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protein kinase D1

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Target not currently curated in GtoImmuPdb

Target id: 1489

Nomenclature: protein kinase D1

Abbreviated Name: PKD1

Family: Protein kinase D (PKD) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 912 14q12 PRKD1 protein kinase D1
Mouse - 918 12 B3 Prkd1 protein kinase D1
Rat - 918 6q22 Prkd1 protein kinase D1
Previous and Unofficial Names Click here for help
PKCM | PRKCM | serine/threonine-protein kinase D1 | PKC-mu
Database Links Click here for help
Alphafold Q15139 (Hs), Q62101 (Mm), Q9WTQ1 (Rn)
BRENDA 2.7.11.13
CATH/Gene3D 2.30.29.30
ChEMBL Target CHEMBL3863 (Hs)
Ensembl Gene ENSG00000184304 (Hs), ENSMUSG00000002688 (Mm), ENSRNOG00000004165 (Rn)
Entrez Gene 5587 (Hs), 18760 (Mm), 85421 (Rn)
Human Protein Atlas ENSG00000184304 (Hs)
KEGG Enzyme 2.7.11.13
KEGG Gene hsa:5587 (Hs), mmu:18760 (Mm), rno:85421 (Rn)
OMIM 605435 (Hs)
Pharos Q15139 (Hs)
RefSeq Nucleotide NM_002742 (Hs), NM_008858 (Mm), NM_001276715 (Rn)
RefSeq Protein NP_002733 (Hs), NP_032884 (Mm), NP_001263644 (Rn)
UniProtKB Q15139 (Hs), Q62101 (Mm), Q9WTQ1 (Rn)
Wikipedia PRKD1 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.13

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
NIK SMI1 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.1 pKi 3
⤷ pKi 7.1 (Ki 7.52x10-8 M) [3]
compound 13c [PMID: 20684591] Small molecule or natural product 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 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.0 pIC50 7
⤷ pIC50 9.0 (IC50 1x10-9 M) [7]
BPKDi Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.0 pIC50 9
⤷ pIC50 9.0 (IC50 1x10-9 M) [9]
Description: In a biochemical enzyme assay.
Gö 6976 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.7 pIC50 6
⤷ pIC50 7.7 (IC50 2x10-8 M) [6]
kb-NB142-70 Small molecule or natural product Hs Inhibition 7.6 pIC50 2
⤷ pIC50 7.6 (IC50 2.83x10-8 M) [2]
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: 4,10
Key to terms and symbols Click column headers to sort
Target used in screen: PRKD1
Ligand Sp. Type Action Value Parameter
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.8 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
BI-2536 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
GSK-1838705A Small molecule or natural product Hs Inhibitor Inhibition 6.2 pKd
neratinib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 6.1 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand 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 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: 1,5
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 Small molecule or natural product Hs Inhibitor Inhibition 1.3 1.0 0.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.4 1.5 -1.5
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 1.9 87.0 49.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 2.1 6.0 1.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 4.1 5.0 4.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 2.0 4.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.2 8.0 16.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 11.3 38.0 4.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 17.3 5.0 12.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 20.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Antigen presentation
Immuno Process:  Inflammation

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. 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 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1489.