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citron rho-interacting serine/threonine kinase

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Target id: 1509

Nomenclature: citron rho-interacting serine/threonine kinase

Abbreviated Name: CRIK

Family: Other DMPK family kinases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 2027 12q24.23 CIT citron rho-interacting serine/threonine kinase
Mouse - 2055 5 F Cit citron
Rat - 2055 12q16 Cit citron rho-interacting serine/threonine kinase
Previous and Unofficial Names Click here for help
citron-K kinase | postsynaptic density protein (citron) | Cit-k | citron-N | CRIK-SK | serine/threonine-protein kinase 21 | STK21 | citron (rho-interacting, serine/threonine kinase 21)
Database Links Click here for help
Alphafold O14578 (Hs), P49025 (Mm)
BRENDA 2.7.11.1
CATH/Gene3D 2.30.29.30
ChEMBL Target CHEMBL5579 (Hs)
Ensembl Gene ENSG00000122966 (Hs), ENSMUSG00000029516 (Mm), ENSRNOG00000001143 (Rn)
Entrez Gene 11113 (Hs), 12704 (Mm), 83620 (Rn)
Human Protein Atlas ENSG00000122966 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:11113 (Hs), mmu:12704 (Mm), rno:83620 (Rn)
OMIM 605629 (Hs)
Pharos O14578 (Hs)
RefSeq Nucleotide NM_001206999 (Hs), NM_007708 (Mm), NM_001029911 (Rn)
RefSeq Protein NP_009105 (Hs), NP_031734 (Mm), NP_001025082 (Rn)
UniProtKB O14578 (Hs), P49025 (Mm)
Wikipedia CIT (Hs)
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
C3TD879 Small molecule or natural product Hs Inhibition >8.0 pKd 2
⤷ pKd >8.0 (Kd <1x10-8 M) [2]
Description: Binding affinity
C3TD879 Small molecule or natural product Hs Inhibition 7.9 pIC50 2
⤷ pIC50 7.9 (IC50 1.2x10-8 M) [2]
Description: Catalytic inhibition in a biochemical assay.
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: 1,3
Key to terms and symbols Click column headers to sort
Target used in screen: CIT
Ligand Sp. Type Action Value Parameter
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.3 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
CHIR-265 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 7.0 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
motesanib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

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. Maw JJ, Coker JA, Arya T, Goins CM, Sonawane D, Han SH, Rees MG, Ronan MM, Roth JA, Wang NS et al.. (2024) Discovery and Characterization of Selective, First-in-Class Inhibitors of Citron Kinase. J Med Chem, 67 (4): 2631-2666. [PMID:38330278]

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

Other DMPK family kinases: citron rho-interacting serine/threonine kinase. Last modified on 15/02/2024. Accessed on 16/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1509.