calcium/calmodulin dependent serine protein kinase | CASK family | IUPHAR/BPS Guide to PHARMACOLOGY

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calcium/calmodulin dependent serine protein kinase

Target not currently curated in GtoImmuPdb

Target id: 1959

Nomenclature: calcium/calmodulin dependent serine protein kinase

Abbreviated Name: CASK

Family: CASK family

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 898 Xp11.4 CASK calcium/calmodulin dependent serine protein kinase
Mouse - 897 X A1.1 Cask calcium/calmodulin-dependent serine protein kinase (MAGUK family)
Rat - 909 Xq12 Cask calcium/calmodulin dependent serine protein kinase
Previous and Unofficial Names
CAGH39 | FGS4 | LIN2 | Pals3 | peripheral plasma membrane protein CASK | TNRC8 | trinucleotide repeat containing 8 | calcium/calmodulin-dependent serine protein kinase (MAGUK family)
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of the Guanylate Kinase-like Domain of Human CASK
Resolution:  1.31Å
Species:  Human
References:  2
Enzyme Reaction
EC Number:
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: CASK
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 7.7 pKd
AT-7519 Hs Inhibitor Inhibition 7.6 pKd
R547 Hs Inhibitor Inhibition 7.2 pKd
crizotinib Hs Inhibitor Inhibition 6.8 pKd
lestaurtinib Hs Inhibitor Inhibition 6.5 pKd
BMS-387032 Hs Inhibitor Inhibition 6.4 pKd
bosutinib Hs Inhibitor Inhibition 6.1 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.0 pKd
ruxolitinib Hs Inhibitor Inhibition 5.8 pKd
PP-242 Hs Inhibitor Inhibition 5.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  FG syndrome 4
Synonyms: FG syndrome [Disease Ontology: DOID:14711] [Orphanet: ORPHA323]
Keller syndrome
Disease Ontology: DOID:14711
OMIM: 300422
Orphanet: ORPHA323
Disease:  Mental retardation and microcephaly with pontine and cerebellar hypoplasia
Synonyms: X-linked intellectual disability, Najm type [Orphanet: ORPHA163937]
OMIM: 300749
Orphanet: ORPHA163937


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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. Li Y, Spangenberg O, Paarmann I, Konrad M, Lavie A. (2002) Structural basis for nucleotide-dependent regulation of membrane-associated guanylate kinase-like domains. J. Biol. Chem., 277 (6): 4159-65. [PMID:11729206]

3. 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

CASK family: calcium/calmodulin dependent serine protein kinase. Last modified on 21/03/2014. Accessed on 24/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY,