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protein kinase, membrane associated tyrosine/threonine 1

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Target not currently curated in GtoImmuPdb

Target id: 2167

Nomenclature: protein kinase, membrane associated tyrosine/threonine 1

Abbreviated Name: Myt1

Family: WEE family

Contents:

Gene and Protein Information Click here for help
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 Click here for help
MYT1 | protein kinase
Database Links Click here for help
Alphafold Q99640 (Hs), Q9ESG9 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL3984 (Hs)
Ensembl Gene ENSG00000127564 (Hs), ENSMUSG00000023908 (Mm), ENSRNOG00000003657 (Rn)
Entrez Gene 9088 (Hs), 268930 (Mm), 287101 (Rn)
Human Protein Atlas ENSG00000127564 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:9088 (Hs), mmu:268930 (Mm), rno:287101 (Rn)
OMIM 602474 (Hs)
Pharos Q99640 (Hs)
RefSeq Nucleotide NM_001258450 (Hs), NM_023058 (Mm), NM_001105766 (Rn)
RefSeq Protein NP_004194 (Hs), NP_075545 (Mm), NP_001099236 (Rn)
UniProtKB Q99640 (Hs), Q9ESG9 (Mm)
Wikipedia PKMYT1 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Human Myt1 Kinase domain Bounded with RP-6306
PDB Id:  8D6E
Ligand:  (S)-RP-6306
Resolution:  2.15Å
Species:  Human
References:  3
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 Click here for help
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
(S)-RP-6306 Small molecule or natural product Hs Inhibition 8.7 pIC50 3
⤷ pIC50 8.7 (IC50 2x10-9 M) [3]
Description: Determined in a NanoBRET target engagement assay
PD166285 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 – 8.1 pIC50 2,4
⤷ pIC50 7.1 – 8.1 (IC50 7.2x10-8 – 7x10-9 M) [2,4]
DiscoveRx KINOMEscan® screen Click here for help
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: 1,5
Key to terms and symbols Click column headers to sort
Target used in screen: PKMYT1
Ligand Sp. Type Action Value Parameter
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.9 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition <5.5 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure 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. Szychowski J, Papp R, Dietrich E, Liu B, Vallée F, Leclaire ME, Fourtounis J, Martino G, Perryman AL, Pau V et al.. (2022) Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306. J Med Chem, 65 (15): 10251-10284. [PMID:35880755]

4. 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]

5. 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 27/07/2022. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2167.