Services | Premier Screen

Premier 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 a Premier Screen, we will interrogate your compound against a series of 140 enzymes that facilitates acquisition of a detailed profile of selectivity of your compound in a more in-depth manner.

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

25th September 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.

Amount:

  • Dry: Must be soluble in Dimethyl Sulfoxide (DMSO)
  • Wet:  
  • 0.3 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
ABL [118 - 535] Abelson murine leukemia viral oncogene homolog 1 NM_005157 Human 5
AMPKA1 [11 – 559] + AMPKB2 [1 – 272] + AMPKG1 [1 - 331] § AMP-activated protein kinase NM_006251.5, NM_005399.3, BC000358.2 Human 20
ASK1 [670 - 950] † Apoptosis Signal Regulating Kinase 1 (MAP3K5) NM_005923 Human 50
Aurora A [2-403] Serine / threonine protein kinase 6 BC027464 Human 5
Aurora B [1-344] Aurora B NM_004217 Human 20
BRK [1 - 451] Breast tumour kinase, also know as PTK6 (protein tyrosine kinase 6) NM_005975 Human 20
BRSK1 [2-778] Brain-specific kinase 1 NM_032430 Human 20
BRSK2 [2-674] BR serine/threonine kinase 2 AF533878 Human 50
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
CDK2 [2 – 298] / Cyclin A2 [171 – 432] cyclin-dependent kinase 2-cyclin A complex NM_001798 Human 20
CDK9 [1 – 372] / Cyclin T1 [1 – 726] cyclin-dependent kinase 9 NM_001261 [CDK9] and NM_001240.2 [Cyclin T1] Human 50
CHK1 [1-476] checkpoint kinase-1 AF016582 Human 20
CHK2 [5-543] Checkpoint kinase-2 NM_007194 Human 20
CK1γ2 [1 – 415] casein kinase 1, gamma 2 BC018693.2 Human 20
CK1δ [1-415] casein kinase-1 NM_001893 Human 20
CK2α1 [2-391] casein kinase-2α NM_001895 Human 5
CLK2 [138 - 499] CDC-like Kinase 2 NM_003993.2 Human 5
CSK [1-450] C-terminal Src kinase NM_004383 Human 20
DAPK1 [1 - 363] Death-Associated Protein Kinase 1 NM_004938.2 Human 5
DDR2 [467 - 854] Discoidin domain receptor tyrosine kinase 2 NM_006182 Human 5
DYRK1a [1-502] Dual specificity tyrosine phosphorylation Regulated Kinase 1A NM_130437.2 Human 50
DYRK2 [3-528] Dual specificity tyrosine phosphorylation Regulated Kinase 2 NM_003583 Human 50
DYRK3 [1-588] Dual specificity tyrosine phosphorylation Regulated Kinase 3 AY590695 Human 5
EF2K [2-725] Elongation factor kinase AAH32665 Human 5
eIF2AK3 [536 – 1116] eukaryotic translation initiation factor 2-alpha kinase 3 NM_004836.5 Human 5
EPH A2 [591-976] Ephrin receptor A2 NM_004431 Human 50
EPH A4 [570 - 986] Ephrin receptor A4 NM_004438 Human 50
EPH B1 [565 – 984] Ephrin receptor B1 NM_004441 Human 20
EPH B2 [560 - 987] Ephrin receptor B2 NM_004442 Human 20
EPH B3 [561-998] Ephrin receptor B3 NM_004443 Human 20
EPH B4 [561 - 987] Ephrin receptor B4 NP_004435.3 Human 5
ERK1 [2-379] mitogen-activated protein kinase 1 BC013992 Human 5
ERK2 [2 – 360] mitogen-activated protein kinase X58712 Human 20
ERK5 [1 – 816] mitogen-activated protein kinase 7 (MAPK7) NM_002749 Human 50
ERK8 [2-544] mitogen-activated protein kinase 8 AY065978 Human 5
FGF-R1 [400-820] Fibroblast Growth Receptor 1 M34641 Human 20
GCK [2-812] Germinal Centre Kinase BC047865 Human 20
GCKR Germinal centre kinase NM_006575.4 Human 5
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
HIPK1 [158–555] Homeodomain-interacting protein kinase 1 NM_198268 Human 20
HIPK2 [165-564] Homeodomain-interacting protein kinase 2 AF326592 Human 5
HIPK3 [161-562] Homeodomain-interacting protein kinase 3 NM_005734 Human 20
IGF1R [954-1367] Insulin-like Growth Factor 1 Receptor NM_000875 Human 5
IKKß [1-736] inhibitory κB kinase ß XM_032491 Human 5
IKKε [1-716] inhibitory κB kinase ε NM_014002 Human 50
InsR [1001-1382] Insulin Receptor NM_000208.2 Human 20
IRAK1 [1 - 712] interleukin-1 receptor-associated kinase 1 NM_001569.3 Human 5
IRAK4 [14 -460] Interleukin-1 Receptor-Associated Kinase 4 BC013316.1 Human 20
IRR [944-1236] Insulin Receptor Related Receptor 1 NM_014215 Human 5
JAK3 [781 - 1124] Janus Kinase 3 NP_000206.2 Human 20
JNK1 [1-384] c-Jun N-terminal kinase L26318 Human 20
JNK2 [1-424] c-Jun N-terminal kinase 2 L31951 Human 20
JNK3 [40-422] c-Jun N-terminal kinase 3 NM_002753 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
MAP4K3 [1 – 873] mitogen-activated protein kinase kinase kinase kinase 3 BC071579.1 Human 20
MAPKAP-K1a/RSK1/p90RSK [1-735] MAPK-activated protein kinase-1a NM_002953.3 Human 50
MAPKAP-K1b/RSK2 MAPK-activated protein kinase-1b NM_004586 Human 50
MAPKAP-K2 [46-400] MAPK-activated protein kinase-2 NM_032960 Human 20
MAPKAP-K3 [2-382] MAPK-activated protein kinase 3 NM_004635 Human 20
MARK1 [2 – 795] Microtubule-affinity-regulating kinase 1 AF154845 Human 20
MARK2 [2-691] Microtubule-affinity-regulating kinase 2 NM_004954 Human 20
MARK3 [2-729] Microtubile affinity regulating kinase (C-TAK1) U64205 Human 5
MARK4 [2-752] Microtubule-affinity-regulating kinase 4 AK075272 Human 50
MEKK1 [877 - 1563] mitogen-activated protein kinase kinase kinase 1 (MAP3K1) XM_042066 Human 50
MELK [2-651] maternal embryonic leucine zipper kinase NM_014791 Human 50
MINK1 [1-320] Misshapen-like KInase 1 (MAP4K6) NM_015716 Human 50
MKK1/MEK1/MAP2K1 [2-393] MAPK kinase L05624 Human 5
MKK2/MEK2/MAP2K2 [2 - 400] Mitogen Activated Protein Kinase Kinase 2 (MAP2K2) NM_030662 Human 5
MKK6 [2 - 334] † Mitogen Activated Protein Kinase Kinase 6 (MAP2K6) NM_002758 Human 50
MLK1 [132-413] Mixed Lineage Kinase 1 NM_033141 Human 20
MLK3 [96-386] Mixed Lineage Kinase 3 NM_002419 Human 20
MNK1 [2-424] # MAP kinase interacting Kinase 1 AB000409 Human 50
MNK2α [2-465] # MAP kinase interacting Kinase 2α AF237775 Human 50
MPSK1 [1 - 305] Myristoylated and Palmitoylated serine/threonine protein Kinase,also know as STK16 CR407675 Human 50
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
MST3 [1 - 431] mammalian homologue Ste20-like kinase AAH65378 Human 20
MST4 [1-416] Mammalian sterile 20-like 4 NM_016542.3 Human 20
NEK2A [1-445] NIMA related Protein Kinase 2a NM_002479 Human 50
NEK6 [8-313] NIMA related Protein Kinase 6 XM_044814 Human 50
NUAK1 [2–660] SnF1-like Kinase 1 NM_014840 Human 20
OSR1 T185E [1 – 342] Oxidative Stress Responsive 1 NM_005109.2 Human 5
p38ß MAPK [1-364] stress-activated protein kinase-2ß Y14440 Human 20
p38α MAPK [1-360] stress-activated protein kinase-2α L35264 Human 50
p38γ MAPK [1-367] stress-activated protein kinase-3 Y10487 Human 5
p38δ MAPK [1-365] stress-activated protein kinase-4 Y10488 Human 5
PAK2 T402E [1-524] p21-activated protein kinase 2 NM_002577 Human 20
PAK4 [2-591] p21 activated kinase 4 O96013 Human 5
PAK5 [2-719] (PAK7) p21 activated kinase 5 Q9P286 Human 20
PAK6 [2-681] p21 activated kinase 6 Q9NQU5 Human 20
PDGFRα [551 – 10589] platelet-derived growth factor receptor NM_006206 Human 5
PDK1 [52-556] 3-phosphoinositide-dependent protein kinase-1 AF017995 Human 20
PhKγ1[2-297] phosphorylase B kinase X80590 Human 50
PIM1 [2-313] provirus integration site for Moloney murine leukaemia virus NM_002648 Human 20
PIM2 [2-334] provirus integration site for Moloney murine leukaemia virus U77735 Human 5
PIM3 [2-326] provirus integration site for Moloney murine leukaemia virus Q86V86 Human 20
PINK1 [1 – 570] PTEN induced putative kinase 1 XM_963274 Tribolium castaneum 5
PKAα [2-351] cyclic AMP-dependent protein kinase P17612 Human 20
PKBß (S474D) [120-481] protein kinase B ß NM_001626 Human 50
PKBα (S473D) [118-480] protein kinase B M63167 Human 5
PKCα [1-672] protein kinase C alpha NM_002737 Human 20
PKCγ [1 – 697] protein kinase C gamma NM_002739 Human 20
PKCζ [2-592] protein kinase C zeta NM_002744 Human 5
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
PRAK/MAPKAPK5 [1-471] p38-regulated/activated kinase AF032437 Human 20
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
SIK2 [2 - 926] salt inducible protein kinase 2 NM_015191.1 Human 50
SIK3 [2 - 1369] salt inducible protein kinase 3 Sugen Kinase Database 15721 Human 50
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
STK33 [1 – 514] † Serine / Threonine Kinase 33 BC031231.1 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
TAO kinase 1 [1 – 356] Thousand and One Amino Acid Protein Kinase NM_020791 Human 20
TBK1 [1-729] TANK Binding Kinase 1 NM_013254 Human 50
TESK1 [1 – 345] testis-specific kinase 1 NM_006285.2 Human 50
TGFβR1/ALK5 (T204D) [200 – 501] transforming growth factor, beta receptor 1 NM_004612 Human 20
TIE2 [771 – 1124] Tunica Interna Endothelial cell kinase, also know as TEK BC035514.1 Human 20
TLK1 [1 – 766] tousled-like kinase 1 NM_012290.4 Human 5
TrkA [441 – 760] Neurotrophic tyrosine kinase, receptor, type 1 NM_001007792.1 Human 20
TSSK1 [1 - 367] testis-specific serine kinase 1 AY028964 Human 20
TTBK1 [1 - 1321] tau tubulin kinase 1 NM_032538.1 Human 5
TTBK2 [1 – 450] tau tubulin kinase 2 BC071556 Human 5
TTK [1-857] Phosphotyrosine picked threonine kinase NM_003318 Human 20
ULK1 [2 – 1050] unc-51-like kinase 1 NM_003565 Human 20
ULK2 [1 – 1036] unc-51-like kinase 2 NM_014683 Human 5
VEGFR1/FLT1 [784-1338] Vascular Endothelial Growth Factor Receptor 1 NM_002019.3 Human 20
WNK1 [1 - 661] With No Lysine deficient protein kinase 1 NM_018979.3 Human 20
YES1 [1-543] Yamaguchi sarcoma viral oncogene homolog 1 NM_005433 Human 20
ZAP70 [1 – 619] zeta chain (TCR) associated protein kinase 70 NM_001079 Human 5

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.