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

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protein kinase, cAMP-dependent, catalytic, alpha subunit

Target not currently curated in GtoImmuPdb

Target id: 1476

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

Abbreviated Name: PKACa

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 19p13.1 PRKACA protein kinase cAMP-activated catalytic subunit alpha
Mouse - 351 8 C3 Prkaca protein kinase, cAMP dependent, catalytic, alpha
Rat - 351 19q11 Prkaca protein kinase cAMP-activated catalytic subunit alpha
Previous and Unofficial Names
cAMP-dependent protein kinase catalytic subunit C alpha | Cs-PKA | PKA C-alpha | PKCA1 | Pkaca | protein kinase, cAMP-dependent, catalytic, alpha | protein kinase, cAMP-dependent, alpha catalytic subunit | protein kinase, cAMP dependent, catalytic, alpha | protein kinase
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Complex of PKA with the bisubstrate protein kinase inhibitor ARC-1039
Resolution:  2.1Å
Species:  Human
References:  6
Enzyme Reaction
EC Number:

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

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GSK690693 Hs Inhibition 7.7 pKd 3
pKd 7.7 (Kd 1.9x10-8 M) [3]
H-89 Hs Inhibition 7.3 pKi 2
pKi 7.3 (Ki 4.8x10-8 M) [2]
ripasudil Hs Inhibition 5.7 pIC50 5
pIC50 5.7 (IC50 2.1x10-6 M) [5]
Inhibitor Comments
The data for H-89 provided here is derived from [2], but species and PKA subunit information is from BindingDB's entry for this ligand.
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 3,7

Key to terms and symbols Click column headers to sort
Target used in screen: PKAC-alpha
Ligand Sp. Type Action Value Parameter
GSK690693 Hs Inhibitor Inhibition 7.7 pKd
staurosporine Hs Inhibitor Inhibition 7.7 pKd
A-674563 Hs Inhibitor Inhibition 7.3 pKd
lestaurtinib Hs Inhibitor Inhibition 6.7 pKd
enzastaurin Hs Inhibitor Inhibition 6.5 pKd
tamatinib Hs Inhibitor Inhibition 6.2 pKd
midostaurin Hs Inhibitor Inhibition 6.1 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
crizotinib Hs Inhibitor Inhibition <5.5 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.

Reference: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: PKA/PKA
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 1.9 0.5 2.5
H-89 Hs Inhibitor Inhibition 10.5 2.0 6.0
K-252a Hs Inhibitor Inhibition 18.0 7.0 3.0
midostaurin Hs Inhibitor Inhibition 34.0 13.0 10.0
PKR inhibitor Hs Inhibitor Inhibition 40.1 25.0 5.0
SB 218078 Hs Inhibitor Inhibition 44.7 70.0 68.0
PP1 analog II Hs Inhibitor Inhibition 54.3 34.0 8.0
GF109203X Hs Inhibitor Inhibition 72.0 60.0 20.0
bosutinib Hs Inhibitor Inhibition 73.8
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 76.6 95.0 82.0
Displaying the top 10 most potent ligands  View all ligands in screen »


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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. Chijiwa T, Mishima A, Hagiwara M, Sano M, Hayashi K, Inoue T, Naito K, Toshioka T, Hidaka H. (1990) Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma cells. J. Biol. Chem., 265 (9): 5267-72. [PMID:2156866]

3. 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]

4. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

5. Isobe T, Mizuno K, Kaneko Y, Ohta M, Koide T, Tanabe S. (2014) Effects of K-115, a rho-kinase inhibitor, on aqueous humor dynamics in rabbits. Curr. Eye Res., 39 (8): 813-22. [PMID:24502505]

6. Pflug A, Rogozina J, Lavogina D, Enkvist E, Uri A, Engh RA, Bossemeyer D. (2010) Diversity of bisubstrate binding modes of adenosine analogue-oligoarginine conjugates in protein kinase a and implications for protein substrate interactions. J. Mol. Biol., 403 (1): 66-77. [PMID:20732331]

7. 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, alpha subunit. Last modified on 09/07/2019. Accessed on 12/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY,