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NIMA related kinase 8

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Target not currently curated in GtoImmuPdb

Target id: 2123

Nomenclature: NIMA related kinase 8

Abbreviated Name: NEK8

Family: NIMA (never in mitosis gene a)- related kinase (NEK) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 692 17q11.2 NEK8 NIMA related kinase 8
Mouse - 698 11 46.74 cM Nek8 NIMA (never in mitosis gene a)-related expressed kinase 8
Rat - 698 10 q25 Nek8 NIMA-related kinase 8
Previous and Unofficial Names Click here for help
ANPHP9 | JCK | NEK12A | Nima-related protein kinase 12a | NIMA-related kinase 8
Database Links Click here for help
Alphafold Q86SG6 (Hs), Q91ZR4 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL2417353 (Hs)
Ensembl Gene ENSG00000160602 (Hs), ENSMUSG00000017405 (Mm), ENSRNOG00000012866 (Rn)
Entrez Gene 284086 (Hs), 140859 (Mm), 287473 (Rn)
Human Protein Atlas ENSG00000160602 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:284086 (Hs), mmu:140859 (Mm), rno:287473 (Rn)
OMIM 609799 (Hs)
Orphanet ORPHA209484 (Hs)
Pharos Q86SG6 (Hs)
RefSeq Nucleotide NM_178170 (Hs), NM_080849 (Mm), NM_001105804 (Rn)
RefSeq Protein NP_835464 (Hs), NP_543125 (Mm), NP_001099274 (Rn)
UniProtKB Q86SG6 (Hs), Q91ZR4 (Mm)
Wikipedia NEK8 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.1
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: 1-2
Key to terms and symbols Click column headers to sort
Target used in screen: NEK9
Ligand Sp. Type Action Value Parameter
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.8 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.3 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.1 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
GSK-461364A Small molecule or natural product Hs Inhibitor Inhibition 6.0 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 5.7 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin 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 »
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Nephronophthisis 9; NPHP9
Synonyms: Nephronophthisis [Disease Ontology: DOID:12712]
Disease Ontology: DOID:12712
OMIM: 613824
Disease:  Renal-hepatic-pancreatic dysplasia 2; RHPD2
Synonyms: Renal-hepatic-pancreatic dysplasia [Orphanet: ORPHA294415]
OMIM: 615415
Orphanet: ORPHA294415

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. 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

NIMA (never in mitosis gene a)- related kinase (NEK) family: NIMA related kinase 8. Last modified on 29/01/2016. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2123.