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calcium/calmodulin dependent serine protein kinase

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Target id: 1959

Nomenclature: calcium/calmodulin dependent serine protein kinase

Abbreviated Name: CASK

Family: CASK family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 926 Xp11.4 CASK calcium/calmodulin dependent serine protein kinase
Mouse - 926 X 8.43 cM Cask calcium/calmodulin dependent serine protein kinase
Rat - 909 Xq12 Cask calcium/calmodulin dependent serine protein kinase
Previous and Unofficial Names Click here for help
CAGH39 | FGS4 | LIN2 | Pals3 | peripheral plasma membrane protein CASK | TNRC8 | trinucleotide repeat containing 8 | calcium/calmodulin-dependent serine protein kinase (MAGUK family)
Database Links Click here for help
Alphafold O14936 (Hs), O70589 (Mm), Q62915 (Rn)
BRENDA 2.7.11.1
CATH/Gene3D 1.10.287.650
ChEMBL Target CHEMBL1908381 (Hs)
Ensembl Gene ENSG00000147044 (Hs), ENSMUSG00000031012 (Mm), ENSRNOG00000060946 (Rn)
Entrez Gene 8573 (Hs), 12361 (Mm), 29647 (Rn)
Human Protein Atlas ENSG00000147044 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:8573 (Hs), mmu:12361 (Mm), rno:29647 (Rn)
OMIM 300172 (Hs)
Orphanet ORPHA165976 (Hs)
Pharos O14936 (Hs)
RefSeq Nucleotide NM_001126054 (Hs), NM_009806 (Mm), NM_022184 (Rn)
RefSeq Protein NP_001119526 (Hs), NP_033936 (Mm), NP_071520 (Rn)
UniProtKB O14936 (Hs), O70589 (Mm), Q62915 (Rn)
Wikipedia CASK (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of the Guanylate Kinase-like Domain of Human CASK
PDB Id:  1KGD
Resolution:  1.31Å
Species:  Human
References:  2
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of pseudokinase CASK in complex with compound 26
PDB Id:  7OAK
Ligand:  compound 26 [PMID: 34543009]
Resolution:  2.23Å
Species:  None
References:  3
Enzyme Reaction Click here for help
EC Number: 2.7.11.1

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
compound 26 [PMID: 34543009] Small molecule or natural product Ligand has a PDB structure Hs Binding 7.7 pKd 3
⤷ pKd 7.7 (Kd 2.2x10-8 M) [3]
compound 26 [PMID: 34543009] Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.1 pIC50 3
⤷ pIC50 7.1 (IC50 8x10-8 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: 1,4
Key to terms and symbols Click column headers to sort
Target used in screen: CASK
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
AT-7519 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
R547 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.8 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
BMS-387032 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
bosutinib 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 6.0 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.8 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology Click here for help
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

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. 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. Russ N, Schröder M, Berger BT, Mandel S, Aydogan Y, Mauer S, Pohl C, Drewry DH, Chaikuad A, Müller S et al.. (2021) Design and Development of a Chemical Probe for Pseudokinase Ca2+/calmodulin-Dependent Ser/Thr Kinase. J Med Chem, 64 (19): 14358-14376. [PMID:34543009]

4. 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 24/07/2023. Accessed on 30/10/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1959.