – and cannot guarantee a usable profile or curve if your compound excites or emits light at our wavelength (450 nm and 610 nm, respectively) or is unsoluble or cytotoxic.

Do you handle my compound profile confidently?

We do want to use exciting profiles for marketing purposes – however, we will not include any client or name or number associated with your compound profile.

Are you saving my compound profile?

Yes, we intend to save your compound profile in our database – you will always have access to it or we can resend it to you.

Are you storing my sample?

Yes, we will store your sample for up to 6 months – after that the compounds quality cannot be guaranteed anymore and we will dispose of your sample.

Do you offer any discounts?

Please contact us for any info regarding pricing or discounts or get a quote and join our newsletter to stay updated!

How does NanoBRET work?

NanoBRET is a technique developed by Promega. It is a tracer competition assay in living cells – using transiently expressed full-length target proteins – where your molecule will compete with the tracer in a dose-dependant manner.

Can you also determine the affinity for allosteric binders?

Yes, we could for example determine an EC₅₀ for GNF-5 with ABL1.

In theory, an allosteric binder should change the active site in a way, that the normal catalytic activity gets inhibited – and hence will induce changes that we can observe with the tracer signal. However, we often observed a different lower plateau than for competitive binders (here e.g. 25%) which means in a 1-shot displacement assay we would need a different (100% binding) Control using an excess of your inhibitor – which will result in you needing 2 slots if you would like CELLinib96. Please tell us ia advance if you have such a case.