protein kinase D1 | Protein kinase D (PKD) family | IUPHAR/BPS Guide to PHARMACOLOGY

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protein kinase D1

Target not currently curated in GtoImmuPdb

Target id: 1489

Nomenclature: protein kinase D1

Abbreviated Name: PKD1

Family: Protein kinase D (PKD) family

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 - 912 14q11 PRKD1 protein kinase D1
Mouse - 918 12 C1 Prkd1 protein kinase D1
Rat - 918 6q22 Prkd1 protein kinase D1
Previous and Unofficial Names
PKCM | PRKCM | serine/threonine-protein kinase D1 | PKC-mu
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.13

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
NIK SMI1 Hs Inhibition 7.1 pKi 3
pKi 7.1 (Ki 7.52x10-8 M) [3]
compound 13c [PMID: 20684591] Hs Inhibition 9.2 pIC50 8
pIC50 9.2 (IC50 6x10-10 M) [8]
Description: Measuring inhibition of synthetic substrate phosphorylation in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
CRT 0066101 Hs Inhibition 9.0 pIC50 7
pIC50 9.0 (IC50 1x10-9 M) [7]
BPKDi Hs Inhibition 9.0 pIC50 9
pIC50 9.0 (IC50 1x10-9 M) [9]
Description: In a biochemical enzyme assay.
Gö 6976 Hs Inhibition 7.7 pIC50 6
pIC50 7.7 (IC50 2x10-8 M) [6]
kb-NB142-70 Hs Inhibition 7.6 pIC50 2
pIC50 7.6 (IC50 2.83x10-8 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: 4,10

Key to terms and symbols Click column headers to sort
Target used in screen: PRKD1
Ligand Sp. Type Action Value Parameter
lestaurtinib Hs Inhibitor Inhibition 7.8 pKd
staurosporine Hs Inhibitor Inhibition 7.6 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.1 pKd
sunitinib Hs Inhibitor Inhibition 6.5 pKd
BI-2536 Hs Inhibitor Inhibition 6.5 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.4 pKd
alvocidib Hs Inhibitor Inhibition 6.3 pKd
GSK-1838705A Hs Inhibitor Inhibition 6.2 pKd
neratinib Hs Inhibitor Inhibition 6.1 pKd
crizotinib Hs Inhibitor Inhibition 6.0 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: 1,5

Key to terms and symbols Click column headers to sort
Target used in screen: PKCμ/PKCmu(PRKD1)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 1.3 1.0 0.0
staurosporine Hs Inhibitor Inhibition 1.4 1.5 -1.5
SB 218078 Hs Inhibitor Inhibition 1.9 87.0 49.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 2.1 6.0 1.0
PKR inhibitor Hs Inhibitor Inhibition 4.1 5.0 4.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 7.8 2.0 4.0
JAK inhibitor I Hs Inhibitor Inhibition 8.2 8.0 16.0
SU11652 Hs Inhibitor Inhibition 11.3 38.0 4.0
Gö 6976 Hs Inhibitor Inhibition 17.3 5.0 12.0
sunitinib Hs Inhibitor Inhibition 20.0
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. Bravo-Altamirano K, George KM, Frantz MC, Lavalle CR, Tandon M, Leimgruber S, Sharlow ER, Lazo JS, Wang QJ, Wipf P. (2011) Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D. ACS Med Chem Lett, 2 (2): 154-159. [PMID:21617763]

3. Brightbill HD, Suto E, Blaquiere N, Ramamoorthi N, Sujatha-Bhaskar S, Gogol EB, Castanedo GM, Jackson BT, Kwon YC, Haller S et al.. (2018) NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus. Nat Commun, 9 (1): 179. [PMID:29330524]

4. 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]

5. 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]

6. Gschwendt M, Dieterich S, Rennecke J, Kittstein W, Mueller HJ, Johannes FJ. (1996) Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes. FEBS Lett., 392 (2): 77-80. [PMID:8772178]

7. Harikumar KB, Kunnumakkara AB, Ochi N, Tong Z, Deorukhkar A, Sung B, Kelland L, Jamieson S, Sutherland R, Raynham T et al.. (2010) A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo. Mol. Cancer Ther., 9 (5): 1136-46. [PMID:20442301]

8. Meredith EL, Ardayfio O, Beattie K, Dobler MR, Enyedy I, Gaul C, Hosagrahara V, Jewell C, Koch K, Lee W et al.. (2010) Identification of orally available naphthyridine protein kinase D inhibitors. J. Med. Chem., 53 (15): 5400-21. [PMID:20684591]

9. Monovich L, Vega RB, Meredith E, Miranda K, Rao C, Capparelli M, Lemon DD, Phan D, Koch KA, Chapo JA et al.. (2010) A novel kinase inhibitor establishes a predominant role for protein kinase D as a cardiac class IIa histone deacetylase kinase. FEBS Lett., 584 (3): 631-7. [PMID:20018189]

10. 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 D (PKD) family: protein kinase D1. Last modified on 30/05/2018. Accessed on 16/02/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1489.