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calcium/calmodulin dependent protein kinase kinase 1

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Target not currently curated in GtoImmuPdb

Target id: 1956

Nomenclature: calcium/calmodulin dependent protein kinase kinase 1

Abbreviated Name: CAMKK1

Family: Meta subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 505 17p13.2 CAMKK1 calcium/calmodulin dependent protein kinase kinase 1
Mouse - 505 11 B4 Camkk1 calcium/calmodulin-dependent protein kinase kinase 1, alpha
Rat - 505 10q24 Camkk1 calcium/calmodulin-dependent protein kinase kinase 1
Previous and Unofficial Names Click here for help
alpha CaMKK | CaM-kinase IV kinase | CAMKKA | calcium/calmodulin-dependent protein kinase kinase alpha | calcium/calmodulin-dependent protein kinase kinase 1, alpha
Database Links Click here for help
Alphafold Q8N5S9 (Hs), Q8VBY2 (Mm), P97756 (Rn)
BRENDA 2.7.11.17
ChEMBL Target CHEMBL5256 (Hs)
Ensembl Gene ENSG00000004660 (Hs), ENSMUSG00000020785 (Mm), ENSRNOG00000018242 (Rn)
Entrez Gene 84254 (Hs), 55984 (Mm), 60341 (Rn)
Human Protein Atlas ENSG00000004660 (Hs)
KEGG Enzyme 2.7.11.17
KEGG Gene hsa:84254 (Hs), mmu:55984 (Mm), rno:60341 (Rn)
OMIM 611411 (Hs)
Pharos Q8N5S9 (Hs)
RefSeq Nucleotide NM_032294 (Hs), NM_018883 (Mm), NM_031662 (Rn)
RefSeq Protein NP_115670 (Hs), NP_061371 (Mm), NP_113850 (Rn)
UniProtKB Q8N5S9 (Hs), Q8VBY2 (Mm), P97756 (Rn)
Wikipedia CAMKK1 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.17

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
STO609 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.8 pIC50 3
⤷ pIC50 6.8 (IC50 1.4x10-7 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: 2,4
Key to terms and symbols Click column headers to sort
Target used in screen: CAMKK1
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 10.4 pKd
BI-2536 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.6 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 7.2 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.9 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
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
Key to terms and symbols Click column headers to sort
Target used in screen: nd/CAMKK1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition -3.1
K-252a Small molecule or natural product Hs Inhibitor Inhibition 19.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 19.3
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 20.4
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 23.8
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 26.2
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 27.2
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 36.0
Syk inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 44.9
STO609 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 45.8
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. Tokumitsu H, Inuzuka H, Ishikawa Y, Ikeda M, Saji I, Kobayashi R. (2002) STO-609, a specific inhibitor of the Ca(2+)/calmodulin-dependent protein kinase kinase. J Biol Chem, 277 (18): 15813-8. [PMID:11867640]

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

Meta subfamily: calcium/calmodulin dependent protein kinase kinase 1. Last modified on 30/03/2016. Accessed on 14/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1956.