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TargetEnzymes

Ribosomal protein S6 kinase alpha-4

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

Measurements
1
Compounds
1
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

KS6A4_HUMANRPS6KA4Homo sapiens

Ribosomal protein S6 kinase alpha-4

Serine/threonine-protein kinase that is required for the mitogen or stress-induced phosphorylation of the transcription factors CREB1 and ATF1 and for the regulation of the transcription factor RELA, and that contributes to gene activation by histone phosphorylation and functions in the regulation of inflammatory genes. Phosphorylates CREB1 and ATF1 in response to mitogenic or stress stimuli such as UV-C irradiation, epidermal growth factor (EGF) and anisomycin. Plays an essential role in the control of RELA transcriptional activity in response to TNF. Phosphorylates 'Ser-10' of histone H3 in response to mitogenics, stress stimuli and EGF, which results in the transcriptional activation of several immediate early genes, including proto-oncogenes c-fos/FOS and c-jun/JUN. May also phosphorylate 'Ser-28' of histone H3. Mediates the mitogen- and stress-induced phosphorylation of high mobility group protein 1 (HMGN1/HMG14). In lipopolysaccharide-stimulated primary macrophages, acts downstream of the Toll-like receptor TLR4 to limit the production of pro-inflammatory cytokines. Functions probably by inducing transcription of the MAP kinase phosphatase DUSP1 and the anti-inflammatory cytokine interleukin 10 (IL10), via CREB1 and ATF1 transcription factors

Quoted from UniProt’s FUNCTION annotation for O75676 (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
MAPK140.9840.7920.9000.249
MAPK110.9330.2030.9000.129
MAPK130.9170.0750.9000.150
MAPK120.9150.0750.9000.122
RPS6KA50.9040.0000.9000.070
ATF40.9000.0000.9000.000
CREB10.8910.2920.6500.561
ATF20.7080.0510.6500.184
ATF6B0.7000.0000.6500.160
CREB50.6720.0460.6500.089

Where it sits in the cell

  • Nucleoplasm
  • Cytosoladditional

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

UniProt, curated Nucleus

Expression by cell type

Single cell type RNA, the 5 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • pDCs133.1 nCPM
  • Migrating cytotrophoblasts87.7 nCPM
  • Cytotrophoblasts85.6 nCPM
  • Alveolar cells type 148.5 nCPM
  • Syncytiotrophoblasts48 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.

  • brain54.3 nTPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Other measurements 1

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
Ribosomal protein S6 kinase alpha-4EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL4151474