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Services | Express Screen

Express ScreenThere 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 an Express Screen, we will interrogate your compound against a series of key 50 enzymes that provide a representative sampling of the human kinome.

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

16th January 2018

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.

Amount:

  • Dry: Must be soluble in Dimethyl Sulfoxide (DMSO)
  • Wet:  
  • A minimum of 0.15 ml of each compound in 100% DMSO
  • Concentration: 51 times the concentration at which the screen is to be carried out

Number of Compounds:

  • If there are more than 30 compounds please contact the ICKP for additional details regarding submission 

Kinase Panel

Kinase Full Name Accession Species ATPGroup
AMPKA1 [11 – 559] + AMPKB2 [1 – 272] + AMPKG1 [1 - 331] § AMP-activated protein kinase NM_006251.5, NM_005399.3, BC000358.2 Human 20
Aurora B [1-344] Aurora B NM_004217 Human 20
BTK [2-659] Bruton agammaglobulinemia Tyrosine Kinase NP_00052.1 Human 50
CaMK1a [2-369] Calmodulin dependent kinase 1 NM_003656 Human 50
CAMKK2 [1-541] Calmodulin dependent kinase kinase ß NM_153499 Human 20
CHK2 [5-543] Checkpoint kinase-2 NM_007194 Human 20
CK1δ [1-415] casein kinase-1 NM_001893 Human 20
CK2α1 [2-391] casein kinase-2α NM_001895 Human 5
DYRK1a [1-502] Dual specificity tyrosine phosphorylation Regulated Kinase 1A NM_130437.2 Human 50
EF2K [2-725] Elongation factor kinase AAH32665 Human 5
EPH A2 [591-976] Ephrin receptor A2 NM_004431 Human 50
GSK3ß [2-420] glycogen synthase kinase-3-beta L33801 Human 5
HER4 [706-991] V-erb a erythroblastic leukemia viral oncogene homolog 1 NM_005235 Human 5
HIPK2 [165-564] Homeodomain-interacting protein kinase 2 AF326592 Human 5
IGF1R [954-1367] Insulin-like Growth Factor 1 Receptor NM_000875 Human 5
IRAK4 [14 -460] Interleukin-1 Receptor-Associated Kinase 4 BC013316.1 Human 20
JAK3 [781 - 1124] Janus Kinase 3 NP_000206.2 Human 20
JNK1 [1-384] c-Jun N-terminal kinase L26318 Human 20
Lck [2-509] lymphocyte kinase L48845 Mouse 50
LKB1 [1-433], MO25 [1–341], STRAD [1–431] Ser/Thr Kinase 11 NP_000446 Human 20
MAPKAP-K1a/RSK1/p90RSK [1-735] MAPK-activated protein kinase-1a NM_002953.3 Human 50
MARK3 [2-729] Microtubile affinity regulating kinase (C-TAK1) U64205 Human 5
MKK1/MEK1/MAP2K1 [2-393] MAPK kinase L05624 Human 5
MLK3 [96-386] Mixed Lineage Kinase 3 NM_002419 Human 20
MSK1 [2-802] mitogen and stress-activated protein kinase-1 AF074393 Human 20
MST2 [2-491] Mammalian sterile 20-like 2 (KRS1 or Ser/Thr protein kinase 3) U60206 Human 20
NEK6 [8-313] NIMA related Protein Kinase 6 XM_044814 Human 50
p38α MAPK [1-360] stress-activated protein kinase-2α L35264 Human 50
PAK4 [2-591] p21 activated kinase 4 O96013 Human 5
PDK1 [52-556] 3-phosphoinositide-dependent protein kinase-1 AF017995 Human 20
PIM1 [2-313] provirus integration site for Moloney murine leukaemia virus NM_002648 Human 20
PKAα [2-351] cyclic AMP-dependent protein kinase P17612 Human 20
PKBα (S473D) [118-480] protein kinase B M63167 Human 5
PKCα [1-672] protein kinase C alpha NM_002737 Human 20
PKD1 [2-912] Protein kinase D 1 NM_002742 Human 50
PLK1 [1-603] Polo like kinase 1 (Ser/Thr protein kinase 13) NM_005030 Human 5
PRK2 [501-984] PKC like Kinase 2 S75548 Human 5
RIPK2 [2-311] Receptor interacting protein kinase 2 NM_003821 Human 20
ROCK2 [2-543] Rho-dependent protein kinase U38481 Rat 20
S6K1/p70S6K (T412E) [1-421] p70 ribosomal protein S6 kinase NP_003152 Human 20
SGK1 (S422D) [60-431] serum and glucocorticoid-induced kinase NM_005627 Human 20
smMLCK [475-838] Smooth muscle Myosin Light Chain Kinase NM_005965 Human 50
Src [1-536] sarcoma kinase NM_005417.3 Human 50
SRPK1 [2-654] Serine Arginine Protein Kinase NM_003137 Human 50
SYK [1-635] Spleen Tyrosine Kinase AAH01645.1 Human 20
TAK1 [1 – 303] / TAB1 [437 – 504] Fusion Transforming growth factor beta activated kinase 1 (MAP3K7) NM_003188 (TAK1) and NM_006116 (TAB1) Human 5
TBK1 [1-729] TANK Binding Kinase 1 NM_013254 Human 50
TrkA [441 – 760] Neurotrophic tyrosine kinase, receptor, type 1 NM_001007792.1 Human 20
TTK [1-857] Phosphotyrosine picked threonine kinase NM_003318 Human 20
VEGFR1/FLT1 [784-1338] Vascular Endothelial Growth Factor Receptor 1 NM_002019.3 Human 20

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
  • Data is provided 1 week 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.