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leukocyte receptor tyrosine kinase

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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

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 864 15q15.1 LTK leukocyte receptor tyrosine kinase
Mouse 1 888 2 59.97 cM Ltk leukocyte tyrosine kinase
Rat - 577 3q35 Ltk leukocyte receptor tyrosine kinase
Previous and Unofficial Names Click here for help
TYK1
Database Links Click here for help
Alphafold P29376 (Hs), P08923 (Mm)
BRENDA 2.7.10.1
ChEMBL Target CHEMBL5627 (Hs)
Ensembl Gene ENSG00000062524 (Hs), ENSMUSG00000027297 (Mm), ENSRNOG00000025130 (Rn)
Entrez Gene 4058 (Hs), 17005 (Mm), 311337 (Rn)
Human Protein Atlas ENSG00000062524 (Hs)
KEGG Enzyme 2.7.10.1
KEGG Gene hsa:4058 (Hs), mmu:17005 (Mm), rno:311337 (Rn)
OMIM 151520 (Hs)
Pharos P29376 (Hs)
RefSeq Nucleotide NM_001135685 (Hs), NM_008523 (Mm), NM_206941 (Mm), NM_206942 (Mm), NM_203345 (Mm), NM_001107763 (Rn)
RefSeq Protein NP_001129157 (Hs), NP_996824 (Mm), NP_996825 (Mm), NP_032549 (Mm), NP_976220 (Mm), NP_001101233 (Rn)
UniProtKB P29376 (Hs), P08923 (Mm)
Wikipedia LTK (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.10.1

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
belizatinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.6 pKd 5
⤷ pKd 8.6 (Kd 2.5x10-9 M) [5]
Description: Binding affinity in vitro.
compound 20 [PMID: 30998356] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.3 pKi 6
⤷ pKi 6.3 (Ki 5.67x10-7 M) [6]
Description: Measuring in vitro enzyme inhibitory activity.
gilteritinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition ~9.7 pIC50 4
⤷ pIC50 ~9.7 (IC50 ~2x10-10 M) [4]
compound 8e [PMID: 24432909] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.7 pIC50 3
⤷ pIC50 8.7 (IC50 2x10-9 M) [3]
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: 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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.0 pKd
GSK-1838705A Small molecule or natural product Hs Inhibitor Inhibition 9.0 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.9 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.4 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.3 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition 6.3 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure 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 Click here for help
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 0.5
JAK3 inhibitor II Small molecule or natural product Hs Inhibitor Inhibition 5.4
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.8
K-252a Small molecule or natural product Hs Inhibitor Inhibition 9.8
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 11.6
TWS119 Small molecule or natural product Hs Inhibitor Inhibition 16.8
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 20.6
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 21.8
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 27.6
semaxanib Small molecule or natural product Ligand has a PDB structure 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 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1838.