nemo like kinase | nmo subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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nemo like kinase

Target not currently curated in GtoImmuPdb

Target id: 2125

Nomenclature: nemo like kinase

Abbreviated Name: NLK

Family: nmo subfamily

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 - 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
LAK1 | nemo-like kinase
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: 2.7.11.24

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
compound 25 [PMID: 17935989] Hs Inhibition 5.8 pIC50 4
pIC50 5.8 (IC50 1.611x10-6 M) [4]
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: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: NLK
Ligand Sp. Type Action Value Parameter
SB203580 Hs Inhibitor Inhibition 7.6 pKd
PD-173955 Hs Inhibitor Inhibition 7.5 pKd
AST-487 Hs Inhibitor Inhibition 6.8 pKd
foretinib Hs Inhibitor Inhibition 6.8 pKd
staurosporine Hs Inhibitor Inhibition 6.7 pKd
dasatinib Hs Inhibitor Inhibition 6.6 pKd
PP-242 Hs Inhibitor Inhibition 6.3 pKd
sorafenib Hs Inhibitor Inhibition 6.2 pKd
lestaurtinib Hs Inhibitor Inhibition 6.1 pKd
doramapimod 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
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 Hs Inhibitor Inhibition 12.1 34.0 9.0
VX-702 Hs Inhibitor Inhibition 15.8
p38 MAP kinase inhibitor Hs Inhibitor Inhibition 16.0 42.0 12.0
staurosporine Hs Inhibitor Inhibition 20.5 28.0 8.0
PD 169316 Hs Inhibitor Inhibition 23.1 31.0 40.0
JAK inhibitor I Hs Inhibitor Inhibition 26.1 34.0 19.0
dasatinib Hs Inhibitor Inhibition 27.5
p38 MAP kinase inhibitor III Hs Inhibitor Inhibition 30.7 69.0 14.0
PKR inhibitor Hs Inhibitor Inhibition 35.5 29.0 5.0
PKR inhibitor, negative control 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 08/12/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2125.