maternal embryonic leucine zipper kinase (MELK subfamily)

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: MELK/MELK
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 1.0 1.0 -1.5
K-252a Hs Inhibitor Inhibition 1.2 1.0 -1.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 4.6 4.0 1.0
PKR inhibitor Hs Inhibitor Inhibition 4.7 6.0 1.0
midostaurin Hs Inhibitor Inhibition 4.9 5.0 2.0
JAK inhibitor I Hs Inhibitor Inhibition 5.2 2.0 2.0
dorsomorphin Hs Inhibitor Inhibition 6.6 5.0 -1.0
SB 218078 Hs Inhibitor Inhibition 7.1 55.0 72.0
dovitinib Hs Inhibitor Inhibition 7.7
sunitinib Hs Inhibitor Inhibition 10.4
indirubin derivative E804 Hs Inhibitor Inhibition 13.1 7.0 5.0
SU11652 Hs Inhibitor Inhibition 16.7 8.0 3.0
Gö 6976 Hs Inhibitor Inhibition 21.1 9.0 4.0
SP600125 Hs Inhibitor Inhibition 21.6 13.0 0.0
bosutinib Hs Inhibitor Inhibition 25.8
isogranulatimide Hs Inhibitor Inhibition 32.6 27.0 10.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 32.7 17.0 24.0
indirubin-3'-monoxime Hs Inhibitor Inhibition 33.3 15.0 7.0
SU9516 Hs Inhibitor Inhibition 36.5 24.0 3.0
GF109203X Hs Inhibitor Inhibition 42.0 41.0 13.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 43.5 34.0 48.0
Flt-3 inhibitor Hs Inhibitor Inhibition 46.0 78.0 78.0
Cdk4 inhibitor Hs Inhibitor Inhibition 46.6 87.0 82.0
Flt-3 inhibitor II Hs Inhibitor Inhibition 49.2 27.0 3.0
aminopurvalanol A Hs Inhibitor Inhibition 51.5 67.0 16.0
tozasertib Hs Inhibitor Inhibition 53.4
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 55.7 67.0 33.0
compound 52 [PMID: 9677190] Hs Inhibitor Inhibition 59.7 56.0 16.0
Syk inhibitor Hs Inhibitor Inhibition 63.0 42.0 51.0
fascaplysin Hs Inhibitor Inhibition 68.5 85.0 67.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 69.1 46.0 7.0
purvalanol A Hs Inhibitor Inhibition 69.5 66.0 18.0
Gö 6983 Hs Inhibitor Inhibition 70.7 54.0 26.0
alsterpaullone Hs Inhibitor Inhibition 71.7 81.0 64.0
PDGF receptor tyrosine kinase inhibitor IV Hs Inhibitor Inhibition 72.1 47.0 11.0
Cdk2 inhibitor III Hs Inhibitor Inhibition 72.3 77.0 38.0
VEGF receptor 2 kinase inhibitor IV Hs Inhibitor Inhibition 73.6 80.0 87.0
kenpaullone Hs Inhibitor Inhibition 74.8 89.0 68.0
H-89 Hs Inhibitor Inhibition 75.1 45.0 9.0
PI-103 Hs Inhibitor Inhibition 75.5 74.0 88.0
VEGF receptor 2 kinase inhibitor II Hs Inhibitor Inhibition 75.6 78.0 92.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 76.3 40.0 3.0
CGP74514A Hs Inhibitor Inhibition 77.0 59.0 18.0
GTP-14564 Hs Inhibitor Inhibition 77.0 43.0 7.0
gefitinib Hs Inhibitor Inhibition 77.7
semaxanib Hs Inhibitor Inhibition 77.9 56.0 34.0
fasudil Hs Inhibitor Inhibition 78.6 75.0 16.0
SU11274 Hs Inhibitor Inhibition 78.9 71.0 59.0
tofacitinib Hs Inhibitor Inhibition 79.4
IRAK-1/4 inhibitor Hs Inhibitor Inhibition 80.4 65.0 45.0
IKK-2 inhibitor IV Hs Inhibitor Inhibition 81.1 72.0 24.0
dasatinib Hs Inhibitor Inhibition 81.4
AG1478 Hs Inhibitor Inhibition 81.8 89.0 59.0
bisindolylmaleimide IV Hs Inhibitor Inhibition 82.0 80.0 27.0
aloisine A Hs Inhibitor Inhibition 82.5 76.0 72.0
Rho kinase inhibitor IV Hs Inhibitor Inhibition 83.0 74.0 24.0
JNK inhibitor IX Hs Inhibitor Inhibition 83.3 87.0 91.0
JAK3 inhibitor II Hs Inhibitor Inhibition 83.4 73.0 28.0
Flt-3 inhibitor III Hs Inhibitor Inhibition 83.5 64.0 20.0
JNK inhibitor, negative control Hs Inhibitor Inhibition 83.6 67.0 59.0
PKR inhibitor, negative control Hs Inhibitor Inhibition 83.6 60.0 46.0
vatalanib Hs Inhibitor Inhibition 83.7
Cdk/Crk inhibitor Hs Inhibitor Inhibition 84.0 65.0 67.0
IC261 Hs Inhibitor Inhibition 84.2 104.0 77.0
aloisine Hs Inhibitor Inhibition 84.4 74.0 75.0
seliciclib Hs Inhibitor Inhibition 84.7
masitinib Hs Inhibitor Inhibition 84.8
mubritinib Hs Inhibitor Inhibition 85.4
Cdk1 inhibitor Hs Inhibitor Inhibition 85.7 77.0 30.0
p38 MAP kinase inhibitor Hs Inhibitor Inhibition 86.5 104.0 92.0
VEGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 86.8
VX-702 Hs Inhibitor Inhibition 87.1
JNJ-7706621 Hs Inhibitor Inhibition 87.2 83.0 24.0
VEGF receptor 2 kinase inhibitor I Hs Inhibitor Inhibition 87.4 77.0 97.0
pazopanib Hs Inhibitor Inhibition 87.5
tandutinib Hs Inhibitor Inhibition 87.9
Tpl2 kinase inhibitor Hs Inhibitor Inhibition 88.0 2.0 0.0
compound 56 [PMID: 8568816] Hs Inhibitor Inhibition 88.1 91.0 62.0
lapatinib Hs Inhibitor Inhibition 88.5
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 88.6 69.0 52.0
erlotinib Hs Inhibitor Inhibition 88.6
AG 1296 Hs Inhibitor Inhibition 88.9 69.0 60.0
BPIQ-I Hs Inhibitor Inhibition 89.0 92.0 103.0
SU6656 Hs Inhibitor Inhibition 89.1 105.0 95.0
imatinib Hs Inhibitor Inhibition 89.2
DMBI Hs Inhibitor Inhibition 89.3 49.0 26.0
chelerythrine Hs Inhibitor Inhibition 89.6 84.0 31.0
nilotinib Hs Inhibitor Inhibition 90.0
PI 3-Kg inhibitor Hs Inhibitor Inhibition 90.7 64.0 31.0
PP1 analog II Hs Inhibitor Inhibition 90.7 72.0 30.0
casein kinase II inhibitor III Hs Inhibitor Inhibition 91.0 82.0 80.0
AG 1295 Hs Inhibitor Inhibition 91.1 72.0 77.0
LY 294002 Hs Inhibitor Inhibition 91.3 91.0 72.0
AG 1024 Hs Inhibitor Inhibition 91.6 91.0 89.0
PD 158780 Hs Inhibitor Inhibition 91.6 109.0 112.0
JNK inhibitor V Hs Inhibitor Inhibition 91.7 74.0 50.0
BAY 11-7082 Hs Inhibitor Inhibition 92.0 96.0 100.0
CGP53353 Hs Inhibitor Inhibition 92.0 89.0 76.0
VEGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 92.3 75.0 86.0
wortmannin Hs Inhibitor Inhibition 92.4
PP3 Hs Inhibitor Inhibition 92.6 95.0 73.0
TGF-beta RI inhibitor III Hs Inhibitor Inhibition 92.7 75.0 103.0
Cdk1/5 inhibitor Hs Inhibitor Inhibition 92.9 97.0 70.0
bohemine Hs Inhibitor Inhibition 93.0 86.0 77.0
Cdk4 inhibitor III Hs Inhibitor Inhibition 93.2 95.0 85.0
TGF-beta RI kinase inhibitor Hs Inhibitor Inhibition 93.3 97.0 82.0
Akt inhibitor IV Hs Inhibitor Inhibition 93.4 91.0 46.0
TWS119 Hs Inhibitor Inhibition 93.4 73.0 29.0
PD 174265 Hs Inhibitor Inhibition 93.4 90.0 96.0
sorafenib Hs Inhibitor Inhibition 93.6
GSK-3 inhibitor X Hs Inhibitor Inhibition 93.9 69.0 52.0
PD98059 Hs Inhibitor Inhibition 94.0 109.0 113.0
KN-62 Hs Inhibitor Inhibition 94.0 94.0 91.0
p38 MAP kinase inhibitor III Hs Inhibitor Inhibition 94.2 88.0 61.0
PI 3-Kg inhibitor II Hs Inhibitor Inhibition 94.4 114.0 82.0
vandetanib Hs Inhibitor Inhibition 94.4
Bcr-abl inhibitor GNF-2 Hs Inhibitor Inhibition 94.5 74.0 75.0
LY 303511 Hs Inhibitor Inhibition 94.5 80.0 78.0
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 94.6 84.0 48.0
PDGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 94.9 81.0 101.0
Y27632 Hs Inhibitor Inhibition 95.0 104.0 106.0
D4476 Hs Inhibitor Inhibition 95.0 73.0 70.0
Akt inhibitor X Hs Inhibitor Inhibition 95.3 96.0 105.0
MK2a inhibitor Hs Inhibitor Inhibition 95.5 100.0 77.0
AGL 2043 Hs Inhibitor Inhibition 95.6 89.0 67.0
Syk inhibitor II Hs Inhibitor Inhibition 95.8 83.0 49.0
Syk inhibitor III Hs Inhibitor Inhibition 95.9 78.0 84.0
MEK1/2 inhibitor Hs Inhibitor Inhibition 96.1 67.0 62.0
Chk2 inhibitor II Hs Inhibitor Inhibition 96.2 91.0 83.0
Ro-32-0432 Hs Inhibitor Inhibition 96.4
PD 169316 Hs Inhibitor Inhibition 96.4 97.0 87.0
PDGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 96.4 88.0 87.0
MEK inhibitor II Hs Inhibitor Inhibition 96.4 104.0 70.0
Cdk4 inhibitor II Hs Inhibitor Inhibition 96.6 102.0 84.0
NF-kB activation inhibitor Hs Inhibitor Inhibition 96.8 63.0 40.0
MEK inhibitor I Hs Inhibitor Inhibition 97.0 94.0 83.0
STO609 Hs Inhibitor Inhibition 97.0 91.0 53.0
JNK inhibitor VIII Hs Inhibitor Inhibition 97.1 96.0 101.0
GSK-3beta inhibitor II Hs Inhibitor Inhibition 97.7 24.0 13.0
MNK1 inhibitor Hs Inhibitor Inhibition 97.7 89.0 51.0
purvalanol A Hs Inhibitor Inhibition 97.8 66.0 18.0
herbimycin A Hs Inhibitor Inhibition 97.9 60.0 63.0
PDGF RTK inhibitor Hs Inhibitor Inhibition 98.5 98.0 84.0
AG 9 Hs Inhibitor Inhibition 98.6 98.0 86.0
GSK-3beta inhibitor VIII Hs Inhibitor Inhibition 99.0 99.0 93.0
GSK-3beta inhibitor I Hs Inhibitor Inhibition 99.3 88.0 65.0
JAK3 inhibitor IV Hs Inhibitor Inhibition 99.4 75.0 87.0
KN-93 Hs Inhibitor Inhibition 99.4 90.0 63.0
KU-55933 Hs Inhibitor Inhibition 99.9 93.0 90.0
SB220025 Hs Inhibitor Inhibition 100.0 71.0 27.0
AG 490 Hs Inhibitor Inhibition 100.3 80.0 72.0
SKI II Hs Inhibitor Inhibition 100.4 114.0 100.0
PKCbeta inhibitor Hs Inhibitor Inhibition 100.6 89.0 75.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 100.7 46.0 7.0
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibitor Inhibition 100.8 76.0 99.0
Lck inhibitor Hs Inhibitor Inhibition 100.9 72.0 31.0
AG 112 Hs Inhibitor Inhibition 101.0 70.0 78.0
aurora kinase inhibitor III Hs Inhibitor Inhibition 101.1 67.5 69.5
Src kinase inhibitor I Hs Inhibitor Inhibition 101.3 76.0 129.0
ERK inhibitor II Hs Inhibitor Inhibition 101.6 91.0 97.0
SB203580 Hs Inhibitor Inhibition 101.6 107.0 84.0
SKF-86002 Hs Inhibitor Inhibition 101.7 89.0 82.0
SB202190 Hs Inhibitor Inhibition 101.8 92.0 46.0
ATM/ATR kinase inhibitor Hs Inhibitor Inhibition 101.8 76.0 76.0
GW-2580 Hs Inhibitor Inhibition 101.9 89.0 80.0
Rho kinase inhibitor III Hs Inhibitor Inhibition 102.0 91.0 76.0
ERK inhibitor III Hs Inhibitor Inhibition 102.3 92.0 85.0
EGFR/ErbB-2 inhibitor Hs Inhibitor Inhibition 102.3 79.0 77.0
DNA-PK inhibitor III Hs Inhibitor Inhibition 102.5 90.0 100.0
DNA-PK inhibitor V Hs Inhibitor Inhibition 102.6 85.0 65.0
NU-7026 Hs Inhibitor Inhibition 103.4 92.0 91.0
diacylglycerol kinase inhibitor II Hs Inhibitor Inhibition 103.8 86.0 86.0
EGFR inhibitor Hs Inhibitor Inhibition 104.4 89.0 89.0
SC-68376 Hs Inhibitor Inhibition 104.7 104.0 89.0
triciribine Hs Inhibitor Inhibition 105.3 91.0 95.0
PQ401 Hs Inhibitor Inhibition 106.0 88.0 89.0
Akt inhibitor VIII Hs Inhibitor Inhibition 109.6 94.0 65.0
SB 202474 Hs Inhibitor Inhibition 110.3 85.0 65.0

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]