Page last updated: 2024-08-07 18:37:20
Cyclin-dependent kinase 7
A cyclin-dependent kinase 7 that is encoded in the genome of human. [PRO:DNx]
Synonyms
EC 2.7.11.22;
EC 2.7.11.23;
39 kDa protein kinase;
p39 Mo15;
CDK-activating kinase 1;
Cell division protein kinase 7;
Serine/threonine-protein kinase 1;
TFIIH basal transcription factor complex kinase subunit
Research
Bioassay Publications (61)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 15 (24.59) | 29.6817 |
2010's | 32 (52.46) | 24.3611 |
2020's | 14 (22.95) | 2.80 |
Compounds (273)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
gw8510 | Homo sapiens (human) | IC50 | 0.3170 | 1 | 1 |
nu6102 | Homo sapiens (human) | IC50 | 3.7667 | 3 | 3 |
indirubin | Homo sapiens (human) | IC50 | 2.2000 | 1 | 1 |
staurosporine | Homo sapiens (human) | IC50 | 0.2793 | 5 | 5 |
cyc 202 | Homo sapiens (human) | IC50 | 0.5635 | 17 | 21 |
2H-pyrazolo[4,3-b]quinoxalin-3-amine | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
6-bromoindirubin-3'-oxime | Homo sapiens (human) | IC50 | 3.5000 | 1 | 1 |
purvalanol a | Homo sapiens (human) | IC50 | 0.0497 | 1 | 3 |
2-methyl-5-(4-methylanilino)-1,3-benzothiazole-4,7-dione | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
cgp 60474 | Homo sapiens (human) | IC50 | 0.2000 | 1 | 1 |
cid755673 | Homo sapiens (human) | IC50 | 21.5250 | 1 | 4 |
cgp 74514a | Homo sapiens (human) | IC50 | 0.2790 | 1 | 1 |
1,4-dimethoxy-10H-acridine-9-thione | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
bms 387032 | Homo sapiens (human) | IC50 | 0.0773 | 8 | 8 |
harmine | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
wogonin | Homo sapiens (human) | IC50 | 12.3000 | 1 | 1 |
alvocidib | Homo sapiens (human) | IC50 | 0.3365 | 6 | 6 |
su 9516 | Homo sapiens (human) | IC50 | 0.9050 | 1 | 1 |
arcyriaflavin a | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
palbociclib | Homo sapiens (human) | IC50 | 7.7777 | 3 | 3 |
palbociclib | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
cyc 116 | Homo sapiens (human) | Ki | 10.0000 | 2 | 2 |
cvt 313 | Homo sapiens (human) | IC50 | 9.2000 | 1 | 1 |
jnj 10198409 | Homo sapiens (human) | IC50 | 33.3500 | 2 | 2 |
leucettamine b | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
nu 6140 | Homo sapiens (human) | IC50 | 2.3000 | 1 | 1 |
rgb 286638 | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
at 7519 | Homo sapiens (human) | IC50 | 2.4000 | 2 | 2 |
at 7519 | Homo sapiens (human) | Ki | 2.8000 | 1 | 1 |
pf 573228 | Homo sapiens (human) | IC50 | 0.5985 | 2 | 2 |
crizotinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
pha 767491 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
pha 848125 | Homo sapiens (human) | IC50 | 0.1900 | 3 | 3 |
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) | IC50 | 0.0257 | 3 | 3 |
p276-00 | Homo sapiens (human) | IC50 | 2.8700 | 1 | 1 |
cink4 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
ldc067 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
bs 194 | Homo sapiens (human) | IC50 | 0.2500 | 2 | 2 |
(R)-DRF053 | Homo sapiens (human) | IC50 | 0.8220 | 1 | 1 |
pf 3758309 | Homo sapiens (human) | IC50 | 0.0070 | 1 | 1 |
ribociclib | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
bay 1000394 | Homo sapiens (human) | IC50 | 0.0210 | 5 | 5 |
pha 793887 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
abemaciclib | Homo sapiens (human) | IC50 | 2.0270 | 4 | 4 |
abemaciclib | Homo sapiens (human) | Ki | 3.9100 | 1 | 1 |
dinaciclib | Homo sapiens (human) | IC50 | 0.1273 | 3 | 3 |
gilteritinib | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
longdaysin | Homo sapiens (human) | IC50 | 32.0000 | 1 | 1 |
bs-181 | Homo sapiens (human) | IC50 | 0.0662 | 5 | 5 |
on123300 | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
ldc4297 | Homo sapiens (human) | IC50 | 0.0034 | 3 | 3 |
ly2857785 | Homo sapiens (human) | IC50 | 0.2460 | 1 | 1 |
THZ531 | Homo sapiens (human) | IC50 | 4.4025 | 4 | 4 |
can 508 | Homo sapiens (human) | IC50 | 25.2846 | 4 | 13 |
((5z)5-(1,3-benzodioxol-5-yl)methylene-2-phenylamino-3,5-dihydro-4h-imidazol-4-one) | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
ro 3306 | Homo sapiens (human) | IC50 | 17.4000 | 1 | 1 |
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 |
sb 202190 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
imatinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
triciribine phosphate | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
staurosporine | Homo sapiens (human) | Kd | 0.0450 | 2 | 2 |
picropodophyllin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
gefitinib | Homo sapiens (human) | Kd | 13.5367 | 3 | 3 |
lestaurtinib | Homo sapiens (human) | Kd | 10.0580 | 3 | 3 |
perifosine | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
vatalanib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
ruboxistaurin | Homo sapiens (human) | Kd | 13.9000 | 3 | 3 |
canertinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
birb 796 | Homo sapiens (human) | Kd | 6.5500 | 2 | 2 |
cyc 202 | Homo sapiens (human) | Kd | 2.7525 | 2 | 2 |
sb 203580 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
enzastaurin | Homo sapiens (human) | Kd | 16.3000 | 2 | 2 |
erlotinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
lapatinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
sorafenib | Homo sapiens (human) | Kd | 7.6050 | 4 | 4 |
pd 173955 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
s 1033 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
xl147 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
bms 387032 | Homo sapiens (human) | Kd | 0.3547 | 3 | 3 |
sf 2370 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
tandutinib | Homo sapiens (human) | Kd | 13.2750 | 4 | 4 |
vx-745 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
dasatinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
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 | 14.7000 | 3 | 3 |
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
imd 0354 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
sirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
alvocidib | Homo sapiens (human) | Kd | 0.2403 | 3 | 3 |
bosutinib | Homo sapiens (human) | Kd | 15.6000 | 2 | 2 |
orantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
su 11248 | Homo sapiens (human) | Kd | 0.5480 | 4 | 4 |
palbociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
jnj-7706621 | Homo sapiens (human) | Kd | 0.7600 | 1 | 1 |
vx680 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
cyc 116 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
everolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
ekb 569 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
axitinib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
abt-100 | Homo sapiens (human) | Kd | 10.0000 | 1 | 0 |
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 | 0.6800 | 1 | 1 |
lenvatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
pd 0325901 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
midostaurin | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
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 | 10.0000 | 1 | 1 |
scio-469 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
cp 724714 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
pi103 | Homo sapiens (human) | Kd | 8.6000 | 2 | 2 |
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 | 17.5500 | 2 | 2 |
tofacitinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
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 | 20.0000 | 2 | 2 |
masitinib | Homo sapiens (human) | Kd | 23.3333 | 2 | 3 |
ly-2157299 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
pazopanib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
azd 6244 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
su 14813 | Homo sapiens (human) | Kd | 10.6200 | 3 | 3 |
bibw 2992 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
pik 75 | Homo sapiens (human) | Kd | 0.0025 | 1 | 1 |
binimetinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
sotrastaurin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
aee 788 | Homo sapiens (human) | Kd | 30.0000 | 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 | 30.0000 | 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 | 30.0000 | 1 | 1 |
exel-7647 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
volasertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
pha 665752 | Homo sapiens (human) | Kd | 0.1300 | 1 | 1 |
azd 7762 | Homo sapiens (human) | Kd | 30.0000 | 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 | 18.8500 | 2 | 2 |
brivanib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
mp470 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
rgb 286638 | Homo sapiens (human) | Kd | 0.1540 | 1 | 1 |
np 031112 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
at 7519 | Homo sapiens (human) | Kd | 2.0319 | 2 | 2 |
bms-690514 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
bi 2536 | Homo sapiens (human) | Kd | 16.7500 | 2 | 2 |
inno-406 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
nvp-ast487 | Homo sapiens (human) | Kd | 0.0046 | 2 | 2 |
kw 2449 | Homo sapiens (human) | Kd | 1.7955 | 2 | 2 |
danusertib | Homo sapiens (human) | Kd | 0.1080 | 1 | 1 |
abt 869 | Homo sapiens (human) | Kd | 11.9333 | 3 | 3 |
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 | 30.0000 | 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 | 30.0000 | 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 | 2 | 2 |
tak 285 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
idelalisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
crizotinib | Homo sapiens (human) | Kd | 15.1650 | 2 | 2 |
osi 906 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
chir-265 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
motesanib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
fostamatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
trametinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
mln8054 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
pf-562,271 | Homo sapiens (human) | Kd | 1.3340 | 1 | 1 |
GDC-0879 | Homo sapiens (human) | Kd | 10.0000 | 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 | 2 |
gsk 461364 | Homo sapiens (human) | Kd | 18.8500 | 2 | 2 |
azd 1152-hqpa | Homo sapiens (human) | Kd | 14.1333 | 3 | 3 |
nvp-tae684 | Homo sapiens (human) | Kd | 0.1900 | 1 | 1 |
enmd 2076 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
e 7050 | Homo sapiens (human) | Kd | 30.0000 | 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 | 0.2050 | 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 | 30.0000 | 1 | 1 |
pha 848125 | Homo sapiens (human) | Kd | 0.2850 | 1 | 1 |
ro5126766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
fedratinib | Homo sapiens (human) | Kd | 15.0600 | 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 | 0.4730 | 1 | 1 |
azd5438 | Homo sapiens (human) | Kd | 2.3320 | 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 | 10.0000 | 1 | 1 |
mk 5108 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
cx 4945 | Homo sapiens (human) | Kd | 7.1240 | 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 | 30.0000 | 1 | 1 |
sgi 1776 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
pci 32765 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
ponatinib | Homo sapiens (human) | Kd | 30.0000 | 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 | 16.6667 | 3 | 3 |
at13148 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
tak 733 | Homo sapiens (human) | Kd | 30.0000 | 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 | 30.0000 | 1 | 1 |
defactinib | Homo sapiens (human) | Kd | 1.7440 | 1 | 1 |
ly2584702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
incb-018424 | Homo sapiens (human) | Kd | 16.6500 | 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 | 0.0030 | 1 | 1 |
gdc 0980 | Homo sapiens (human) | Kd | 30.0000 | 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 | 30.0000 | 1 | 1 |
gsk 1363089 | Homo sapiens (human) | Kd | 15.0018 | 2 | 2 |
arry-334543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
kin-193 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
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 | 30.0000 | 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 | 1 |
pha 793887 | Homo sapiens (human) | Kd | 0.0080 | 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 | 30.0000 | 1 | 1 |
afuresertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
gsk 1070916 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
jnj38877605 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
dinaciclib | Homo sapiens (human) | Kd | 0.4110 | 1 | 1 |
gilteritinib | Homo sapiens (human) | Kd | 30.0000 | 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 | 1.1270 | 1 | 1 |
azd8186 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
byl719 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
cep-32496 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
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 | 30.0000 | 1 | 2 |
otssp167 | Homo sapiens (human) | Kd | 0.1570 | 1 | 1 |
chir 258 | Homo sapiens (human) | Kd | 11.7333 | 3 | 3 |
osi 027 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
nintedanib | Homo sapiens (human) | Kd | 15.1500 | 2 | 2 |
bay 80-6946 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
pp242 | Homo sapiens (human) | Kd | 5.5000 | 1 | 1 |
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
cyc 202 | Homo sapiens (human) | INH | 24.5000 | 1 | 1 |
olomoucine ii | Homo sapiens (human) | INH | 11.4000 | 1 | 1 |
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Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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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
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 2020
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).Bioorganic & medicinal chemistry letters, , 10-15, Volume: 29, Issue:20, 2019
A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
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CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Development and Therapeutic Potential of NUAKs Inhibitors.Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 2020
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.Bioorganic & medicinal chemistry, , Mar-01, Volume: 18, Issue:5, 2010
Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors.European journal of medicinal chemistry, , May-01, Volume: 193, 2020
Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib.European journal of medicinal chemistry, , Jun-15, Volume: 172, 2019
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Current progress and novel strategies that target CDK12 for drug discovery.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations.European journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).Bioorganic & medicinal chemistry letters, , 10-15, Volume: 29, Issue:20, 2019
5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.European journal of medicinal chemistry, , Mar-03, Volume: 110, 2016
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).Bioorganic & medicinal chemistry letters, , 10-15, Volume: 29, Issue:20, 2019
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry, , May-01, Volume: 23, Issue:9, 2015
Arylazopyrazole AAP1742 inhibits CDKs and induces apoptosis in multiple myeloma cells via Mcl-1 downregulation.Chemical biology & drug design, , Volume: 84, Issue:4, 2014
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
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
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 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] |
ATP-dependent activity, acting on DNA | molecular function | Catalytic activity that acts to modify DNA, driven by ATP hydrolysis. [GOC:pdt] |
RNA polymerase II CTD heptapeptide repeat kinase activity | molecular function | Catalysis of the reaction: ATP + RNA polymerase II large subunit CTD heptapeptide repeat (consensus YSPTSPS) = ADP + H+ + phosphorylated RNA polymerase II. [EC:2.7.11.23, GOC:mah, PMID:28248323] |
protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
cyclin-dependent protein serine/threonine kinase activity | molecular function | Cyclin-dependent catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:pr, GOC:rn, PMID:7877684, PMID:9841670] |
Located In
This protein is located in 7 target(s):
Target | Category | Definition |
fibrillar center | cellular component | A structure found most metazoan nucleoli, but not usually found in lower eukaryotes; surrounded by the dense fibrillar component; the zone of transcription from multiple copies of the pre-rRNA genes is in the border region between these two structures. [PMID:10754561] |
male germ cell nucleus | cellular component | The nucleus of a male germ cell, a reproductive cell in males. [CL:0000015, GOC:hjd, GOC:mtg_sensu] |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
Active In
This protein is active in 2 target(s):
Target | Category | Definition |
cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 5 target(s):
Target | Category | Definition |
cyclin-dependent protein kinase holoenzyme complex | cellular component | Cyclin-dependent protein kinases (CDKs) are enzyme complexes that contain a kinase catalytic subunit associated with a regulatory cyclin partner. [GOC:krc, PMID:11602261] |
transcription factor TFIIH core complex | cellular component | The 7 subunit core of TFIIH that is a part of either the general transcription factor holo-TFIIH or the nucleotide-excision repair factor 3 complex. In S. cerevisiae/humans the complex is composed of: Ssl2/XPB, Tfb1/p62, Tfb2/p52, Ssl1/p44, Tfb4/p34, Tfb5/p8 and Rad3/XPD. [GOC:ew, GOC:krc, PMID:14500720, PMID:17215295, PMID:22308316, PMID:22572993, PMID:23028141, PMID:7813015] |
transcription factor TFIIH holo complex | cellular component | A complex that is capable of kinase activity directed towards the C-terminal Domain (CTD) of the largest subunit of RNA polymerase II and is essential for initiation at RNA polymerase II promoters in vitro. It is composed of the core TFIIH complex and the TFIIK complex. [GOC:ew, GOC:krc, PMID:14500720, PMID:22308316, PMID:22572993, PMID:7813015] |
CAK-ERCC2 complex | cellular component | A protein complex formed by the association of the cyclin-dependent protein kinase activating kinase (CAK) holoenzyme complex with ERCC2. [PMID:8692841, PMID:8692842] |
transcription factor TFIIK complex | cellular component | A transcription factor complex that forms part of the holo TFIIH complex. In Saccharomyces/human, TFIIK contains Ccl1p/Cyclin H, Tfb3p/MAT1 and Kin28p/CDK7. [GOC:mah, PMID:19818408, PMID:22572993] |
Involved In
This protein is involved in 10 target(s):
Target | Category | Definition |
DNA repair | biological process | The process of restoring DNA after damage. Genomes are subject to damage by chemical and physical agents in the environment (e.g. UV and ionizing radiations, chemical mutagens, fungal and bacterial toxins, etc.) and by free radicals or alkylating agents endogenously generated in metabolism. DNA is also damaged because of errors during its replication. A variety of different DNA repair pathways have been reported that include direct reversal, base excision repair, nucleotide excision repair, photoreactivation, bypass, double-strand break repair pathway, and mismatch repair pathway. [PMID:11563486] |
transcription by RNA polymerase II | biological process | The synthesis of RNA from a DNA template by RNA polymerase II (RNAP II), originating at an RNA polymerase II promoter. Includes transcription of messenger RNA (mRNA) and certain small nuclear RNAs (snRNAs). [GOC:jl, GOC:txnOH, ISBN:0321000382] |
transcription initiation at RNA polymerase II promoter | biological process | A transcription initiation process that takes place at a RNA polymerase II gene promoter. Messenger RNAs (mRNA) genes, as well as some non-coding RNAs, are transcribed by RNA polymerase II. [GOC:mah, GOC:txnOH] |
snRNA transcription by RNA polymerase II | biological process | The synthesis of small nuclear RNA (snRNA) from a DNA template by RNA Polymerase II (Pol II), originating at a Pol II promoter. [GOC:jl, ISBN:0321000382] |
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] |
protein stabilization | biological process | Any process involved in maintaining the structure and integrity of a protein and preventing it from degradation or aggregation. [GOC:ai] |
cell division | biological process | The process resulting in division and partitioning of components of a cell to form more cells; may or may not be accompanied by the physical separation of a cell into distinct, individually membrane-bounded daughter cells. [GOC:di, GOC:go_curators, GOC:pr] |
regulation of cell cycle | biological process | Any process that modulates the rate or extent of progression through the cell cycle. [GOC:ai, GOC:dph, GOC:tb] |
regulation of G1/S transition of mitotic cell cycle | biological process | Any signaling pathway that modulates the activity of a cell cycle cyclin-dependent protein kinase to modulate the switch from G1 phase to S phase of the mitotic cell cycle. [GOC:mtg_cell_cycle] |
protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |