leukocyte receptor tyrosine kinase | Type XIX RTKs: Leukocyte tyrosine kinase (LTK) receptor family | IUPHAR/BPS Guide to PHARMACOLOGY

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leukocyte receptor tyrosine kinase

Target not currently curated in GtoImmuPdb

Target id: 1838

Nomenclature: leukocyte receptor tyrosine kinase

Abbreviated Name: LTK

Family: Type XIX RTKs: Leukocyte tyrosine kinase (LTK) receptor 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 1 734 15q15.1-q21.1 LTK leukocyte receptor tyrosine kinase
Mouse 1 827 2 Ltk leukocyte tyrosine kinase
Rat - 577 3q35 Ltk leukocyte receptor tyrosine kinase
Previous and Unofficial Names
TYK1
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.10.1

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 Value Parameter Reference
belizatinib Hs Inhibition 8.6 pKd 5
pKd 8.6 (Kd 2.5x10-9 M) [5]
Description: Binding affinity in vitro.
compound 20 [PMID: 30998356] Hs Inhibition 6.3 pKi 6
pKi 6.3 (Ki 5.67x10-7 M) [6]
Description: Measuring in vitro enzyme inhibitory activity.
gilteritinib Hs Inhibition ~9.7 pIC50 4
pIC50 ~9.7 (IC50 ~2x10-10 M) [4]
compound 8e [PMID: 24432909] Hs Inhibition 8.7 pIC50 3
pIC50 8.7 (IC50 2x10-9 M) [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: 2,7

Key to terms and symbols Click column headers to sort
Target used in screen: LTK
Ligand Sp. Type Action Value Parameter
NVP-TAE684 Hs Inhibitor Inhibition 9.0 pKd
GSK-1838705A Hs Inhibitor Inhibition 9.0 pKd
crizotinib Hs Inhibitor Inhibition 7.9 pKd
staurosporine Hs Inhibitor Inhibition 7.4 pKd
foretinib Hs Inhibitor Inhibition 7.0 pKd
AST-487 Hs Inhibitor Inhibition 6.8 pKd
ruxolitinib Hs Inhibitor Inhibition 6.4 pKd
lestaurtinib Hs Inhibitor Inhibition 6.3 pKd
vandetanib Hs Inhibitor Inhibition 6.3 pKd
linifanib Hs Inhibitor Inhibition 6.3 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/TYK1(LTK)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 0.5
JAK3 inhibitor II Hs Inhibitor Inhibition 5.4
Gö 6976 Hs Inhibitor Inhibition 8.8
K-252a Hs Inhibitor Inhibition 9.8
SU11652 Hs Inhibitor Inhibition 11.6
TWS119 Hs Inhibitor Inhibition 16.8
JAK inhibitor I Hs Inhibitor Inhibition 20.6
SB 218078 Hs Inhibitor Inhibition 21.8
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 27.6
semaxanib Hs Inhibitor Inhibition 28.2
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. 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]

3. Huang Q, Johnson TW, Bailey S, Brooun A, Bunker KD, Burke BJ, Collins MR, Cook AS, Cui JJ, Dack KN et al.. (2014) Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. J. Med. Chem., 57 (4): 1170-87. [PMID:24432909]

4. Lee LY, Hernandez D, Rajkhowa T, Smith SC, Raman JR, Nguyen B, Small D, Levis M. (2017) Preclinical studies of gilteritinib, a next-generation FLT3 inhibitor. Blood, 129 (2): 257-260. [PMID:27908881]

5. Lewis RT, Bode CM, Choquette DM, Potashman M, Romero K, Stellwagen JC, Teffera Y, Moore E, Whittington DA, Chen H et al.. (2012) The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer. J. Med. Chem., 55 (14): 6523-40. [PMID:22734674]

6. Riggs JR, Elsner J, Cashion D, Robinson D, Tehrani L, Nagy M, Fultz KE, Krishna Narla R, Peng X, Tran T et al.. (2019) Design and Optimization Leading to an Orally Active TTK Protein Kinase Inhibitor with Robust Single Agent Efficacy. J. Med. Chem., 62 (9): 4401-4410. [PMID:30998356]

7. 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

Type XIX RTKs: Leukocyte tyrosine kinase (LTK) receptor family: leukocyte receptor tyrosine kinase. Last modified on 04/09/2019. Accessed on 20/10/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1838.