Proteins > Dual specificity mitogen-activated protein kinase kinase 5
Page last updated: 2024-08-07 23:48:26
Dual specificity mitogen-activated protein kinase kinase 5
A dual specificity mitogen-activated protein kinase kinase 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13163]
Synonyms
MAP kinase kinase 5;
MAPKK 5;
EC 2.7.12.2;
MAPK/ERK kinase 5;
MEK 5
Research
Bioassay Publications (9)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 7 (77.78) | 24.3611 |
2020's | 2 (22.22) | 2.80 |
Compounds (234)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
staurosporine | Homo sapiens (human) | IC50 | 0.0252 | 2 | 2 |
tak 285 | Homo sapiens (human) | IC50 | 5.7000 | 1 | 1 |
ly3009120 | Homo sapiens (human) | IC50 | 0.8000 | 1 | 1 |
bix 02188 | Homo sapiens (human) | IC50 | 0.0043 | 1 | 1 |
bix 02189 | Homo sapiens (human) | IC50 | 0.0015 | 3 | 3 |
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
fasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
imatinib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
triciribine phosphate | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
staurosporine | Homo sapiens (human) | Kd | 0.0029 | 1 | 1 |
picropodophyllin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
gefitinib | Homo sapiens (human) | Kd | 20.2000 | 2 | 3 |
lestaurtinib | Homo sapiens (human) | Kd | 0.9005 | 2 | 2 |
perifosine | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
vatalanib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
ruboxistaurin | Homo sapiens (human) | Kd | 15.5500 | 2 | 2 |
canertinib | Homo sapiens (human) | Kd | 15.0300 | 2 | 2 |
birb 796 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
cyc 202 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
sb 203580 | Homo sapiens (human) | Kd | 1.4000 | 1 | 1 |
enzastaurin | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
erlotinib | Homo sapiens (human) | Kd | 2.0010 | 2 | 2 |
lapatinib | Homo sapiens (human) | Kd | 15.5500 | 2 | 2 |
sorafenib | Homo sapiens (human) | Kd | 15.0950 | 2 | 2 |
pd 173955 | Homo sapiens (human) | Kd | 0.0580 | 1 | 1 |
s 1033 | Homo sapiens (human) | Kd | 15.0950 | 2 | 2 |
xl147 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
bms 387032 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
sf 2370 | Homo sapiens (human) | Kd | 2.0330 | 1 | 1 |
tandutinib | Homo sapiens (human) | Kd | 21.0333 | 2 | 3 |
vx-745 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
dasatinib | Homo sapiens (human) | Kd | 0.7176 | 2 | 2 |
ha 1100 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
7-epi-hydroxystaurosporine | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
zd 6474 | Homo sapiens (human) | Kd | 15.0245 | 2 | 2 |
imd 0354 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
sirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
alvocidib | Homo sapiens (human) | Kd | 15.0900 | 2 | 2 |
bosutinib | Homo sapiens (human) | Kd | 0.8386 | 2 | 2 |
orantinib | Homo sapiens (human) | Kd | 4.9380 | 1 | 1 |
su 11248 | Homo sapiens (human) | Kd | 1.7855 | 2 | 2 |
palbociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
vx680 | Homo sapiens (human) | Kd | 15.1300 | 2 | 2 |
cyc 116 | Homo sapiens (human) | Kd | 1.4780 | 1 | 1 |
everolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
ekb 569 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
axitinib | Homo sapiens (human) | Kd | 15.0700 | 2 | 2 |
temsirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
on 01910 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
av 412 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
telatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
y-39983 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
cp 547632 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
bms345541 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
lenvatinib | Homo sapiens (human) | Kd | 2.9100 | 1 | 1 |
pd 0325901 | Homo sapiens (human) | Kd | 0.8080 | 1 | 1 |
midostaurin | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
px-866 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
ripasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
osi 930 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
ki 20227 | Homo sapiens (human) | Kd | 0.0074 | 1 | 1 |
scio-469 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
cp 724714 | Homo sapiens (human) | Kd | 1.2550 | 1 | 1 |
pi103 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
hmn-214 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
tivozanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
hki 272 | Homo sapiens (human) | Kd | 15.0315 | 2 | 2 |
tofacitinib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
cediranib | Homo sapiens (human) | Kd | 15.7500 | 2 | 2 |
masitinib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
ly-2157299 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
pazopanib | Homo sapiens (human) | Kd | 15.2400 | 2 | 2 |
azd 6244 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
su 14813 | Homo sapiens (human) | Kd | 15.0375 | 2 | 2 |
bibw 2992 | Homo sapiens (human) | Kd | 15.6500 | 2 | 2 |
binimetinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
sotrastaurin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
aee 788 | Homo sapiens (human) | Kd | 9.4300 | 1 | 1 |
saracatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
vx 702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
crenolanib | Homo sapiens (human) | Kd | 0.0410 | 1 | 1 |
tg100-115 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
cc 401 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
bms 599626 | Homo sapiens (human) | Kd | 5.9270 | 1 | 1 |
exel-7647 | Homo sapiens (human) | Kd | 65.6770 | 1 | 1 |
volasertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
pha 665752 | Homo sapiens (human) | Kd | 1.4000 | 1 | 1 |
azd 7762 | Homo sapiens (human) | Kd | 0.1470 | 1 | 1 |
regorafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | Homo sapiens (human) | Kd | 15.0205 | 2 | 2 |
brivanib | Homo sapiens (human) | Kd | 16.5500 | 2 | 2 |
mp470 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
rgb 286638 | Homo sapiens (human) | Kd | 0.5350 | 1 | 1 |
np 031112 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
at 7519 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
bms-690514 | Homo sapiens (human) | Kd | 0.9720 | 1 | 1 |
bi 2536 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
inno-406 | Homo sapiens (human) | Kd | 11.3920 | 1 | 1 |
nvp-ast487 | Homo sapiens (human) | Kd | 0.0740 | 1 | 1 |
kw 2449 | Homo sapiens (human) | Kd | 15.0600 | 2 | 2 |
danusertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
abt 869 | Homo sapiens (human) | Kd | 15.6000 | 2 | 2 |
azd 8931 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
arq 197 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
azd 1152 | Homo sapiens (human) | Kd | 0.0820 | 1 | 1 |
pf 00299804 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
ridaforolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
ch 4987655 | Homo sapiens (human) | Kd | 30.4840 | 1 | 1 |
6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-n-(2,2-dimethylprpyl)-3-pyridinecarboxamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
cc-930 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
gw 2580 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
tak 285 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
idelalisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
crizotinib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
osi 906 | Homo sapiens (human) | Kd | 6.5580 | 1 | 1 |
chir-265 | Homo sapiens (human) | Kd | 15.9500 | 2 | 2 |
motesanib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
fostamatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
trametinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
mln8054 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
pf-562,271 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
GDC-0879 | Homo sapiens (human) | Kd | 5.1000 | 1 | 1 |
jnj-26483327 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
ly2603618 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
tg100801 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
dactolisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
bgt226 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
gsk 461364 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
azd 1152-hqpa | Homo sapiens (human) | Kd | 0.2039 | 2 | 2 |
nvp-tae684 | Homo sapiens (human) | Kd | 0.2000 | 1 | 1 |
enmd 2076 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
e 7050 | Homo sapiens (human) | Kd | 2.4520 | 1 | 1 |
2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinone | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
tak-901 | Homo sapiens (human) | Kd | 6.7970 | 1 | 1 |
gdc-0973 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
buparlisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
azd 1480 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
azd8330 | Homo sapiens (human) | Kd | 2.6570 | 1 | 1 |
pha 848125 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
ro5126766 | Homo sapiens (human) | Kd | 1.9960 | 1 | 1 |
fedratinib | Homo sapiens (human) | Kd | 15.1800 | 2 | 2 |
gsk690693 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
azd5438 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
pf 04217903 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
gdc 0941 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
icotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
ph 797804 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
kx-01 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
plx 4720 | Homo sapiens (human) | Kd | 0.0002 | 1 | 1 |
mk 5108 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
cx 4945 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
cudc 101 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
arry-614 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
tak 593 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
mln 8237 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
sgx 523 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
bms 754807 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
bms 777607 | Homo sapiens (human) | Kd | 2.0850 | 1 | 1 |
sgi 1776 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
pci 32765 | Homo sapiens (human) | Kd | 0.2430 | 1 | 1 |
ponatinib | Homo sapiens (human) | Kd | 2.9520 | 1 | 1 |
amg 900 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
mk-1775 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
AMG-208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
quizartinib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
at13148 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
tak 733 | Homo sapiens (human) | Kd | 3.3480 | 1 | 1 |
mk 2206 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
sns 314 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
lucitanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
pf-04691502 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
dcc-2036 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
cabozantinib | Homo sapiens (human) | Kd | 2.3880 | 1 | 1 |
defactinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
ly2584702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
incb-018424 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
poziotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
asp3026 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
entrectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
pexidartinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
TAK-580 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
gsk 2126458 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
emd1214063 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
gsk 1838705a | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
pf 3758309 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
gdc 0980 | Homo sapiens (human) | Kd | 3.5760 | 1 | 1 |
azd2014 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
(5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
plx4032 | Homo sapiens (human) | Kd | 0.7340 | 1 | 1 |
gsk 1363089 | Homo sapiens (human) | Kd | 0.0812 | 2 | 2 |
arry-334543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
kin-193 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
mk 2461 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
bay 869766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
as 703026 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
baricitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
dabrafenib | Homo sapiens (human) | Kd | 2.2940 | 1 | 1 |
pki 587 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
ribociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
mk-8033 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
pha 793887 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
sb 1518 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
abemaciclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
mk-8776 | Homo sapiens (human) | Kd | 0.6090 | 1 | 1 |
afuresertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
gsk 1070916 | Homo sapiens (human) | Kd | 1.9290 | 1 | 1 |
jnj38877605 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
dinaciclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
gilteritinib | Homo sapiens (human) | Kd | 2.0400 | 1 | 1 |
alectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
glpg0634 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
encorafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
bms-911543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
gsk2141795 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
azd8186 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
byl719 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
cep-32496 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
rociletinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
ceritinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
azd1208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
vx-509 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
debio 1347 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
volitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
osimertinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
at 9283 | Homo sapiens (human) | Kd | 0.0470 | 1 | 1 |
otssp167 | Homo sapiens (human) | Kd | 0.0580 | 1 | 1 |
chir 258 | Homo sapiens (human) | Kd | 0.8150 | 2 | 2 |
osi 027 | Homo sapiens (human) | Kd | 4.9140 | 1 | 1 |
nintedanib | Homo sapiens (human) | Kd | 0.0909 | 2 | 2 |
bay 80-6946 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
pp242 | Homo sapiens (human) | Kd | 0.0073 | 1 | 1 |
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Non-'classical' MEKs: A review of MEK3-7 inhibitors.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 30, Issue:13, 2020
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Enables
This protein enables 8 target(s):
Target | Category | Definition |
protein kinase activity | molecular function | Catalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640] |
protein serine/threonine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925] |
protein tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
MAP kinase kinase activity | molecular function | Catalysis of the concomitant phosphorylation of threonine (T) and tyrosine (Y) residues in a Thr-Glu-Tyr (TEY) thiolester sequence in a MAP kinase (MAPK) substrate. [ISBN:0198547684] |
Located In
This protein is located in 1 target(s):
Target | Category | Definition |
spindle | cellular component | The array of microtubules and associated molecules that forms between opposite poles of a eukaryotic cell during mitosis or meiosis and serves to move the duplicated chromosomes apart. [ISBN:0198547684] |
Involved In
This protein is involved in 22 target(s):
Target | Category | Definition |
negative regulation of transcription by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
MAPK cascade | biological process | An intracellular protein kinase cascade containing at least a MAP kinase (MAPK). It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and a MAPK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinase in the downstream tier to transmit a signal within a cell. [PMID:20811974, PMID:9561267] |
signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
heart development | biological process | The process whose specific outcome is the progression of the heart over time, from its formation to the mature structure. The heart is a hollow, muscular organ, which, by contracting rhythmically, keeps up the circulation of the blood. [GOC:jid, UBERON:0000948] |
positive regulation of cell growth | biological process | Any process that activates or increases the frequency, rate, extent or direction of cell growth. [GOC:go_curators] |
negative regulation of NF-kappaB transcription factor activity | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the activity of the transcription factor NF-kappaB. [GOC:dph, GOC:rl, GOC:tb] |
negative regulation of interleukin-8 production | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of interleukin-8 production. [GOC:mah] |
negative regulation of heterotypic cell-cell adhesion | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of heterotypic cell-cell adhesion. [GOC:add] |
negative regulation of smooth muscle cell apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of smooth muscle cell apoptotic process. [GOC:BHF, GOC:mtg_apoptosis, GOC:rl] |
negative regulation of cysteine-type endopeptidase activity involved in apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of a cysteine-type endopeptidase activity involved in the apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
positive regulation of MAP kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of MAP kinase activity. [GOC:dph, GOC:go_curators] |
positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
insulin-like growth factor receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to an insulin-like growth factor receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb] |
positive regulation of epithelial cell proliferation | biological process | Any process that activates or increases the rate or extent of epithelial cell proliferation. [GOC:ai] |
positive regulation of protein metabolic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways involving a protein. [GOC:ai] |
negative regulation of response to cytokine stimulus | biological process | Any process that decreases the rate, frequency, or extent of a response to cytokine stimulus. [GOC:BHF, GOC:dph, GOC:tb] |
ERK5 cascade | biological process | A MAPK cascade containing at least the ERK5 MAP kinase (MAPK7; also called BMK1). It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and of ERK5. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinases in the downstream tier. The ERK5 cascade is activated by stress, mitogens, and by G protein-coupled receptors, and results in cellular responses such as cell growth, cell differentiation and development. [PMID:16376520, PMID:16880823, PMID:20811974, PMID:23125017, PMID:28903453] |
cellular response to growth factor stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a growth factor stimulus. [GOC:mah] |
cellular response to laminar fluid shear stress | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a laminar fluid shear stress stimulus. Laminar fluid flow is the force acting on an object in a system where the fluid is moving across a solid surface in parallel layers. [GOC:mah] |
negative regulation of cell migration involved in sprouting angiogenesis | biological process | Any process that decreases the frequency, rate or extent of cell migration involved in sprouting angiogenesis. Cell migration involved in sprouting angiogenesis is the orderly movement of endothelial cells into the extracellular matrix in order to form new blood vessels contributing to the process of sprouting angiogenesis. [GOC:BHF, GOC:dph, GOC:rl, GOC:tb] |
negative regulation of chemokine (C-X-C motif) ligand 2 production | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of chemokine (C-X-C motif) ligand 2 production. [GOC:BHF, GOC:mah] |
negative regulation of extrinsic apoptotic signaling pathway in absence of ligand | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of extrinsic apoptotic signaling pathway in absence of ligand. [GOC:mtg_apoptosis] |