protein kinase, membrane associated tyrosine/threonine 1 | WEE family | IUPHAR/BPS Guide to PHARMACOLOGY

protein kinase, membrane associated tyrosine/threonine 1

Target id: 2167

Nomenclature: protein kinase, membrane associated tyrosine/threonine 1

Abbreviated Name: Myt1

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

   GtoImmuPdb view: OFF :     Currently no data for protein kinase, membrane associated tyrosine/threonine 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 499 16p13.3 PKMYT1 protein kinase, membrane associated tyrosine/threonine 1
Mouse - 490 17 A3.3 Pkmyt1 protein kinase, membrane associated tyrosine/threonine 1
Rat - 490 10 q12 Pkmyt1 protein kinase, membrane associated tyrosine/threonine 1
Previous and Unofficial Names
MYT1 | protein kinase
Database Links
BRENDA
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 Membrane-associated Tyrosine- and Threonine-specific cdc2-inhibitory kinase MYT1 (PKMYT1)
PDB Id:  3P1A
Resolution:  1.7Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.11.1

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 Affinity Units Reference
PD166285 Hs Inhibition 7.1 – 8.1 pIC50 2-3
pIC50 7.1 – 8.1 (IC50 7.2x10-8 – 7x10-9 M) [2-3]
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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: PKMYT1
Ligand Sp. Type Action Affinity Units
PD-173955 Hs Inhibitor Inhibition 7.4 pKd
dasatinib Hs Inhibitor Inhibition 6.9 pKd
bosutinib Hs Inhibitor Inhibition 6.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
masitinib Hs Inhibitor Inhibition <5.5 pKd
A-674563 Hs Inhibitor Inhibition <5.5 pKd
gefitinib Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. 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]

2. Rohe A, Erdmann F, Bäßler C, Wichapong K, Sippl W, Schmidt M. (2012) In vitro and in silico studies on substrate recognition and acceptance of human PKMYT1, a Cdk1 inhibitory kinase. Bioorg. Med. Chem. Lett., 22 (2): 1219-23. [PMID:22189141]

3. 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]

4. 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: protein kinase, membrane associated tyrosine/threonine 1. Last modified on 19/02/2015. Accessed on 14/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2167.