WNK lysine deficient protein kinase 3 (Wnk 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: WNK3/WNK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 60.3 70.0 8.0
staurosporine Hs Inhibitor Inhibition 73.6 83.5 40.0
Flt-3 inhibitor II Hs Inhibitor Inhibition 74.6 88.0 44.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 74.9 74.0 31.0
aminopurvalanol A Hs Inhibitor Inhibition 76.9 88.0 37.0
compound 52 [PMID: 9677190] Hs Inhibitor Inhibition 77.7 88.0 57.0
dorsomorphin Hs Inhibitor Inhibition 78.1 107.0 91.0
isogranulatimide Hs Inhibitor Inhibition 79.1 74.0 45.0
indirubin derivative E804 Hs Inhibitor Inhibition 79.7 76.0 50.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 80.6 90.0 63.0
JNK inhibitor V Hs Inhibitor Inhibition 81.3 73.0 39.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 82.2 77.0 64.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 82.6 99.0 58.0
IRAK-1/4 inhibitor Hs Inhibitor Inhibition 84.8 96.0 78.0
PKR inhibitor Hs Inhibitor Inhibition 84.9 84.0 67.0
Lck inhibitor Hs Inhibitor Inhibition 85.2 91.0 52.0
PI 3-Kg inhibitor Hs Inhibitor Inhibition 85.8 83.0 79.0
Akt inhibitor IV Hs Inhibitor Inhibition 85.9 100.0 44.0
SB 218078 Hs Inhibitor Inhibition 86.0 94.0 90.0
SU11652 Hs Inhibitor Inhibition 86.3 94.0 63.0
Src kinase inhibitor I Hs Inhibitor Inhibition 87.8 88.0 49.0
dasatinib Hs Inhibitor Inhibition 88.1
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 88.1 83.0 74.0
aloisine Hs Inhibitor Inhibition 88.4 103.0 96.0
SU9516 Hs Inhibitor Inhibition 88.5 112.0 96.0
TWS119 Hs Inhibitor Inhibition 88.5 93.0 49.0
purvalanol A Hs Inhibitor Inhibition 89.1 82.0 51.0
LY 294002 Hs Inhibitor Inhibition 89.2 103.0 93.0
indirubin-3'-monoxime Hs Inhibitor Inhibition 89.4 89.0 60.0
casein kinase II inhibitor III Hs Inhibitor Inhibition 89.8 108.0 94.0
SP600125 Hs Inhibitor Inhibition 89.9 87.0 77.0
JAK inhibitor I Hs Inhibitor Inhibition 90.0 101.0 78.0
aloisine A Hs Inhibitor Inhibition 90.3 104.0 98.0
PKR inhibitor, negative control Hs Inhibitor Inhibition 90.7 100.0 80.0
EGFR/ErbB-2 inhibitor Hs Inhibitor Inhibition 90.8 95.0 64.0
IKK-2 inhibitor IV Hs Inhibitor Inhibition 91.1 81.0 75.0
seliciclib Hs Inhibitor Inhibition 91.2
PP1 analog II Hs Inhibitor Inhibition 91.2 95.0 72.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 91.3 74.0 31.0
midostaurin Hs Inhibitor Inhibition 91.4 91.0 76.0
PI 3-Kg inhibitor II Hs Inhibitor Inhibition 91.5 104.0 98.0
GTP-14564 Hs Inhibitor Inhibition 91.5 112.0 89.0
bosutinib Hs Inhibitor Inhibition 91.8
CGP74514A Hs Inhibitor Inhibition 92.0 87.0 56.0
Gö 6983 Hs Inhibitor Inhibition 92.0 105.0 77.0
JNK inhibitor, negative control Hs Inhibitor Inhibition 92.0 95.0 67.0
Cdk4 inhibitor Hs Inhibitor Inhibition 92.3 85.0 82.0
Tpl2 kinase inhibitor Hs Inhibitor Inhibition 92.4 97.0 87.0
CGP53353 Hs Inhibitor Inhibition 92.7 87.0 46.0
VEGF receptor 2 kinase inhibitor IV Hs Inhibitor Inhibition 92.7 106.0 103.0
VEGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 92.9 97.0 97.0
GSK-3 inhibitor X Hs Inhibitor Inhibition 93.0 101.0 94.0
Gö 6976 Hs Inhibitor Inhibition 93.1 105.0 88.0
H-89 Hs Inhibitor Inhibition 93.1 86.0 92.0
tozasertib Hs Inhibitor Inhibition 93.3
JNK inhibitor VIII Hs Inhibitor Inhibition 93.3 92.0 73.0
LY 303511 Hs Inhibitor Inhibition 93.4 133.0 98.0
p38 MAP kinase inhibitor Hs Inhibitor Inhibition 93.6 89.0 102.0
VEGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 93.8
VEGF receptor 2 kinase inhibitor II Hs Inhibitor Inhibition 93.8 118.0 105.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 93.8 93.0 93.0
PI-103 Hs Inhibitor Inhibition 93.9 119.0 93.0
TGF-beta RI inhibitor III Hs Inhibitor Inhibition 94.1 89.0 89.0
sunitinib Hs Inhibitor Inhibition 94.3
Cdk2 inhibitor III Hs Inhibitor Inhibition 94.6 97.0 93.0
Y27632 Hs Inhibitor Inhibition 94.9 108.0 94.0
MEK1/2 inhibitor Hs Inhibitor Inhibition 94.9 93.0 89.0
AG 490 Hs Inhibitor Inhibition 95.0 106.0 99.0
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibitor Inhibition 95.1 102.0 79.0
SB220025 Hs Inhibitor Inhibition 95.3 95.0 77.0
kenpaullone Hs Inhibitor Inhibition 95.5 88.0 70.0
JAK3 inhibitor II Hs Inhibitor Inhibition 95.7 87.0 77.0
STO609 Hs Inhibitor Inhibition 95.8 111.0 97.0
BPIQ-I Hs Inhibitor Inhibition 95.8 93.0 90.0
dovitinib Hs Inhibitor Inhibition 96.1
AG 9 Hs Inhibitor Inhibition 96.2 102.0 97.0
PD98059 Hs Inhibitor Inhibition 96.3 82.0 100.0
MEK inhibitor II Hs Inhibitor Inhibition 96.4 94.0 95.0
Flt-3 inhibitor Hs Inhibitor Inhibition 96.4 101.0 94.0
compound 56 [PMID: 8568816] Hs Inhibitor Inhibition 96.5 99.0 86.0
SU6656 Hs Inhibitor Inhibition 96.5 100.0 89.0
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 96.5 101.0 89.0
ERK inhibitor III Hs Inhibitor Inhibition 96.6 108.0 85.0
VX-702 Hs Inhibitor Inhibition 96.6
Cdk/Crk inhibitor Hs Inhibitor Inhibition 96.7 113.0 97.0
AGL 2043 Hs Inhibitor Inhibition 96.9 124.0 71.0
JAK3 inhibitor IV Hs Inhibitor Inhibition 97.0 103.0 91.0
PP3 Hs Inhibitor Inhibition 97.2 99.0 92.0
Rho kinase inhibitor IV Hs Inhibitor Inhibition 97.3 103.0 92.0
SB 202474 Hs Inhibitor Inhibition 97.3 87.0 108.0
PD 158780 Hs Inhibitor Inhibition 97.4 101.0 91.0
AG 1296 Hs Inhibitor Inhibition 97.5 126.0 95.0
NU-7026 Hs Inhibitor Inhibition 97.5 103.0 92.0
p38 MAP kinase inhibitor III Hs Inhibitor Inhibition 97.6 96.0 94.0
Chk2 inhibitor II Hs Inhibitor Inhibition 97.6 93.0 86.0
IC261 Hs Inhibitor Inhibition 97.6 93.0 83.0
AG1478 Hs Inhibitor Inhibition 97.8 93.0 87.0
vandetanib Hs Inhibitor Inhibition 98.0
Cdk1/5 inhibitor Hs Inhibitor Inhibition 98.0 103.0 104.0
Syk inhibitor II Hs Inhibitor Inhibition 98.0 85.0 78.0
fasudil Hs Inhibitor Inhibition 98.1 96.0 102.0
DMBI Hs Inhibitor Inhibition 98.1 117.0 90.0
JNJ-7706621 Hs Inhibitor Inhibition 98.3 100.0 80.0
bisindolylmaleimide IV Hs Inhibitor Inhibition 98.3 106.0 89.0
GF109203X Hs Inhibitor Inhibition 98.4 121.0 97.0
mubritinib Hs Inhibitor Inhibition 98.5
MEK inhibitor I Hs Inhibitor Inhibition 98.6 100.0 89.0
pazopanib Hs Inhibitor Inhibition 98.6
SKI II Hs Inhibitor Inhibition 98.7 109.0 91.0
bohemine Hs Inhibitor Inhibition 99.0 105.0 92.0
SB203580 Hs Inhibitor Inhibition 99.0 110.0 100.0
Flt-3 inhibitor III Hs Inhibitor Inhibition 99.0 114.0 100.0
Syk inhibitor Hs Inhibitor Inhibition 99.0 97.0 75.0
vatalanib Hs Inhibitor Inhibition 99.1
Cdk4 inhibitor II Hs Inhibitor Inhibition 99.1 89.0 89.0
JNK inhibitor IX Hs Inhibitor Inhibition 99.2 107.0 84.0
sorafenib Hs Inhibitor Inhibition 99.2
PD 174265 Hs Inhibitor Inhibition 99.3 95.0 80.0
imatinib Hs Inhibitor Inhibition 99.4
herbimycin A Hs Inhibitor Inhibition 99.4 112.0 106.0
KN-93 Hs Inhibitor Inhibition 99.4 100.0 88.0
wortmannin Hs Inhibitor Inhibition 99.5
alsterpaullone Hs Inhibitor Inhibition 99.7 95.0 93.0
AG 112 Hs Inhibitor Inhibition 99.8 96.0 75.0
PQ401 Hs Inhibitor Inhibition 99.9 94.0 78.0
masitinib Hs Inhibitor Inhibition 99.9
EGFR inhibitor Hs Inhibitor Inhibition 100.0 95.0 85.0
Ro-32-0432 Hs Inhibitor Inhibition 100.0
semaxanib Hs Inhibitor Inhibition 100.0 110.0 97.0
PKCbeta inhibitor Hs Inhibitor Inhibition 100.1 91.0 86.0
GW-2580 Hs Inhibitor Inhibition 100.4 108.0 92.0
Rho kinase inhibitor III Hs Inhibitor Inhibition 100.4 98.0 96.0
nilotinib Hs Inhibitor Inhibition 100.4
GSK-3beta inhibitor VIII Hs Inhibitor Inhibition 100.6 88.0 81.0
PDGF RTK inhibitor Hs Inhibitor Inhibition 100.6 82.0 49.0
PDGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 100.7 80.0 58.0
SB202190 Hs Inhibitor Inhibition 100.8 109.0 75.0
GSK-3beta inhibitor I Hs Inhibitor Inhibition 100.9 99.0 79.0
PDGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 101.1 102.0 85.0
chelerythrine Hs Inhibitor Inhibition 101.1 117.0 84.0
KN-62 Hs Inhibitor Inhibition 101.2 100.0 99.0
ERK inhibitor II Hs Inhibitor Inhibition 101.3 83.0 86.0
D4476 Hs Inhibitor Inhibition 101.3 123.0 98.0
Cdk1 inhibitor Hs Inhibitor Inhibition 101.3 95.0 64.0
GSK-3beta inhibitor II Hs Inhibitor Inhibition 101.4 89.0 89.0
erlotinib Hs Inhibitor Inhibition 101.5
triciribine Hs Inhibitor Inhibition 101.5 105.0 100.0
Cdk4 inhibitor III Hs Inhibitor Inhibition 101.5 80.0 95.0
PD 169316 Hs Inhibitor Inhibition 101.7 92.0 98.0
purvalanol A Hs Inhibitor Inhibition 102.0 82.0 51.0
tandutinib Hs Inhibitor Inhibition 102.0
Syk inhibitor III Hs Inhibitor Inhibition 102.1 88.0 94.0
gefitinib Hs Inhibitor Inhibition 102.1
fascaplysin Hs Inhibitor Inhibition 102.4 91.0 93.0
AG 1295 Hs Inhibitor Inhibition 103.1 96.0 92.0
MNK1 inhibitor Hs Inhibitor Inhibition 103.4 101.0 87.0
tofacitinib Hs Inhibitor Inhibition 103.9
lapatinib Hs Inhibitor Inhibition 103.9
DNA-PK inhibitor III Hs Inhibitor Inhibition 104.0 104.0 104.0
DNA-PK inhibitor V Hs Inhibitor Inhibition 104.1 112.0 97.0
PDGF receptor tyrosine kinase inhibitor IV Hs Inhibitor Inhibition 104.2 85.0 59.0
VEGF receptor 2 kinase inhibitor I Hs Inhibitor Inhibition 104.4 93.0 92.0
aurora kinase inhibitor III Hs Inhibitor Inhibition 104.6 104.5 63.0
Bcr-abl inhibitor GNF-2 Hs Inhibitor Inhibition 104.7 123.0 109.0
SKF-86002 Hs Inhibitor Inhibition 105.1 107.0 104.0
Akt inhibitor VIII Hs Inhibitor Inhibition 105.6 116.0 85.0
SC-68376 Hs Inhibitor Inhibition 105.9 104.0 100.0
AG 1024 Hs Inhibitor Inhibition 106.2 111.0 105.0
diacylglycerol kinase inhibitor II Hs Inhibitor Inhibition 107.0 116.0 102.0
Akt inhibitor X Hs Inhibitor Inhibition 107.5 126.0 104.0
ATM/ATR kinase inhibitor Hs Inhibitor Inhibition 108.2 104.0 106.0
KU-55933 Hs Inhibitor Inhibition 108.8 95.0 87.0
MK2a inhibitor Hs Inhibitor Inhibition 109.2 94.0 91.0
BAY 11-7082 Hs Inhibitor Inhibition 110.4 98.0 98.0
NF-kB activation inhibitor Hs Inhibitor Inhibition 114.2 102.0 87.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 116.1 115.0 103.0
TGF-beta RI kinase inhibitor Hs Inhibitor Inhibition 97.0 91.0
SU11274 Hs Inhibitor Inhibition 111.0 95.0

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]