Page last updated: 2024-08-07 21:22:41

Cyclin-dependent kinase 12

A cyclin-dependent kinase 12 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYV4]

Synonyms

EC 2.7.11.22;
EC 2.7.11.23;
Cdc2-related kinase, arginine/serine-rich;
CrkRS;
Cell division cycle 2-related protein kinase 7;
CDC2-related protein kinase 7;
Cell division protein kinase 12;
hCDK12

Research

Bioassay Publications (10)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (50.00)24.3611
2020's5 (50.00)2.80

Compounds (219)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
indirubinHomo sapiens (human)IC502.200011
staurosporineHomo sapiens (human)IC500.053011
1-tert-butyl-3-naphthalen-1-ylmethyl-1h-pyrazolo(3,4-d)pyrimidin-4-ylemineHomo sapiens (human)IC500.100011
alvocidibHomo sapiens (human)IC501.370011
dinaciclibHomo sapiens (human)IC500.032333
sr-3029Homo sapiens (human)IC500.054521
THZ531Homo sapiens (human)IC502.324644

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
fasudilHomo sapiens (human)Kd3.480011
4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazolineHomo sapiens (human)Kd30.000011
imatinibHomo sapiens (human)Kd30.000011
triciribine phosphateHomo sapiens (human)Kd30.000011
picropodophyllinHomo sapiens (human)Kd30.000011
gefitinibHomo sapiens (human)Kd30.000011
lestaurtinibHomo sapiens (human)Kd30.000011
perifosineHomo sapiens (human)Kd30.000011
vatalanibHomo sapiens (human)Kd30.000011
ruboxistaurinHomo sapiens (human)Kd30.000011
canertinibHomo sapiens (human)Kd30.000011
cyc 202Homo sapiens (human)Kd30.000011
enzastaurinHomo sapiens (human)Kd30.000011
erlotinibHomo sapiens (human)Kd30.000011
lapatinibHomo sapiens (human)Kd30.000011
sorafenibHomo sapiens (human)Kd30.000011
s 1033Homo sapiens (human)Kd30.000011
xl147Homo sapiens (human)Kd30.000011
bms 387032Homo sapiens (human)Kd0.167011
sf 2370Homo sapiens (human)Kd30.000011
tandutinibHomo sapiens (human)Kd30.000011
dasatinibHomo sapiens (human)Kd30.000011
ha 1100Homo sapiens (human)Kd30.000011
7-epi-hydroxystaurosporineHomo sapiens (human)Kd30.000011
zd 6474Homo sapiens (human)Kd30.000011
imd 0354Homo sapiens (human)Kd30.000011
sirolimusHomo sapiens (human)Kd30.000011
alvocidibHomo sapiens (human)Kd0.157011
bosutinibHomo sapiens (human)Kd30.000011
orantinibHomo sapiens (human)Kd30.000011
su 11248Homo sapiens (human)Kd30.000011
palbociclibHomo sapiens (human)Kd30.000011
vx680Homo sapiens (human)Kd30.000011
cyc 116Homo sapiens (human)Kd30.000011
everolimusHomo sapiens (human)Kd30.000011
ekb 569Homo sapiens (human)Kd30.000011
axitinibHomo sapiens (human)Kd30.000011
temsirolimusHomo sapiens (human)Kd30.000011
on 01910Homo sapiens (human)Kd30.000011
av 412Homo sapiens (human)Kd30.000011
telatinibHomo sapiens (human)Kd30.000011
y-39983Homo sapiens (human)Kd30.000011
cp 547632Homo sapiens (human)Kd30.000012
lenvatinibHomo sapiens (human)Kd30.000011
pd 0325901Homo sapiens (human)Kd30.000011
midostaurinHomo sapiens (human)Kd30.000012
px-866Homo sapiens (human)Kd30.000011
ripasudilHomo sapiens (human)Kd30.000011
osi 930Homo sapiens (human)Kd30.000012
scio-469Homo sapiens (human)Kd30.000011
cp 724714Homo sapiens (human)Kd30.000011
hmn-214Homo sapiens (human)Kd30.000011
tivozanibHomo sapiens (human)Kd30.000011
hki 272Homo sapiens (human)Kd30.000011
tofacitinibHomo sapiens (human)Kd30.000011
cediranibHomo sapiens (human)Kd30.000012
masitinibHomo sapiens (human)Kd30.000011
ly-2157299Homo sapiens (human)Kd30.000011
pazopanibHomo sapiens (human)Kd30.000011
azd 6244Homo sapiens (human)Kd30.000011
su 14813Homo sapiens (human)Kd30.000011
bibw 2992Homo sapiens (human)Kd30.000011
binimetinibHomo sapiens (human)Kd30.000011
sotrastaurinHomo sapiens (human)Kd30.000011
aee 788Homo sapiens (human)Kd30.000011
saracatinibHomo sapiens (human)Kd30.000011
vx 702Homo sapiens (human)Kd30.000011
crenolanibHomo sapiens (human)Kd30.000011
tg100-115Homo sapiens (human)Kd30.000011
cc 401Homo sapiens (human)Kd30.000011
bms 599626Homo sapiens (human)Kd30.000011
exel-7647Homo sapiens (human)Kd30.000011
volasertibHomo sapiens (human)Kd30.000011
azd 7762Homo sapiens (human)Kd30.000011
regorafenibHomo sapiens (human)Kd30.000011
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-oneHomo sapiens (human)Kd30.000011
brivanibHomo sapiens (human)Kd30.000011
mp470Homo sapiens (human)Kd30.000011
rgb 286638Homo sapiens (human)Kd0.947011
np 031112Homo sapiens (human)Kd30.000011
at 7519Homo sapiens (human)Kd0.250011
bms-690514Homo sapiens (human)Kd30.000011
bi 2536Homo sapiens (human)Kd30.000011
inno-406Homo sapiens (human)Kd30.000011
kw 2449Homo sapiens (human)Kd30.000011
danusertibHomo sapiens (human)Kd30.000011
abt 869Homo sapiens (human)Kd30.000012
azd 8931Homo sapiens (human)Kd30.000011
arq 197Homo sapiens (human)Kd30.000011
azd 1152Homo sapiens (human)Kd30.000011
pf 00299804Homo sapiens (human)Kd30.000011
ridaforolimusHomo sapiens (human)Kd30.000011
ch 4987655Homo sapiens (human)Kd30.000011
6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-n-(2,2-dimethylprpyl)-3-pyridinecarboxamideHomo sapiens (human)Kd30.000011
cc-930Homo sapiens (human)Kd30.000011
tak 285Homo sapiens (human)Kd30.000011
idelalisibHomo sapiens (human)Kd30.000011
crizotinibHomo sapiens (human)Kd30.000011
osi 906Homo sapiens (human)Kd30.000011
chir-265Homo sapiens (human)Kd30.000011
motesanibHomo sapiens (human)Kd30.000012
fostamatinibHomo sapiens (human)Kd30.000011
trametinibHomo sapiens (human)Kd30.000011
mln8054Homo sapiens (human)Kd30.000011
pf-562,271Homo sapiens (human)Kd30.000011
jnj-26483327Homo sapiens (human)Kd30.000011
ly2603618Homo sapiens (human)Kd30.000012
tg100801Homo sapiens (human)Kd30.000011
dactolisibHomo sapiens (human)Kd30.000011
bgt226Homo sapiens (human)Kd30.000011
gsk 461364Homo sapiens (human)Kd30.000011
azd 1152-hqpaHomo sapiens (human)Kd30.000011
enmd 2076Homo sapiens (human)Kd30.000011
e 7050Homo sapiens (human)Kd30.000011
2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinoneHomo sapiens (human)Kd30.000011
tak-901Homo sapiens (human)Kd30.000011
gdc-0973Homo sapiens (human)Kd30.000011
buparlisibHomo sapiens (human)Kd30.000011
azd 1480Homo sapiens (human)Kd30.000011
azd8330Homo sapiens (human)Kd30.000011
pha 848125Homo sapiens (human)Kd30.000011
ro5126766Homo sapiens (human)Kd30.000012
fedratinibHomo sapiens (human)Kd30.000011
gsk690693Homo sapiens (human)Kd30.000011
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-decaeneHomo sapiens (human)Kd5.635011
azd5438Homo sapiens (human)Kd30.000011
pf 04217903Homo sapiens (human)Kd30.000011
gdc 0941Homo sapiens (human)Kd30.000011
icotinibHomo sapiens (human)Kd30.000011
ph 797804Homo sapiens (human)Kd30.000011
kx-01Homo sapiens (human)Kd30.000011
mk 5108Homo sapiens (human)Kd30.000011
cx 4945Homo sapiens (human)Kd30.000011
cudc 101Homo sapiens (human)Kd30.000012
arry-614Homo sapiens (human)Kd30.000011
tak 593Homo sapiens (human)Kd30.000011
mln 8237Homo sapiens (human)Kd30.000011
sgx 523Homo sapiens (human)Kd30.000011
bms 754807Homo sapiens (human)Kd30.000011
bms 777607Homo sapiens (human)Kd30.000011
sgi 1776Homo sapiens (human)Kd30.000012
pci 32765Homo sapiens (human)Kd30.000011
ponatinibHomo sapiens (human)Kd30.000011
amg 900Homo sapiens (human)Kd2.977011
mk-1775Homo sapiens (human)Kd30.000011
AMG-208Homo sapiens (human)Kd30.000011
quizartinibHomo sapiens (human)Kd30.000011
at13148Homo sapiens (human)Kd30.000011
tak 733Homo sapiens (human)Kd30.000011
mk 2206Homo sapiens (human)Kd30.000011
sns 314Homo sapiens (human)Kd30.000011
lucitanibHomo sapiens (human)Kd30.000011
pf-04691502Homo sapiens (human)Kd30.000011
n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamideHomo sapiens (human)Kd30.000011
dcc-2036Homo sapiens (human)Kd30.000011
cabozantinibHomo sapiens (human)Kd30.000011
defactinibHomo sapiens (human)Kd0.730011
ly2584702Homo sapiens (human)Kd30.000011
incb-018424Homo sapiens (human)Kd30.000011
poziotinibHomo sapiens (human)Kd30.000011
asp3026Homo sapiens (human)Kd30.000011
entrectinibHomo sapiens (human)Kd30.000011
pexidartinibHomo sapiens (human)Kd30.000011
TAK-580Homo sapiens (human)Kd30.000011
gsk 2126458Homo sapiens (human)Kd30.000011
emd1214063Homo sapiens (human)Kd30.000011
pf 3758309Homo sapiens (human)Kd30.000011
gdc 0980Homo sapiens (human)Kd30.000011
azd2014Homo sapiens (human)Kd30.000011
(5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanolHomo sapiens (human)Kd30.000011
plx4032Homo sapiens (human)Kd30.000011
gsk 1363089Homo sapiens (human)Kd30.000011
arry-334543Homo sapiens (human)Kd30.000011
kin-193Homo sapiens (human)Kd30.000011
mk 2461Homo sapiens (human)Kd30.000011
bay 869766Homo sapiens (human)Kd30.000011
as 703026Homo sapiens (human)Kd30.000011
baricitinibHomo sapiens (human)Kd30.000011
dabrafenibHomo sapiens (human)Kd30.000011
pki 587Homo sapiens (human)Kd30.000011
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-carboxamideHomo sapiens (human)Kd30.000011
ribociclibHomo sapiens (human)Kd30.000012
mk-8033Homo sapiens (human)Kd30.000012
pha 793887Homo sapiens (human)Kd3.657011
sb 1518Homo sapiens (human)Kd30.000011
abemaciclibHomo sapiens (human)Kd30.000011
mk-8776Homo sapiens (human)Kd30.000011
afuresertibHomo sapiens (human)Kd30.000011
gsk 1070916Homo sapiens (human)Kd30.000011
jnj38877605Homo sapiens (human)Kd30.000011
dinaciclibHomo sapiens (human)Kd0.032011
gilteritinibHomo sapiens (human)Kd30.000011
alectinibHomo sapiens (human)Kd30.000011
glpg0634Homo sapiens (human)Kd30.000011
encorafenibHomo sapiens (human)Kd30.000011
bms-911543Homo sapiens (human)Kd30.000011
gsk2141795Homo sapiens (human)Kd30.000011
azd8186Homo sapiens (human)Kd30.000011
byl719Homo sapiens (human)Kd30.000011
cep-32496Homo sapiens (human)Kd30.000011
rociletinibHomo sapiens (human)Kd30.000011
ceritinibHomo sapiens (human)Kd30.000011
azd1208Homo sapiens (human)Kd30.000011
vx-509Homo sapiens (human)Kd30.000011
debio 1347Homo sapiens (human)Kd30.000011
volitinibHomo sapiens (human)Kd30.000011
osimertinibHomo sapiens (human)Kd30.000011
at 9283Homo sapiens (human)Kd30.000011
otssp167Homo sapiens (human)Kd30.000011
chir 258Homo sapiens (human)Kd30.000011
osi 027Homo sapiens (human)Kd30.000011
nintedanibHomo sapiens (human)Kd30.000012
bay 80-6946Homo sapiens (human)Kd30.000011

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
cyc 202Homo sapiens (human)INH24.500011
olomoucine iiHomo sapiens (human)INH11.400011

Enables

This protein enables 8 target(s):

TargetCategoryDefinition
protein kinase activitymolecular functionCatalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640]
cyclin-dependent protein serine/threonine kinase activitymolecular functionCyclin-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]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
ATP bindingmolecular functionBinding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732]
RNA polymerase II CTD heptapeptide repeat kinase activitymolecular functionCatalysis 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 kinase bindingmolecular functionBinding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl]
cyclin bindingmolecular functionBinding to cyclins, proteins whose levels in a cell varies markedly during the cell cycle, rising steadily until mitosis, then falling abruptly to zero. As cyclins reach a threshold level, they are thought to drive cells into G2 phase and thus to mitosis. [GOC:ai]
protein serine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]

Located In

This protein is located in 2 target(s):

TargetCategoryDefinition
nucleoplasmcellular componentThat part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653]
nuclear speckcellular componentA discrete extra-nucleolar subnuclear domain, 20-50 in number, in which splicing factors are seen to be localized by immunofluorescence microscopy. [http://www.cellnucleus.com/]

Active In

This protein is active in 1 target(s):

TargetCategoryDefinition
nucleuscellular componentA 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 3 target(s):

TargetCategoryDefinition
cyclin K-CDK12 complexcellular componentA protein complex consisting of cyclin Kand cyclin-dependent kinase 12 (CDK12). Cyclins are characterized by periodicity in protein abundance throughout the cell cycle. Cyclin-dependent kinases represent a family of serine/threonine protein kinases that become active upon binding to a cyclin regulatory partner. [PMID:22012619]
nuclear cyclin-dependent protein kinase holoenzyme complexcellular componentCyclin-dependent protein kinase (CDK) complex found in the nucleus. [GOC:krc]
cyclin/CDK positive transcription elongation factor complexcellular componentA transcription elongation factor complex that facilitates the transition from abortive to productive elongation by phosphorylating the CTD domain of the large subunit of DNA-directed RNA polymerase II, holoenzyme. Contains a cyclin and a cyclin-dependent protein kinase catalytic subunit. [GOC:bhm, GOC:vw, PMID:10766736, PMID:16721054, PMID:17079683, PMID:19328067, PMID:7759473]

Involved In

This protein is involved in 10 target(s):

TargetCategoryDefinition
transcription by RNA polymerase IIbiological processThe 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]
mRNA processingbiological processAny process involved in the conversion of a primary mRNA transcript into one or more mature mRNA(s) prior to translation into polypeptide. [GOC:mah]
RNA splicingbiological processThe process of removing sections of the primary RNA transcript to remove sequences not present in the mature form of the RNA and joining the remaining sections to form the mature form of the RNA. [GOC:krc, GOC:mah]
positive regulation of transcription elongation by RNA polymerase IIbiological processAny process that activates or increases the frequency, rate or extent of transcription elongation, the extension of an RNA molecule after transcription initiation and promoter clearance by the addition of ribonucleotides, catalyzed by RNA polymerase II. [GOC:mah, GOC:txnOH]
regulation of MAP kinase activitybiological processAny process that modulates the frequency, rate or extent of MAP kinase activity. [GOC:dph, GOC:go_curators]
positive regulation of transcription by RNA polymerase IIbiological processAny process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH]
protein autophosphorylationbiological processThe phosphorylation by a protein of one or more of its own amino acid residues (cis-autophosphorylation), or residues on an identical protein (trans-autophosphorylation). [ISBN:0198506732]
regulation of cell cyclebiological processAny process that modulates the rate or extent of progression through the cell cycle. [GOC:ai, GOC:dph, GOC:tb]
negative regulation of stem cell differentiationbiological processAny process that stops, prevents or reduces the frequency, rate or extent of stem cell differentiation. [GOC:obol]
protein phosphorylationbiological processThe process of introducing a phosphate group on to a protein. [GOC:hb]