protein kinase, cAMP-dependent, catalytic, beta subunit | Protein kinase A (PKA) family | IUPHAR/BPS Guide to PHARMACOLOGY

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protein kinase, cAMP-dependent, catalytic, beta subunit

Target not currently curated in GtoImmuPdb

Target id: 1477

Nomenclature: protein kinase, cAMP-dependent, catalytic, beta subunit

Abbreviated Name: PKACb

Family: Protein kinase A (PKA) family

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

Quaternary Structure: Complexes
protein kinase A
Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 351 1p36.1 PRKACB protein kinase cAMP-activated catalytic subunit beta
Mouse - 351 3 H3 Prkacb protein kinase, cAMP dependent, catalytic, beta
Rat - 351 2q44 Prkacb protein kinase cAMP-activated catalytic subunit beta
Previous and Unofficial Names
PKA C-beta | cAMP-dependent protein kinase C beta | protein kinase, cAMP-dependent, catalytic, beta | protein kinase, cAMP-dependent, beta catalytic subunit | protein kinase
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: 2.7.11.11

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
GSK690693 Hs Inhibition 7.9 pKd 1
pKd 7.9 (Kd 1.3x10-8 M) [1]
staurosporine Hs Inhibition 7.5 pIC50 2
pIC50 7.5 (IC50 3.3x10-8 M) [2]
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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: PKAC-beta
Ligand Sp. Type Action Value Parameter
GSK690693 Hs Inhibitor Inhibition 7.9 pKd
staurosporine Hs Inhibitor Inhibition 7.5 pKd
A-674563 Hs Inhibitor Inhibition 7.1 pKd
lestaurtinib Hs Inhibitor Inhibition 6.8 pKd
midostaurin Hs Inhibitor Inhibition 6.6 pKd
AST-487 Hs Inhibitor Inhibition 6.6 pKd
tamatinib Hs Inhibitor Inhibition 6.3 pKd
enzastaurin Hs Inhibitor Inhibition 6.2 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 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. Djung JF, Mears RJ, Montalbetti CA, Coulter TS, Golebiowski A, Carr AN, Barker O, Greis KD, Zhou S, Dolan E et al.. (2011) The synthesis and evaluation of indolylureas as PKCĪ± inhibitors. Bioorg. Med. Chem., 19 (8): 2742-50. [PMID:21435888]

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

Protein kinase A (PKA) family: protein kinase, cAMP-dependent, catalytic, beta subunit. Last modified on 12/04/2019. Accessed on 14/12/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1477.