TXK tyrosine kinase (Tec 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: Txk/TXK
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
dasatinib Hs Inhibitor Inhibition 1.4
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibitor Inhibition 1.7 52.0 14.0
Gö 6976 Hs Inhibitor Inhibition 6.4 8.0 8.0
staurosporine Hs Inhibitor Inhibition 7.3 22.5 4.0
Lck inhibitor Hs Inhibitor Inhibition 17.3 18.0 1.0
SB 218078 Hs Inhibitor Inhibition 22.7 71.0 81.0
K-252a Hs Inhibitor Inhibition 24.4 35.0 5.0
TWS119 Hs Inhibitor Inhibition 24.5 27.0 3.0
indirubin derivative E804 Hs Inhibitor Inhibition 25.6 31.0 3.0
bosutinib Hs Inhibitor Inhibition 27.5
GSK-3 inhibitor IX Hs Inhibitor Inhibition 27.7 13.0 23.0
PP1 analog II Hs Inhibitor Inhibition 28.6 43.0 7.0
pazopanib Hs Inhibitor Inhibition 40.2
PD 169316 Hs Inhibitor Inhibition 42.1 61.0 66.0
aminopurvalanol A Hs Inhibitor Inhibition 42.5 63.0 17.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 45.3 30.0 2.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 46.0 49.0 5.0
GSK-3 inhibitor X Hs Inhibitor Inhibition 46.4 74.0 19.0
JNK inhibitor V Hs Inhibitor Inhibition 49.3 75.0 20.0
Syk inhibitor Hs Inhibitor Inhibition 51.3 75.0 47.0
purvalanol A Hs Inhibitor Inhibition 54.1 66.0 16.0
dorsomorphin Hs Inhibitor Inhibition 54.4 44.0 7.0
vandetanib Hs Inhibitor Inhibition 57.5
PDGF receptor tyrosine kinase inhibitor IV Hs Inhibitor Inhibition 60.6 64.0 20.0
IKK-2 inhibitor IV Hs Inhibitor Inhibition 62.4 49.0 12.0
SB203580 Hs Inhibitor Inhibition 63.9 77.0 42.0
aloisine A Hs Inhibitor Inhibition 65.0 47.0 14.0
indirubin-3'-monoxime Hs Inhibitor Inhibition 66.7 45.0 11.0
PDGF RTK inhibitor Hs Inhibitor Inhibition 66.9 88.0 37.0
MNK1 inhibitor Hs Inhibitor Inhibition 67.6 66.0 18.0
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 67.6 26.0 9.0
CGP74514A Hs Inhibitor Inhibition 69.1 52.0 10.0
PKR inhibitor Hs Inhibitor Inhibition 70.1 82.0 30.0
midostaurin Hs Inhibitor Inhibition 71.7 82.0 69.0
aloisine Hs Inhibitor Inhibition 72.7 53.0 55.0
SP600125 Hs Inhibitor Inhibition 73.4 58.0 23.0
Flt-3 inhibitor II Hs Inhibitor Inhibition 74.9 64.0 22.0
AG1478 Hs Inhibitor Inhibition 75.0 87.0 49.0
dovitinib Hs Inhibitor Inhibition 75.1
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 75.3 30.0 2.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 75.7 53.0 12.0
isogranulatimide Hs Inhibitor Inhibition 76.4 71.0 79.0
JAK inhibitor I Hs Inhibitor Inhibition 77.1 63.0 57.0
Src kinase inhibitor I Hs Inhibitor Inhibition 78.0 56.0 34.0
compound 52 [PMID: 9677190] Hs Inhibitor Inhibition 78.1 68.0 37.0
SB202190 Hs Inhibitor Inhibition 78.5 78.0 43.0
tozasertib Hs Inhibitor Inhibition 78.8
SU11652 Hs Inhibitor Inhibition 79.5 70.0 21.0
PD 158780 Hs Inhibitor Inhibition 79.9 98.0 64.0
compound 56 [PMID: 8568816] Hs Inhibitor Inhibition 80.2 75.0 24.0
GTP-14564 Hs Inhibitor Inhibition 81.5 97.0 73.0
kenpaullone Hs Inhibitor Inhibition 82.6 73.0 18.0
Gö 6983 Hs Inhibitor Inhibition 82.8 84.0 73.0
gefitinib Hs Inhibitor Inhibition 83.2
JAK3 inhibitor II Hs Inhibitor Inhibition 83.3 81.0 46.0
CGP53353 Hs Inhibitor Inhibition 84.1 79.0 27.0
fasudil Hs Inhibitor Inhibition 84.1 91.0 87.0
Syk inhibitor II Hs Inhibitor Inhibition 85.2 94.0 61.0
VEGF receptor 2 kinase inhibitor IV Hs Inhibitor Inhibition 85.2 70.0 83.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 85.8 71.0 32.0
PKR inhibitor, negative control Hs Inhibitor Inhibition 86.6 93.0 80.0
BPIQ-I Hs Inhibitor Inhibition 86.7 89.0 60.0
H-89 Hs Inhibitor Inhibition 86.8 74.0 61.0
alsterpaullone Hs Inhibitor Inhibition 87.3 49.0 39.0
Tpl2 kinase inhibitor Hs Inhibitor Inhibition 88.1 86.0 69.0
erlotinib Hs Inhibitor Inhibition 88.5
ERK inhibitor II Hs Inhibitor Inhibition 88.8 77.0 60.0
TGF-beta RI kinase inhibitor Hs Inhibitor Inhibition 89.1 113.0 64.0
aurora kinase inhibitor III Hs Inhibitor Inhibition 90.2 53.0 27.0
Cdk4 inhibitor Hs Inhibitor Inhibition 90.3 89.0 72.0
PD 174265 Hs Inhibitor Inhibition 90.5 108.0 78.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 90.8 103.0 73.0
Flt-3 inhibitor III Hs Inhibitor Inhibition 91.1 95.0 60.0
JNK inhibitor, negative control Hs Inhibitor Inhibition 92.0 82.0 61.0
MEK inhibitor I Hs Inhibitor Inhibition 92.2 87.0 66.0
sunitinib Hs Inhibitor Inhibition 92.6
IRAK-1/4 inhibitor Hs Inhibitor Inhibition 92.9 104.0 77.0
JNK inhibitor VIII Hs Inhibitor Inhibition 93.0 79.0 76.0
p38 MAP kinase inhibitor III Hs Inhibitor Inhibition 93.1 86.0 86.0
semaxanib Hs Inhibitor Inhibition 93.4 103.0 92.0
AG 1296 Hs Inhibitor Inhibition 93.4 96.0 73.0
SU9516 Hs Inhibitor Inhibition 93.5 77.0 46.0
LY 294002 Hs Inhibitor Inhibition 93.6 82.0 69.0
KN-62 Hs Inhibitor Inhibition 94.3 98.0 102.0
p38 MAP kinase inhibitor Hs Inhibitor Inhibition 94.4 84.0 90.0
PD98059 Hs Inhibitor Inhibition 94.6 77.0 73.0
PI-103 Hs Inhibitor Inhibition 94.8 93.0 92.0
PP3 Hs Inhibitor Inhibition 94.8 108.0 78.0
PKCbeta inhibitor Hs Inhibitor Inhibition 95.3 117.0 91.0
PI 3-Kg inhibitor II Hs Inhibitor Inhibition 95.4 109.0 104.0
LY 303511 Hs Inhibitor Inhibition 95.4 113.0 98.0
MEK inhibitor II Hs Inhibitor Inhibition 95.5 76.0 87.0
KN-93 Hs Inhibitor Inhibition 95.6 94.0 67.0
JNJ-7706621 Hs Inhibitor Inhibition 95.8 91.0 41.0
SU6656 Hs Inhibitor Inhibition 96.0 92.0 90.0
VEGF receptor 2 kinase inhibitor I Hs Inhibitor Inhibition 96.1 97.0 91.0
DMBI Hs Inhibitor Inhibition 96.1 108.0 69.0
Flt-3 inhibitor Hs Inhibitor Inhibition 96.2 93.0 73.0
PI 3-Kg inhibitor Hs Inhibitor Inhibition 96.8 100.0 93.0
GSK-3beta inhibitor II Hs Inhibitor Inhibition 96.8 75.0 81.0
GSK-3beta inhibitor VIII Hs Inhibitor Inhibition 96.9 67.0 74.0
JNK inhibitor IX Hs Inhibitor Inhibition 97.0 90.0 80.0
EGFR inhibitor Hs Inhibitor Inhibition 97.1 109.0 69.0
JAK3 inhibitor IV Hs Inhibitor Inhibition 97.1 92.0 42.0
VEGF receptor 2 kinase inhibitor II Hs Inhibitor Inhibition 97.3 107.0 76.0
Cdk1/5 inhibitor Hs Inhibitor Inhibition 97.6 87.0 76.0
MK2a inhibitor Hs Inhibitor Inhibition 97.7 99.0 89.0
VEGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 97.7 88.0 78.0
herbimycin A Hs Inhibitor Inhibition 98.1 89.0 103.0
ERK inhibitor III Hs Inhibitor Inhibition 98.3 104.0 80.0
tofacitinib Hs Inhibitor Inhibition 98.4
DNA-PK inhibitor V Hs Inhibitor Inhibition 98.5 82.0 70.0
MEK1/2 inhibitor Hs Inhibitor Inhibition 98.7 74.0 86.0
casein kinase II inhibitor III Hs Inhibitor Inhibition 98.7 94.0 95.0
Cdk4 inhibitor III Hs Inhibitor Inhibition 98.8 80.0 83.0
SKF-86002 Hs Inhibitor Inhibition 98.9 93.0 97.0
PQ401 Hs Inhibitor Inhibition 98.9 103.0 60.0
NU-7026 Hs Inhibitor Inhibition 98.9 90.0 85.0
Y27632 Hs Inhibitor Inhibition 98.9 85.0 39.0
wortmannin Hs Inhibitor Inhibition 99.0
PDGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 99.1 102.0 82.0
SB220025 Hs Inhibitor Inhibition 99.1 83.0 64.0
D4476 Hs Inhibitor Inhibition 99.2 90.0 94.0
IC261 Hs Inhibitor Inhibition 99.2 107.0 100.0
PDGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 99.3 108.0 119.0
SC-68376 Hs Inhibitor Inhibition 99.4 86.0 88.0
EGFR/ErbB-2 inhibitor Hs Inhibitor Inhibition 99.4 97.0 57.0
AG 1295 Hs Inhibitor Inhibition 99.5 90.0 84.0
Cdk1 inhibitor Hs Inhibitor Inhibition 99.6 83.0 74.0
fascaplysin Hs Inhibitor Inhibition 99.7 75.0 75.0
GSK-3beta inhibitor I Hs Inhibitor Inhibition 99.8 83.0 88.0
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 100.0 81.0 77.0
AG 112 Hs Inhibitor Inhibition 100.1 78.0 67.0
chelerythrine Hs Inhibitor Inhibition 100.1 94.0 59.0
diacylglycerol kinase inhibitor II Hs Inhibitor Inhibition 100.1 102.0 80.0
SB 202474 Hs Inhibitor Inhibition 100.1 100.0 87.0
TGF-beta RI inhibitor III Hs Inhibitor Inhibition 100.2 114.0 98.0
Chk2 inhibitor II Hs Inhibitor Inhibition 100.4 96.0 92.0
SKI II Hs Inhibitor Inhibition 100.5 97.0 79.0
Akt inhibitor X Hs Inhibitor Inhibition 100.6 99.0 81.0
Cdk4 inhibitor II Hs Inhibitor Inhibition 100.6 84.0 86.0
Cdk2 inhibitor III Hs Inhibitor Inhibition 100.7 87.0 89.0
VEGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 100.7
mubritinib Hs Inhibitor Inhibition 100.7
Cdk/Crk inhibitor Hs Inhibitor Inhibition 100.8 96.0 99.0
GW-2580 Hs Inhibitor Inhibition 101.0 83.0 68.0
bisindolylmaleimide IV Hs Inhibitor Inhibition 101.2 112.0 91.0
masitinib Hs Inhibitor Inhibition 101.3
AG 9 Hs Inhibitor Inhibition 101.5 100.0 99.0
bohemine Hs Inhibitor Inhibition 101.7 75.0 74.0
SU11274 Hs Inhibitor Inhibition 101.8 111.0 99.0
Syk inhibitor III Hs Inhibitor Inhibition 101.9 76.0 77.0
STO609 Hs Inhibitor Inhibition 101.9 77.0 60.0
AGL 2043 Hs Inhibitor Inhibition 102.4 108.0 75.0
NF-kB activation inhibitor Hs Inhibitor Inhibition 102.4 80.0 61.0
DNA-PK inhibitor III Hs Inhibitor Inhibition 102.6 85.0 86.0
BAY 11-7082 Hs Inhibitor Inhibition 103.0 79.0 87.0
Rho kinase inhibitor IV Hs Inhibitor Inhibition 103.1 100.0 91.0
Ro-32-0432 Hs Inhibitor Inhibition 103.1
nilotinib Hs Inhibitor Inhibition 103.6
AG 490 Hs Inhibitor Inhibition 103.7 99.0 86.0
VX-702 Hs Inhibitor Inhibition 103.7
Akt inhibitor VIII Hs Inhibitor Inhibition 104.0 102.0 94.0
Rho kinase inhibitor III Hs Inhibitor Inhibition 104.2 109.0 97.0
purvalanol A Hs Inhibitor Inhibition 104.7 66.0 16.0
tandutinib Hs Inhibitor Inhibition 105.2
sorafenib Hs Inhibitor Inhibition 105.7
KU-55933 Hs Inhibitor Inhibition 105.9 91.0 91.0
seliciclib Hs Inhibitor Inhibition 106.4
GF109203X Hs Inhibitor Inhibition 106.5 97.0 79.0
triciribine Hs Inhibitor Inhibition 106.7 83.0 83.0
Akt inhibitor IV Hs Inhibitor Inhibition 107.1 83.0 51.0
AG 1024 Hs Inhibitor Inhibition 107.6 112.0 104.0
ATM/ATR kinase inhibitor Hs Inhibitor Inhibition 107.9 82.0 76.0
imatinib Hs Inhibitor Inhibition 108.0
lapatinib Hs Inhibitor Inhibition 109.7
vatalanib Hs Inhibitor Inhibition 110.3
Bcr-abl inhibitor GNF-2 Hs Inhibitor Inhibition 110.7 101.0 101.0

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]