calcium/calmodulin dependent protein kinase kinase 1 | Meta subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

calcium/calmodulin dependent protein kinase kinase 1

Target not currently curated in GtoImmuPdb

Target id: 1956

Nomenclature: calcium/calmodulin dependent protein kinase kinase 1

Abbreviated Name: CAMKK1

Family: Meta subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 505 17p13.3 CAMKK1 calcium/calmodulin dependent protein kinase kinase 1
Mouse - 505 11 B4 Camkk1 calcium/calmodulin-dependent protein kinase kinase 1, alpha
Rat - 505 10 q24 Camkk1 calcium/calmodulin-dependent protein kinase kinase 1
Previous and Unofficial Names
alpha CaMKK | CaM-kinase IV kinase | CAMKKA | calcium/calmodulin-dependent protein kinase kinase alpha | calcium/calmodulin-dependent protein kinase kinase 1, alpha
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.17

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
STO609 Hs Inhibition 6.8 pIC50 3
pIC50 6.8 (IC50 1.4x10-7 M) [3]
DiscoveRx KINOMEscan® screen
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 Hs Inhibitor Inhibition 10.4 pKd
BI-2536 Hs Inhibitor Inhibition 7.7 pKd
lestaurtinib Hs Inhibitor Inhibition 7.6 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.3 pKd
PHA-665752 Hs Inhibitor Inhibition 7.2 pKd
alvocidib Hs Inhibitor Inhibition 7.1 pKd
midostaurin Hs Inhibitor Inhibition 6.9 pKd
KW-2449 Hs Inhibitor Inhibition 6.7 pKd
AST-487 Hs Inhibitor Inhibition 6.7 pKd
sunitinib 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
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 Hs Inhibitor Inhibition -3.1
K-252a Hs Inhibitor Inhibition 19.0
Gö 6976 Hs Inhibitor Inhibition 19.3
midostaurin Hs Inhibitor Inhibition 20.4
JAK3 inhibitor VI Hs Inhibitor Inhibition 23.8
indirubin derivative E804 Hs Inhibitor Inhibition 26.2
SB 218078 Hs Inhibitor Inhibition 27.2
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 36.0
Syk inhibitor Hs Inhibitor Inhibition 44.9
STO609 Hs Inhibitor Inhibition 45.8
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

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 22/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1956.