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TargetEnzymes

Calcium/calmodulin-dependent protein kinase type 1

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
4
Compounds
4
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

KCC1A_HUMANCAMK1Homo sapiens

Calcium/calmodulin-dependent protein kinase type 1

Calcium/calmodulin-dependent protein kinase that operates in the calcium-triggered CaMKK-CaMK1 signaling cascade and, upon calcium influx, regulates transcription activators activity, cell cycle, hormone production, cell differentiation, actin filament organization and neurite outgrowth. Recognizes the substrate consensus sequence [MVLIF]-x-R-x(2)-[ST]-x(3)-[MVLIF]. Regulates axonal extension and growth cone motility in hippocampal and cerebellar nerve cells. Upon NMDA receptor-mediated Ca(2+) elevation, promotes dendritic growth in hippocampal neurons and is essential in synapses for full long-term potentiation (LTP) and ERK2-dependent translational activation. Downstream of NMDA receptors, promotes the formation of spines and synapses in hippocampal neurons by phosphorylating ARHGEF7/BETAPIX on 'Ser-694', which results in the enhancement of ARHGEF7 activity and activation of RAC1. Promotes neuronal differentiation and neurite outgrowth by activation and phosphorylation of MARK2 on 'Ser-91', 'Ser-92', 'Ser-93' and 'Ser-294'. Promotes nuclear export of HDAC5 and binding to 14-3-3 by phosphorylation of 'Ser-259' and 'Ser-498' in the regulation of muscle cell differentiation. Regulates NUMB-mediated endocytosis by phosphorylation of NUMB on 'Ser-276' and 'Ser-295'. Involved in the regulation of basal and estrogen-stimulated migration of medulloblastoma cells through ARHGEF7/BETAPIX phosphorylation (By similarity). Is required for proper activation of cyclin-D1/CDK4 complex during G1 progression in diploid fibroblasts. Plays a role in K(+) and ANG2-mediated regulation of the aldosterone synthase (CYP11B2) to produce aldosterone in the adrenal cortex. Phosphorylates EIF4G3/eIF4GII. In vitro phosphorylates CREB1, ATF1, CFTR, MYL9 and SYN1/synapsin I

Quoted from UniProt’s FUNCTION annotation for Q14012 (reviewed).

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
CALM30.9980.9520.6500.916
CALM10.9820.9360.7000.155
CALM20.9690.9330.0000.545
CALML30.9580.2750.6500.844
CALML50.9560.2460.6500.844
CALML40.9490.1290.6500.844
CALML60.9460.1290.6500.833
NOS30.9360.0740.9000.353
CREB10.8630.0950.6500.602
PPM1F0.8130.0810.7500.246

Where it sits in the cell

  • Cytosol

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cytoplasm · Nucleus

Expression by cell type

Single cell type RNA, the 3 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Megakaryocytes333.8 nCPM
  • Adrenal cortex cells105.6 nCPM
  • Sertoli cells76.6 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • adrenal gland99.5 nTPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Other measurements 4

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Calcium/calmodulin-dependent protein kinase type 1EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1051272
Calcium/calmodulin-dependent protein kinase type 1EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1051272
Calcium/calmodulin-dependent protein kinase type 1EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1051272
Calcium/calmodulin-dependent protein kinase type 1EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1051272