Calcium/calmodulin-dependent protein kinase kinase 1

A calcium/calmodulin-dependent protein kinase kinase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8N5S9]

Synonyms

CaM-KK 1;
CaM-kinase kinase 1;
CaMKK 1;
EC 2.7.11.17;
CaM-kinase IV kinase;
Calcium/calmodulin-dependent protein kinase kinase alpha;
CaM-KK alpha;
CaM-kinase kinase alpha;
CaMKK alpha

Research

Bioassay Publications (7)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	3 (42.86)	29.6817
2010's	3 (42.86)	24.3611
2020's	1 (14.29)	2.80

Compounds (76)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
staurosporine	Homo sapiens (human)	IC50	0.0359	2	2
gsk 650394	Homo sapiens (human)	IC50	0.0330	1	1

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
sb 202190	Homo sapiens (human)	Kd	10.0000	1	1
imatinib	Homo sapiens (human)	Kd	10.0000	2	2
staurosporine	Homo sapiens (human)	Kd	0.0000	3	3
gefitinib	Homo sapiens (human)	Kd	10.0000	2	2
lestaurtinib	Homo sapiens (human)	Kd	0.0230	2	2
vatalanib	Homo sapiens (human)	Kd	10.0000	2	2
ruboxistaurin	Homo sapiens (human)	Kd	3.8333	3	3
canertinib	Homo sapiens (human)	Kd	10.0000	2	2
birb 796	Homo sapiens (human)	Kd	10.0000	2	2
cyc 202	Homo sapiens (human)	Kd	10.0000	1	1
sb 203580	Homo sapiens (human)	Kd	10.0000	2	2
enzastaurin	Homo sapiens (human)	Kd	10.0000	1	1
erlotinib	Homo sapiens (human)	Kd	10.0000	2	2
lapatinib	Homo sapiens (human)	Kd	10.0000	2	2
sorafenib	Homo sapiens (human)	Kd	10.0000	3	3
pd 173955	Homo sapiens (human)	Kd	10.0000	1	1
s 1033	Homo sapiens (human)	Kd	10.0000	1	1
bms 387032	Homo sapiens (human)	Kd	10.0000	2	2
tandutinib	Homo sapiens (human)	Kd	10.0000	3	3
vx-745	Homo sapiens (human)	Kd	10.0000	2	2
dasatinib	Homo sapiens (human)	Kd	10.0000	2	2
zd 6474	Homo sapiens (human)	Kd	10.0000	2	2
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
alvocidib	Homo sapiens (human)	Kd	0.0590	3	3
bosutinib	Homo sapiens (human)	Kd	10.0000	1	1
su 11248	Homo sapiens (human)	Kd	0.5400	4	4
jnj-7706621	Homo sapiens (human)	Kd	2.9000	1	1
vx680	Homo sapiens (human)	Kd	7.3000	2	2
ekb 569	Homo sapiens (human)	Kd	5.1000	1	1
axitinib	Homo sapiens (human)	Kd	1.4000	1	1
pd 184352	Homo sapiens (human)	Kd	10.0000	1	1
bms345541	Homo sapiens (human)	Kd	10.0000	1	1
midostaurin	Homo sapiens (human)	Kd	0.1300	3	3
ki 20227	Homo sapiens (human)	Kd	10.0000	1	1
cp 724714	Homo sapiens (human)	Kd	10.0000	1	1
pi103	Homo sapiens (human)	Kd	10.0000	2	2
hki 272	Homo sapiens (human)	Kd	10.0000	1	1
tofacitinib	Homo sapiens (human)	Kd	10.0000	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	10.0000	1	1
masitinib	Homo sapiens (human)	Kd	10.0000	1	1
pazopanib	Homo sapiens (human)	Kd	10.0000	2	2
azd 6244	Homo sapiens (human)	Kd	10.0000	1	1
su 14813	Homo sapiens (human)	Kd	0.8500	2	2
bibw 2992	Homo sapiens (human)	Kd	10.0000	1	1
tg100-115	Homo sapiens (human)	Kd	10.0000	1	1
pha 665752	Homo sapiens (human)	Kd	0.0640	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	10.0000	1	1
brivanib	Homo sapiens (human)	Kd	10.0000	1	1
at 7519	Homo sapiens (human)	Kd	10.0000	1	1
bi 2536	Homo sapiens (human)	Kd	0.0220	1	1
nvp-ast487	Homo sapiens (human)	Kd	0.2200	2	2
kw 2449	Homo sapiens (human)	Kd	0.2100	1	1
abt 869	Homo sapiens (human)	Kd	10.0000	2	2
gw 2580	Homo sapiens (human)	Kd	10.0000	2	2
crizotinib	Homo sapiens (human)	Kd	10.0000	1	1
chir-265	Homo sapiens (human)	Kd	10.0000	2	2
motesanib	Homo sapiens (human)	Kd	10.0000	2	2
mln8054	Homo sapiens (human)	Kd	10.0000	2	2
GDC-0879	Homo sapiens (human)	Kd	10.0000	1	1
gsk 461364	Homo sapiens (human)	Kd	10.0000	1	1
azd 1152-hqpa	Homo sapiens (human)	Kd	10.0000	2	2
nvp-tae684	Homo sapiens (human)	Kd	0.0500	1	1
fedratinib	Homo sapiens (human)	Kd	1.8000	1	1
gsk690693	Homo sapiens (human)	Kd	10.0000	1	1
gdc 0941	Homo sapiens (human)	Kd	10.0000	1	1
plx 4720	Homo sapiens (human)	Kd	10.0000	1	1
sgx 523	Homo sapiens (human)	Kd	10.0000	1	1
quizartinib	Homo sapiens (human)	Kd	10.0000	2	2
incb-018424	Homo sapiens (human)	Kd	10.0000	1	1
gsk 1838705a	Homo sapiens (human)	Kd	10.0000	1	1
gsk 1363089	Homo sapiens (human)	Kd	0.5500	1	1
chir 258	Homo sapiens (human)	Kd	3.1000	2	2
nintedanib	Homo sapiens (human)	Kd	0.6300	1	1
pp242	Homo sapiens (human)	Kd	10.0000	1	1

Enables

This protein enables 5 target(s):

Target	Category	Definition
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]
protein serine kinase activity	molecular function	Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]
calmodulin-dependent protein kinase activity	molecular function	Calmodulin-dependent catalysis of the reactions: ATP + a protein serine = ADP + protein serine phosphate; and ATP + a protein threonine = ADP + protein threonine phosphate. [GOC:mah, PMID:11264466]
calmodulin binding	molecular function	Binding to calmodulin, a calcium-binding protein with many roles, both in the calcium-bound and calcium-free states. [GOC:krc]

Located In

This protein is located in 2 target(s):

Target	Category	Definition
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]

Active In

This protein is active in 1 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]

Involved In

This protein is involved in 1 target(s):

Target	Category	Definition
intracellular signal transduction	biological process	The process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782]

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