WEE1 G2 checkpoint kinase | WEE family | IUPHAR/BPS Guide to PHARMACOLOGY

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WEE1 G2 checkpoint kinase

Target not currently curated in GtoImmuPdb

Target id: 2278

Nomenclature: WEE1 G2 checkpoint kinase

Abbreviated Name: Wee1

Family: WEE family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 646 11p15.3-p15.1 WEE1 WEE1 G2 checkpoint kinase
Mouse - 646 7 F1 Wee1 WEE 1 homolog 1 (S. pombe)
Rat - 646 1 q33 Wee1 WEE1 G2 checkpoint kinase
Previous and Unofficial Names
WEE1 tyrosine kinase | Wee1A | WEE1 homolog (S. pombe) | wee 1 homolog (S. pombe)
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structure of human Wee1A kinase: kinase domain complexed with inhibitor PD0407824.
PDB Id:  1X8B
Resolution:  1.81Å
Species:  Human
References:  4
Enzyme Reaction
EC Number: 2.7.10.2

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
adavosertib Hs Inhibition 8.3 pIC50 2
pIC50 8.3 (IC50 5.18x10-9 M) [2]
PD166285 Hs Inhibition 7.6 pIC50 5
pIC50 7.6 (IC50 2.4x10-8 M) [5]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 3,6

Key to terms and symbols Click column headers to sort
Target used in screen: WEE1
Ligand Sp. Type Action Value Parameter
PD-173955 Hs Inhibitor Inhibition 7.2 pKd
fedratinib Hs Inhibitor Inhibition 6.4 pKd
bosutinib Hs Inhibitor Inhibition 6.3 pKd
tamatinib Hs Inhibitor Inhibition 6.1 pKd
sunitinib Hs Inhibitor Inhibition 6.0 pKd
dovitinib Hs Inhibitor Inhibition 5.9 pKd
lestaurtinib Hs Inhibitor Inhibition 5.9 pKd
staurosporine Hs Inhibitor Inhibition 5.8 pKd
KW-2449 Hs Inhibitor Inhibition 5.6 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: ...1

Key to terms and symbols Click column headers to sort
Target used in screen: nd/WEE1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
SB 218078 Hs Inhibitor Inhibition 16.9
bosutinib Hs Inhibitor Inhibition 40.5
JAK3 inhibitor VI Hs Inhibitor Inhibition 69.4
aminopurvalanol A Hs Inhibitor Inhibition 70.8
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 70.9
MEK inhibitor I Hs Inhibitor Inhibition 70.9
K-252a Hs Inhibitor Inhibition 72.9
staurosporine Hs Inhibitor Inhibition 73.1
MEK1/2 inhibitor Hs Inhibitor Inhibition 73.8
Tpl2 kinase inhibitor Hs Inhibitor Inhibition 74.3
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. AstraZeneca. AZD1775. Accessed on 11/09/2014. Modified on 11/09/2014. astrazeneca.com, http://openinnovation.astrazeneca.com/what-we-offer/compound/867-2/

3. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

4. Squire CJ, Dickson JM, Ivanovic I, Baker EN. (2005) Structure and inhibition of the human cell cycle checkpoint kinase, Wee1A kinase: an atypical tyrosine kinase with a key role in CDK1 regulation. Structure, 13 (4): 541-50. [PMID:15837193]

5. Wang Y, Li J, Booher RN, Kraker A, Lawrence T, Leopold WR, Sun Y. (2001) Radiosensitization of p53 mutant cells by PD0166285, a novel G(2) checkpoint abrogator. Cancer Res., 61 (22): 8211-7. [PMID:11719452]

6. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

WEE family: WEE1 G2 checkpoint kinase. Last modified on 19/02/2015. Accessed on 22/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2278.