protein kinase D1 (Protein kinase D (PKD) family)

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: 1-2
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
PP1 analog II Hs Inhibitor Inhibition 26.2 22.0 9.0
SP600125 Hs Inhibitor Inhibition 28.6 32.0 -1.0
Syk inhibitor II Hs Inhibitor Inhibition 30.3 35.0 8.0
bosutinib Hs Inhibitor Inhibition 43.7
SU9516 Hs Inhibitor Inhibition 47.9 57.0 4.0
Cdk4 inhibitor Hs Inhibitor Inhibition 51.9 111.0 72.0
SB220025 Hs Inhibitor Inhibition 54.6 46.0 3.0
Flt-3 inhibitor II Hs Inhibitor Inhibition 58.5 80.0 23.0
isogranulatimide Hs Inhibitor Inhibition 61.4 41.0 25.0
SU11274 Hs Inhibitor Inhibition 61.8 87.0 45.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 62.6 72.0 23.0
TGF-beta RI kinase inhibitor Hs Inhibitor Inhibition 63.0 65.0 22.0
fasudil Hs Inhibitor Inhibition 65.1 84.0 20.0
JNJ-7706621 Hs Inhibitor Inhibition 66.5 75.0 19.0
PD 169316 Hs Inhibitor Inhibition 67.4 64.0 52.0
ERK inhibitor II Hs Inhibitor Inhibition 68.4 56.0 12.0
Gö 6983 Hs Inhibitor Inhibition 68.8 108.0 58.0
dovitinib Hs Inhibitor Inhibition 69.0
JNK inhibitor, negative control Hs Inhibitor Inhibition 69.3 61.0 54.0
JAK3 inhibitor II Hs Inhibitor Inhibition 70.1 47.0 16.0
GF109203X Hs Inhibitor Inhibition 71.6 108.0 43.0
midostaurin Hs Inhibitor Inhibition 71.6 85.0 79.0
indirubin derivative E804 Hs Inhibitor Inhibition 72.7 73.0 32.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 77.4 88.0 82.0
aloisine A Hs Inhibitor Inhibition 77.7 83.0 59.0
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 78.1 59.0 18.0
Flt-3 inhibitor III Hs Inhibitor Inhibition 78.4 93.0 36.0
GTP-14564 Hs Inhibitor Inhibition 79.2 103.0 72.0
IKK-2 inhibitor IV Hs Inhibitor Inhibition 79.6 58.0 29.0
Syk inhibitor Hs Inhibitor Inhibition 80.0 84.0 59.0
dorsomorphin Hs Inhibitor Inhibition 81.9 96.0 54.0
GSK-3 inhibitor X Hs Inhibitor Inhibition 82.1 85.0 81.0
JNK inhibitor V Hs Inhibitor Inhibition 82.4 73.0 36.0
p38 MAP kinase inhibitor Hs Inhibitor Inhibition 84.7 99.0 37.0
indirubin-3'-monoxime Hs Inhibitor Inhibition 85.0 113.0 65.0
semaxanib Hs Inhibitor Inhibition 85.3 78.0 88.0
gefitinib Hs Inhibitor Inhibition 85.4
STO609 Hs Inhibitor Inhibition 86.2 110.0 57.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 86.5 104.0 106.0
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 87.5 89.0 76.0
JNK inhibitor VIII Hs Inhibitor Inhibition 88.4 90.0 54.0
PDGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 88.7 101.0 103.0
casein kinase II inhibitor III Hs Inhibitor Inhibition 88.9 109.0 64.0
Cdk1 inhibitor Hs Inhibitor Inhibition 89.5 99.0 65.0
p38 MAP kinase inhibitor III Hs Inhibitor Inhibition 90.1 97.0 44.0
SKF-86002 Hs Inhibitor Inhibition 90.2 102.0 48.0
KU-55933 Hs Inhibitor Inhibition 90.3 86.0 80.0
SB202190 Hs Inhibitor Inhibition 90.7 94.0 36.0
CGP74514A Hs Inhibitor Inhibition 90.8 97.0 61.0
VEGF receptor 2 kinase inhibitor I Hs Inhibitor Inhibition 91.3 88.0 106.0
PKR inhibitor, negative control Hs Inhibitor Inhibition 91.5 106.0 67.0
LY 303511 Hs Inhibitor Inhibition 91.9 96.0 90.0
Akt inhibitor IV Hs Inhibitor Inhibition 91.9 92.0 90.0
CGP53353 Hs Inhibitor Inhibition 92.2 94.0 72.0
TGF-beta RI inhibitor III Hs Inhibitor Inhibition 92.3 109.0 72.0
PD 158780 Hs Inhibitor Inhibition 92.3 86.0 49.0
AG1478 Hs Inhibitor Inhibition 92.3 110.0 73.0
AG 490 Hs Inhibitor Inhibition 92.5 108.0 98.0
VEGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 92.9
aloisine Hs Inhibitor Inhibition 92.9 121.0 84.0
mubritinib Hs Inhibitor Inhibition 93.2
VEGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 93.2 89.0 95.0
AG 1296 Hs Inhibitor Inhibition 93.3 102.0 96.0
PDGF receptor tyrosine kinase inhibitor IV Hs Inhibitor Inhibition 93.6 78.0 88.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 93.6 90.0 100.0
VEGF receptor 2 kinase inhibitor II Hs Inhibitor Inhibition 93.8 91.0 93.0
BAY 11-7082 Hs Inhibitor Inhibition 93.8 98.0 84.0
aurora kinase inhibitor III Hs Inhibitor Inhibition 94.1 103.0 111.0
aminopurvalanol A Hs Inhibitor Inhibition 94.2 99.0 81.0
PKCbeta inhibitor Hs Inhibitor Inhibition 94.4 91.0 58.0
TWS119 Hs Inhibitor Inhibition 94.4 80.0 51.0
Tpl2 kinase inhibitor Hs Inhibitor Inhibition 94.5 80.0 39.0
Akt inhibitor VIII Hs Inhibitor Inhibition 94.7 96.0 97.0
PI 3-Kg inhibitor II Hs Inhibitor Inhibition 94.8 105.0 77.0
erlotinib Hs Inhibitor Inhibition 94.8
PI 3-Kg inhibitor Hs Inhibitor Inhibition 94.8 103.0 88.0
Cdk1/5 inhibitor Hs Inhibitor Inhibition 94.9 83.0 69.0
VEGF receptor 2 kinase inhibitor IV Hs Inhibitor Inhibition 95.1 84.0 97.0
GW-2580 Hs Inhibitor Inhibition 95.2 81.0 77.0
compound 56 [PMID: 8568816] Hs Inhibitor Inhibition 95.4 101.0 54.0
Rho kinase inhibitor III Hs Inhibitor Inhibition 95.5 87.0 69.0
Src kinase inhibitor I Hs Inhibitor Inhibition 95.6 95.0 103.0
SC-68376 Hs Inhibitor Inhibition 95.6 113.0 80.0
alsterpaullone Hs Inhibitor Inhibition 95.6 93.0 79.0
bohemine Hs Inhibitor Inhibition 95.8 91.0 72.0
SB203580 Hs Inhibitor Inhibition 95.8 123.0 66.0
tandutinib Hs Inhibitor Inhibition 96.1
Lck inhibitor Hs Inhibitor Inhibition 96.2 77.0 47.0
D4476 Hs Inhibitor Inhibition 96.3 87.0 62.0
triciribine Hs Inhibitor Inhibition 96.4 88.0 102.0
PQ401 Hs Inhibitor Inhibition 96.6 95.0 87.0
Rho kinase inhibitor IV Hs Inhibitor Inhibition 96.7 83.0 71.0
SKI II Hs Inhibitor Inhibition 96.8 94.0 100.0
purvalanol A Hs Inhibitor Inhibition 96.9 81.0 86.0
ATM/ATR kinase inhibitor Hs Inhibitor Inhibition 96.9 110.0 88.0
pazopanib Hs Inhibitor Inhibition 96.9
Cdk2 inhibitor III Hs Inhibitor Inhibition 97.2 91.0 71.0
wortmannin Hs Inhibitor Inhibition 97.3
herbimycin A Hs Inhibitor Inhibition 97.3 119.0 102.0
tofacitinib Hs Inhibitor Inhibition 97.3
Y27632 Hs Inhibitor Inhibition 97.5 63.0 17.0
IRAK-1/4 inhibitor Hs Inhibitor Inhibition 97.5 76.0 89.0
bisindolylmaleimide IV Hs Inhibitor Inhibition 97.6 89.0 71.0
GSK-3beta inhibitor II Hs Inhibitor Inhibition 97.6 72.0 71.0
AGL 2043 Hs Inhibitor Inhibition 97.7 94.0 95.0
VX-702 Hs Inhibitor Inhibition 97.7
imatinib Hs Inhibitor Inhibition 97.9
PD 174265 Hs Inhibitor Inhibition 97.9 85.0 82.0
IC261 Hs Inhibitor Inhibition 98.0 84.0 90.0
JAK3 inhibitor IV Hs Inhibitor Inhibition 98.0 74.0 84.0
PP3 Hs Inhibitor Inhibition 98.1 92.0 104.0
purvalanol A Hs Inhibitor Inhibition 98.2 81.0 86.0
masitinib Hs Inhibitor Inhibition 98.2
LY 294002 Hs Inhibitor Inhibition 98.3 110.0 92.0
PI-103 Hs Inhibitor Inhibition 98.3 97.0 89.0
MK2a inhibitor Hs Inhibitor Inhibition 98.4 113.0 105.0
MEK inhibitor I Hs Inhibitor Inhibition 98.5 83.0 64.0
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibitor Inhibition 98.7 89.0 84.0
H-89 Hs Inhibitor Inhibition 98.7 101.0 20.0
AG 9 Hs Inhibitor Inhibition 98.7 102.0 106.0
seliciclib Hs Inhibitor Inhibition 98.8
MNK1 inhibitor Hs Inhibitor Inhibition 98.9 81.0 64.0
dasatinib Hs Inhibitor Inhibition 98.9
compound 52 [PMID: 9677190] Hs Inhibitor Inhibition 99.2 77.0 57.0
Chk2 inhibitor II Hs Inhibitor Inhibition 99.3 109.0 79.0
NF-kB activation inhibitor Hs Inhibitor Inhibition 99.3 91.0 82.0
fascaplysin Hs Inhibitor Inhibition 99.3 83.0 71.0
vandetanib Hs Inhibitor Inhibition 99.3
BPIQ-I Hs Inhibitor Inhibition 99.4 94.0 82.0
lapatinib Hs Inhibitor Inhibition 99.4
Bcr-abl inhibitor GNF-2 Hs Inhibitor Inhibition 99.5 108.0 98.0
Flt-3 inhibitor Hs Inhibitor Inhibition 99.6 89.0 96.0
sorafenib Hs Inhibitor Inhibition 99.7
nilotinib Hs Inhibitor Inhibition 99.7
Cdk4 inhibitor II Hs Inhibitor Inhibition 99.8 96.0 73.0
KN-93 Hs Inhibitor Inhibition 100.0 83.0 77.0
chelerythrine Hs Inhibitor Inhibition 100.0 110.0 61.0
SB 202474 Hs Inhibitor Inhibition 100.0 103.0 92.0
AG 1024 Hs Inhibitor Inhibition 100.1 98.0 117.0
AG 1295 Hs Inhibitor Inhibition 100.2 116.0 115.0
DMBI Hs Inhibitor Inhibition 100.3 96.0 81.0
EGFR inhibitor Hs Inhibitor Inhibition 100.4 99.0 88.0
vatalanib Hs Inhibitor Inhibition 100.5
GSK-3beta inhibitor I Hs Inhibitor Inhibition 100.6 90.0 64.0
Ro-32-0432 Hs Inhibitor Inhibition 100.7
kenpaullone Hs Inhibitor Inhibition 100.8 99.0 80.0
Akt inhibitor X Hs Inhibitor Inhibition 100.9 92.0 95.0
KN-62 Hs Inhibitor Inhibition 101.0 113.0 89.0
EGFR/ErbB-2 inhibitor Hs Inhibitor Inhibition 101.3 93.0 113.0
AG 112 Hs Inhibitor Inhibition 101.3 93.0 103.0
JNK inhibitor IX Hs Inhibitor Inhibition 101.3 92.0 83.0
diacylglycerol kinase inhibitor II Hs Inhibitor Inhibition 101.3 113.0 84.0
NU-7026 Hs Inhibitor Inhibition 101.7 77.0 79.0
Syk inhibitor III Hs Inhibitor Inhibition 101.7 91.0 88.0
tozasertib Hs Inhibitor Inhibition 101.7
SU6656 Hs Inhibitor Inhibition 101.8 91.0 101.0
PDGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 102.1 102.0 66.0
DNA-PK inhibitor III Hs Inhibitor Inhibition 102.3 92.0 95.0
Cdk4 inhibitor III Hs Inhibitor Inhibition 102.4 76.0 73.0
DNA-PK inhibitor V Hs Inhibitor Inhibition 102.5 95.0 109.0
Cdk/Crk inhibitor Hs Inhibitor Inhibition 102.5 110.0 95.0
ERK inhibitor III Hs Inhibitor Inhibition 102.5 106.0 104.0
PD98059 Hs Inhibitor Inhibition 102.9 85.0 95.0
MEK1/2 inhibitor Hs Inhibitor Inhibition 102.9 82.0 68.0
MEK inhibitor II Hs Inhibitor Inhibition 104.0 72.0 76.0
GSK-3beta inhibitor VIII Hs Inhibitor Inhibition 104.1 95.0 86.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 106.5 88.0 82.0
PDGF RTK inhibitor Hs Inhibitor Inhibition 137.2 87.0 89.0

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. 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]