mitogen-activated protein kinase 14 (p38 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: SAPK2a/P38a(MAPK14)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
VX-702 Hs Inhibitor Inhibition 5.2
SB202190 Hs Inhibitor Inhibition 7.4 1.0 1.0
p38 MAP kinase inhibitor III Hs Inhibitor Inhibition 7.6 -1.0 0.0
PD 169316 Hs Inhibitor Inhibition 7.8 1.0 2.0
p38 MAP kinase inhibitor Hs Inhibitor Inhibition 11.2 3.0 0.0
SB220025 Hs Inhibitor Inhibition 13.1 2.0 1.0
SB203580 Hs Inhibitor Inhibition 22.8 5.0 2.0
nilotinib Hs Inhibitor Inhibition 23.3
dasatinib Hs Inhibitor Inhibition 36.5
sorafenib Hs Inhibitor Inhibition 40.2
SKF-86002 Hs Inhibitor Inhibition 43.1 16.0 3.0
PP1 analog II Hs Inhibitor Inhibition 63.3 41.0 7.0
PKR inhibitor, negative control Hs Inhibitor Inhibition 74.6 54.0 10.0
gefitinib Hs Inhibitor Inhibition 74.6
PD98059 Hs Inhibitor Inhibition 76.2 86.0 94.0
SC-68376 Hs Inhibitor Inhibition 76.3 57.0 14.0
Lck inhibitor Hs Inhibitor Inhibition 76.3 86.0 63.0
MNK1 inhibitor Hs Inhibitor Inhibition 79.5 78.0 47.0
PDGF RTK inhibitor Hs Inhibitor Inhibition 80.2 82.0 68.0
PDGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 81.0 78.0 79.0
PD 174265 Hs Inhibitor Inhibition 82.8 78.0 50.0
LY 303511 Hs Inhibitor Inhibition 82.8 101.0 98.0
SU11274 Hs Inhibitor Inhibition 86.2 94.0 95.0
PI 3-Kg inhibitor II Hs Inhibitor Inhibition 86.7 99.0 109.0
MEK inhibitor I Hs Inhibitor Inhibition 86.9 85.0 53.0
JAK3 inhibitor II Hs Inhibitor Inhibition 87.3 51.0 14.0
compound 56 [PMID: 8568816] Hs Inhibitor Inhibition 87.5 57.0 13.0
LY 294002 Hs Inhibitor Inhibition 87.7 90.0 95.0
MEK inhibitor II Hs Inhibitor Inhibition 88.1 86.0 92.0
PKCbeta inhibitor Hs Inhibitor Inhibition 88.3 62.0 78.0
CGP53353 Hs Inhibitor Inhibition 88.3 57.0 23.0
bosutinib Hs Inhibitor Inhibition 88.6
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 88.6 111.0 112.0
MK2a inhibitor Hs Inhibitor Inhibition 89.0 91.0 59.0
JNK inhibitor V Hs Inhibitor Inhibition 89.1 76.0 41.0
PP3 Hs Inhibitor Inhibition 89.2 83.0 103.0
TGF-beta RI inhibitor III Hs Inhibitor Inhibition 89.7 49.0 16.0
PD 158780 Hs Inhibitor Inhibition 90.0 83.0 77.0
ERK inhibitor III Hs Inhibitor Inhibition 90.2 81.0 91.0
fascaplysin Hs Inhibitor Inhibition 90.2 87.0 85.0
Cdk4 inhibitor Hs Inhibitor Inhibition 90.6 93.0 85.0
GF109203X Hs Inhibitor Inhibition 90.7 109.0 106.0
compound 52 [PMID: 9677190] Hs Inhibitor Inhibition 90.7 84.0 74.0
KN-62 Hs Inhibitor Inhibition 91.0 107.0 109.0
pazopanib Hs Inhibitor Inhibition 91.2
aurora kinase inhibitor III Hs Inhibitor Inhibition 91.5 75.0 59.0
vandetanib Hs Inhibitor Inhibition 91.8
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 91.8 100.0 98.0
D4476 Hs Inhibitor Inhibition 91.9 77.0 37.0
Bcr-abl inhibitor GNF-2 Hs Inhibitor Inhibition 92.0 106.0 107.0
K-252a Hs Inhibitor Inhibition 92.1 92.0 67.0
alsterpaullone Hs Inhibitor Inhibition 92.1 99.0 100.0
dorsomorphin Hs Inhibitor Inhibition 92.2 96.0 89.0
DMBI Hs Inhibitor Inhibition 92.4 102.0 106.0
Cdk4 inhibitor III Hs Inhibitor Inhibition 92.4 97.0 93.0
PI 3-Kg inhibitor Hs Inhibitor Inhibition 92.9 82.0 91.0
kenpaullone Hs Inhibitor Inhibition 93.0 90.0 84.0
tofacitinib Hs Inhibitor Inhibition 93.4
JAK inhibitor I Hs Inhibitor Inhibition 93.5 73.0 69.0
Gö 6976 Hs Inhibitor Inhibition 93.5 84.0 88.0
JNK inhibitor, negative control Hs Inhibitor Inhibition 93.6 91.0 90.0
BPIQ-I Hs Inhibitor Inhibition 93.6 64.0 25.0
midostaurin Hs Inhibitor Inhibition 93.7 71.0 78.0
PKR inhibitor Hs Inhibitor Inhibition 93.9 80.0 74.0
JNK inhibitor VIII Hs Inhibitor Inhibition 93.9 98.0 84.0
herbimycin A Hs Inhibitor Inhibition 93.9 95.0 106.0
dovitinib Hs Inhibitor Inhibition 94.0
tandutinib Hs Inhibitor Inhibition 94.1
chelerythrine Hs Inhibitor Inhibition 94.1 106.0 115.0
PDGF receptor tyrosine kinase inhibitor IV Hs Inhibitor Inhibition 94.3 69.0 44.0
JAK3 inhibitor IV Hs Inhibitor Inhibition 94.4 81.0 79.0
ERK inhibitor II Hs Inhibitor Inhibition 94.6 78.0 33.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 94.7 87.0 70.0
Chk2 inhibitor II Hs Inhibitor Inhibition 94.9 90.0 84.0
Akt inhibitor IV Hs Inhibitor Inhibition 94.9 111.0 73.0
KN-93 Hs Inhibitor Inhibition 95.1 93.0 96.0
erlotinib Hs Inhibitor Inhibition 95.3
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 95.4 89.0 81.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 95.4 88.0 53.0
NF-kB activation inhibitor Hs Inhibitor Inhibition 95.7 90.0 91.0
Akt inhibitor X Hs Inhibitor Inhibition 95.8 93.0 84.0
Cdk2 inhibitor III Hs Inhibitor Inhibition 95.9 96.0 89.0
TGF-beta RI kinase inhibitor Hs Inhibitor Inhibition 96.0 49.0 15.0
MEK1/2 inhibitor Hs Inhibitor Inhibition 96.0 87.0 82.0
triciribine Hs Inhibitor Inhibition 96.2 91.0 97.0
seliciclib Hs Inhibitor Inhibition 96.2
DNA-PK inhibitor V Hs Inhibitor Inhibition 96.3 79.0 83.0
Cdk1/5 inhibitor Hs Inhibitor Inhibition 96.6 90.0 97.0
NU-7026 Hs Inhibitor Inhibition 96.7 100.0 92.0
Cdk/Crk inhibitor Hs Inhibitor Inhibition 96.8 92.0 82.0
DNA-PK inhibitor III Hs Inhibitor Inhibition 97.1 110.0 116.0
indirubin-3'-monoxime Hs Inhibitor Inhibition 97.2 94.0 78.0
tozasertib Hs Inhibitor Inhibition 97.2
BAY 11-7082 Hs Inhibitor Inhibition 97.4 94.0 97.0
AGL 2043 Hs Inhibitor Inhibition 97.5 114.0 112.0
Flt-3 inhibitor Hs Inhibitor Inhibition 97.5 93.0 100.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 97.6 87.0 67.0
SU9516 Hs Inhibitor Inhibition 97.7 94.0 85.0
JNJ-7706621 Hs Inhibitor Inhibition 97.8 93.0 86.0
SP600125 Hs Inhibitor Inhibition 97.9 96.0 85.0
IC261 Hs Inhibitor Inhibition 98.0 89.0 85.0
masitinib Hs Inhibitor Inhibition 98.1
TWS119 Hs Inhibitor Inhibition 98.1 54.0 11.0
JNK inhibitor IX Hs Inhibitor Inhibition 98.1 80.0 102.0
EGFR inhibitor Hs Inhibitor Inhibition 98.2 80.0 40.0
vatalanib Hs Inhibitor Inhibition 98.2
AG 1024 Hs Inhibitor Inhibition 98.3 107.0 112.0
PQ401 Hs Inhibitor Inhibition 98.5 82.0 91.0
SKI II Hs Inhibitor Inhibition 98.6 89.0 35.0
imatinib Hs Inhibitor Inhibition 98.7
SU6656 Hs Inhibitor Inhibition 98.8 87.0 86.0
aminopurvalanol A Hs Inhibitor Inhibition 98.9 97.0 95.0
STO609 Hs Inhibitor Inhibition 99.0 95.0 94.0
diacylglycerol kinase inhibitor II Hs Inhibitor Inhibition 99.0 97.0 104.0
purvalanol A Hs Inhibitor Inhibition 99.1 88.0 80.0
GSK-3 inhibitor X Hs Inhibitor Inhibition 99.2 88.0 85.0
IRAK-1/4 inhibitor Hs Inhibitor Inhibition 99.3 89.0 101.0
KU-55933 Hs Inhibitor Inhibition 99.3 103.0 99.0
GSK-3beta inhibitor II Hs Inhibitor Inhibition 99.3 90.0 79.0
purvalanol A Hs Inhibitor Inhibition 99.4 88.0 80.0
casein kinase II inhibitor III Hs Inhibitor Inhibition 99.5 77.0 90.0
Akt inhibitor VIII Hs Inhibitor Inhibition 99.7 75.0 113.0
CGP74514A Hs Inhibitor Inhibition 100.1 90.0 61.0
IKK-2 inhibitor IV Hs Inhibitor Inhibition 100.6 91.0 77.0
isogranulatimide Hs Inhibitor Inhibition 100.7 93.0 87.0
ATM/ATR kinase inhibitor Hs Inhibitor Inhibition 100.7 105.0 105.0
lapatinib Hs Inhibitor Inhibition 100.9
indirubin derivative E804 Hs Inhibitor Inhibition 101.0 90.0 78.0
staurosporine Hs Inhibitor Inhibition 101.0 85.0 81.5
PI-103 Hs Inhibitor Inhibition 101.1 109.0 101.0
Cdk1 inhibitor Hs Inhibitor Inhibition 101.1 88.0 45.0
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibitor Inhibition 101.2 91.0 98.0
GSK-3beta inhibitor I Hs Inhibitor Inhibition 101.3 87.0 87.0
EGFR/ErbB-2 inhibitor Hs Inhibitor Inhibition 101.4 102.0 106.0
aloisine A Hs Inhibitor Inhibition 101.6 100.0 88.0
SB 218078 Hs Inhibitor Inhibition 101.7 90.0 105.0
bohemine Hs Inhibitor Inhibition 101.9 87.0 82.0
GTP-14564 Hs Inhibitor Inhibition 102.4 93.0 78.0
Flt-3 inhibitor II Hs Inhibitor Inhibition 102.5 75.0 73.0
PDGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 102.5 79.0 81.0
SU11652 Hs Inhibitor Inhibition 102.6 82.0 52.0
AG 1295 Hs Inhibitor Inhibition 102.9 85.0 82.0
Gö 6983 Hs Inhibitor Inhibition 103.0 95.0 91.0
mubritinib Hs Inhibitor Inhibition 103.1
Flt-3 inhibitor III Hs Inhibitor Inhibition 103.2 95.0 87.0
Src kinase inhibitor I Hs Inhibitor Inhibition 103.3 75.0 80.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 103.4 90.0 64.0
Cdk4 inhibitor II Hs Inhibitor Inhibition 103.6 88.0 91.0
GSK-3beta inhibitor VIII Hs Inhibitor Inhibition 103.8 94.0 87.0
Rho kinase inhibitor III Hs Inhibitor Inhibition 104.2 77.0 54.0
semaxanib Hs Inhibitor Inhibition 104.3 79.0 98.0
fasudil Hs Inhibitor Inhibition 104.4 90.0 93.0
AG 112 Hs Inhibitor Inhibition 104.5 78.0 55.0
Y27632 Hs Inhibitor Inhibition 104.7 106.0 107.0
sunitinib Hs Inhibitor Inhibition 104.9
H-89 Hs Inhibitor Inhibition 105.2 88.0 82.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 105.3 85.0 83.0
GW-2580 Hs Inhibitor Inhibition 106.2 84.0 99.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 106.6 90.0 64.0
AG1478 Hs Inhibitor Inhibition 107.3 56.0 25.0
Ro-32-0432 Hs Inhibitor Inhibition 107.5
AG 490 Hs Inhibitor Inhibition 108.4 72.0 102.0
bisindolylmaleimide IV Hs Inhibitor Inhibition 109.4 98.0 73.0
Rho kinase inhibitor IV Hs Inhibitor Inhibition 110.2 74.0 81.0
aloisine Hs Inhibitor Inhibition 112.1 99.0 100.0
SB 202474 Hs Inhibitor Inhibition 112.7 89.0 57.0
Syk inhibitor II Hs Inhibitor Inhibition 113.7 90.0 91.0
Tpl2 kinase inhibitor Hs Inhibitor Inhibition 114.5 87.0 89.0
VEGF receptor 2 kinase inhibitor IV Hs Inhibitor Inhibition 119.5 81.0 102.0
wortmannin Hs Inhibitor Inhibition 119.9
AG 9 Hs Inhibitor Inhibition 120.5 80.0 62.0
AG 1296 Hs Inhibitor Inhibition 121.9 92.0 88.0
VEGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 122.5
Syk inhibitor Hs Inhibitor Inhibition 123.5 94.0 96.0
Syk inhibitor III Hs Inhibitor Inhibition 125.6 93.0 105.0
VEGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 128.4 84.0 66.0
VEGF receptor 2 kinase inhibitor I Hs Inhibitor Inhibition 133.7 89.0 102.0
VEGF receptor 2 kinase inhibitor II Hs Inhibitor Inhibition 86.0 91.0

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. 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]