Protein transformations that change lives

Services | Premier Screen

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 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:

11th October 2024

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

Premier Screen Panel

Kinase	Longname	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
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

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:
0.5 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

Timeline

Timelines for Sample Submission

Customers are asked to ensure that their compounds are sent in advance of assay screening dates (see below).
Samples must be received one full working day before the screening starts to ensure that the samples are included in the preferred screen start date.
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.

Title	Deadline for arrival	Data Returned (Premier, Custom)
PK141	11th October 2024	29th October 2024
PK142	22nd November 2024	10th December 2024

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
School of Life Sciences
University of Dundee
Dow Street
Dundee DD1 5EH
United Kingdom
Phone: +44-(0)1382-388-056

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Workflow

Premier Screen Panel

Submission Guidelines

Timeline

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