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nemo like kinase

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Target not currently curated in GtoImmuPdb

Target id: 2125

Nomenclature: nemo like kinase

Abbreviated Name: NLK

Family: nmo subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 527 17q11.2 NLK nemo like kinase
Mouse - 527 11 B5 Nlk nemo like kinase
Rat - 527 10q25 Nlk nemo like kinase
Previous and Unofficial Names Click here for help
LAK1 | nemo-like kinase
Database Links Click here for help
Alphafold Q9UBE8 (Hs), O54949 (Mm), D3ZSZ3 (Rn)
BRENDA 2.7.11.24
ChEMBL Target CHEMBL5364 (Hs)
Ensembl Gene ENSG00000087095 (Hs), ENSMUSG00000017376 (Mm), ENSRNOG00000008704 (Rn)
Entrez Gene 51701 (Hs), 18099 (Mm), 497961 (Rn)
Human Protein Atlas ENSG00000087095 (Hs)
KEGG Enzyme 2.7.11.24
KEGG Gene hsa:51701 (Hs), mmu:18099 (Mm), rno:497961 (Rn)
OMIM 609476 (Hs)
Pharos Q9UBE8 (Hs)
RefSeq Nucleotide NM_016231 (Hs), NM_008702 (Mm), NM_001191924 (Rn)
RefSeq Protein NP_057315 (Hs), NP_032728 (Mm), NP_001178853 (Rn)
UniProtKB Q9UBE8 (Hs), O54949 (Mm), D3ZSZ3 (Rn)
Wikipedia NLK (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.24

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
compound 25 [PMID: 17935989] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.8 pIC50 4
⤷ pIC50 5.8 (IC50 1.611x10-6 M) [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: 2,5
Key to terms and symbols Click column headers to sort
Target used in screen: NLK
Ligand Sp. Type Action Value Parameter
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 7.6 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
sorafenib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.1 pKd
doramapimod Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.0 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: 1,3
Key to terms and symbols Click column headers to sort
Target used in screen: NLK/NLK
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
SB220025 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 12.1 34.0 9.0
VX-702 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 15.8
p38 MAP kinase inhibitor Small molecule or natural product Hs Inhibitor Inhibition 16.0 42.0 12.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 20.5 28.0 8.0
PD 169316 Small molecule or natural product Hs Inhibitor Inhibition 23.1 31.0 40.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 26.1 34.0 19.0
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 27.5
p38 MAP kinase inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 30.7 69.0 14.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 35.5 29.0 5.0
PKR inhibitor, negative control Small molecule or natural product Hs Inhibitor Inhibition 38.9 47.0 15.0
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. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J, 451 (2): 313-28. [PMID:23398362]

4. Tao ZF, Chen Z, Bui MH, Kovar P, Johnson E, Bouska J, Zhang H, Rosenberg S, Sowin T, Lin NH. (2007) Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. Bioorg Med Chem Lett, 17 (23): 6593-601. [PMID:17935989]

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

nmo subfamily: nemo like kinase. Last modified on 16/09/2015. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2125.