Services | Custom Screening

There are over 500 kinases that have been identified in the human kinome comprising 518 protein kinases, and approximately 20 lipid kinases (Manning, et al. 2002. Science 298(5600):1912-34). 

At the International Centre for Kinase Profiling (ICKP) we understand that ascertaining how your compound behaves in relation to the multitude of related enzymes is critical. 

With a Custom Screen, we will interrogate your compound(s) against your choice of kinase proteins available from our Premier Kinase Panel – you choose!  These may be related family members with high homology or a very select group of disparate kinases that are meaningful to your research.   Additionally, we are happy to provide guidance regarding optimal panel selection that fits your requirements.  With this flexibility, we hope that the IKCP can provide you with more tailored service to suit your needs, thereby accelerating your research.

To be included in the next screen your compounds must arrive at the facility by:

6th November 2017

Submission Guidelines

Download: Compound Submission Form

All customers: Please provide a completed Compound Submission Form.

  • Academic customers are required to read the Terms & Conditions and indicate their agreement on the Compound Submission Form.
  • For-Profit customers are required to complete and return the Overarching Service Agreement before work can commence.

Compounds

  • Dry: Must be soluble in Dimethyl Sulfoxide (DMSO)
  • Volume: This will vary depending upon your screen
    • Concentration: 51 times the concentration at which the screen is to be carried out

Please contact us so that we may help you to design a screen that will be most informative to your research needs

Workflow

The principal method utilized is a radioactive filter binding assay using 33P ATP (Hastie, et al 2006. Nat Protoc. 2006;1(2):968-71; Bain, et al 2007. Biochem J. 2007 Dec 15;408(3):297-315).  This method is sensitive, accurate and provides a direct measure of activity.

Assay step-by-step process:

1. Upon receipt of your small molecule, staff at the ICKP will dilute each to the appropriate concentration (if required)

2. This compound is added to a ‘mother plate’ consisting of customer samples, controls and blanks

  • These serve as the source for ‘daughter plates’ which are stored at -20* until assay initiation
  • Note: All compounds are screened in duplicate

3. Next there will be  3 additions to the assay:

  • Enzyme-substrate mixture
  • Incubation Time: 5 minutes at Room Temperature (RT)
  • 33P ATP - Assay begins with this addition
  • Incubation time varies based upon optimal designatedincubation time(for each enzyme @ RT
  • Orthophosphoric acid - Assay is halted with this addition

4. Assay components are harvested onto P81 filter plate

5. Filter plates are air-dried

6. Scintillation fluid is added to plates

7. Counts are read on a Topcount NXT

Data Analysis:

1. Bar codes assigned to each file ensure that data corresponding to the correct compound is being analysed

2. After completion of each assay, ICKP staff ensure that the run has passed standard quality control measures by examining reference compounds on the QC plate

3. Upon determination that the run has met QC standards, a Z-Prime (Z’) value is calculated utilizing data from the controls/blanks on each individual plate

  • This QC measure is in place to ensure that each individual plate in the run has passed QC

4. Finally, a mean percentage activity is calculated for for each customer.

  • A standard deviation for all the duplicates is also calculated

 

Each customer receives mean percentage activity and standard deviation for

each compound tested against all enzymes

Timeline

  • This  screen is undertaken once every 6 weeks.
  • Screening data is provided 2 weeks from the screen start date.
  • Follow-up studies based on results of initial screen can be provided within a few working days from receipt of request.
  • Start dates for each screen can be found here.

Pricing

  • We work with BOTH academia and industry
  • We offer competitive rates.
  • There will be discounts for larger projects (>40 compounds within the same screen)
  • Please contact us to discuss your requirements

Shipping to the UK

In order to minimize customs delays we encourage all customers to provide a sufficient amount of information on each package including:

  • Compound Name(s)
  • Derivation Source (synthetic, natural)
  • Intended Use (e.g. Research)

Shipping Address:

International Centre for Kinase Profiling Division of Signal Transduction Therapy
College of Life Sciences
University of Dundee
Dow Street
Dundee DD1 5EH
United Kingdom
Phone: +44-(0)1382-388-056

Do you need any help? Please get in touch and we’ll be happy to lend a hand.