Mitogen-activated protein kinase 3
Named enzymes, including the metabolising cytochromes and the monoamine oxidases.
- Measurements
- 18
- Compounds
- 11
- Binding constants
- 7
- 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.
Mitogen-activated protein kinase 3
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway34497368. MAPK1/ERK2 and MAPK3/ERK1 are the 2 MAPKs which play an important role in the MAPK/ERK cascade. They participate also in a signaling cascade initiated by activated KIT and KITLG/SCF. Depending on the cellular context, the MAPK/ERK cascade mediates diverse biological functions such as cell growth, adhesion, survival and differentiation through the regulation of transcription, translation, cytoskeletal rearrangements. The MAPK/ERK cascade also plays a role in initiation and regulation of meiosis, mitosis, and postmitotic functions in differentiated cells by phosphorylating a number of transcription factors. About 160 substrates have already been discovered for ERKs. Many of these substrates are localized in the nucleus, and seem to participate in the regulation of transcription upon stimulation. However, other substrates are found in the cytosol as well as in other cellular organelles, and those are responsible for processes such as translation, mitosis and apoptosis. Moreover, the MAPK/ERK cascade is also involved in the regulation of the endosomal dynamics, including lysosome processing and endosome cycling through the perinuclear recycling compartment (PNRC); as well as in the fragmentation of the Golgi apparatus during mitosis. The substrates include transcription factors (such as ATF2, BCL6, ELK1, ERF, FOS, HSF4 or SPZ1), cytoskeletal elements (such as CANX, CTTN, GJA1, MAP2, MAPT, PXN, SORBS3 or STMN1), regulators of apoptosis (such as BAD, BTG2, CASP9, DAPK1, IER3, MCL1 or PPARG), regulators of translation (such as EIF4EBP1) and a variety of other signaling-related molecules (like ARHGEF2, DEPTOR, FRS2 or GRB10)35216969. Protein kinases (such as RAF1, RPS6KA1/RSK1, RPS6KA3/RSK2, RPS6KA2/RSK3, RPS6KA6/RSK4, SYK, MKNK1/MNK1, MKNK2/MNK2, RPS6KA5/MSK1, RPS6KA4/MSK2, MAPKAPK3 or MAPKAPK5) and phosphatases (such as DUSP1, DUSP4, DUSP6 or DUSP16) are other substrates which enable the propagation the MAPK/ERK signal to additional cytosolic and nuclear targets, thereby extending the specificity of the cascade. Phosphorylates GJA1 at 'Ser-279' and 'Ser-282' resulting in an increase in GJA1 ubiquitination and ultimately lysosomal degradation (By similarity)
Quoted from UniProt’s FUNCTION annotation for P27361 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.
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.
Where it sits in the cell
- Nucleoplasm
- Microtubulesadditional
- Primary ciliumadditional
- Primary cilium tipadditional
- Basal bodyadditional
- Cytosoladditional
Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.
UniProt, curated Cytoplasm · Nucleus · Membrane, caveola · Cell junction, focal adhesion
Expression by cell type
Single cell type RNA, the 8 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.
- Esophageal apical cells543.4 nCPM
- Early spermatids326.3 nCPM
- Colonocytes268.7 nCPM
- Late spermatids229.8 nCPM
- Enterocytes226.1 nCPM
- Goblet cells190 nCPM
- Extravillous trophoblasts188 nCPM
- Foveolar cells172.9 nCPM
II · Anatomy
Where the gene is transcribed
The same two atlases the compound plates use, asked about this gene alone. Brain on the left, peripheral and autonomic tissues on the right.
Brain
basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.
Measured but not drawn — this anatomogram has no outline for them: midbrain 120.0, spinal cord 103.1, retina 66.4, pituitary gland 51.6.
Body
Square-root ramp · shared scale across both plates
Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of MAPK3 transcript above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.
Brain · 10
- amygdala233.4 nTPM
- cerebral cortex222.5 nTPM
- basal ganglia154.0 nTPM
- hippocampal formation140.7 nTPM
- midbrain120.0 nTPM
- hypothalamus117.0 nTPM
- spinal cord103.1 nTPM
- cerebellum87.3 nTPM
- retina66.4 nTPM
- pituitary gland51.6 nTPM
Peripheral and autonomic · 16
- colon109.7 nTPM
- small intestine106.5 nTPM
- duodenum96.9 nTPM
- stomach 181.5 nTPM
- lung68.1 nTPM
- heart muscle63.5 nTPM
- adrenal gland61.4 nTPM
- urinary bladder61.3 nTPM
- salivary gland57.0 nTPM
- thyroid gland55.8 nTPM
- spleen55.0 nTPM
- smooth muscle54.8 nTPM
- kidney50.1 nTPM
- skeletal muscle49.0 nTPM
- pancreas31.8 nTPM
- liver20.3 nTPM
Transcript is not protein. These are RNA levels for MAPK3, shaded on √nTPM so that a three-order range stays legible — on a linear ramp every region but the strongest would read as blank, which looks like absence rather than less. A region carrying no shading is one the atlas reports no consensus value for, not one where the gene is silent. And a gene being transcribed somewhere is not evidence that any compound reaches it. Human Protein Atlas, RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset.
IV · Evidence
Every measurement at this target
Each row links to the ChEMBL assay it came from.
Equilibrium binding constants 7
Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Mitogen-activated protein kinase 3 | Enzymes | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909199 |
| Mitogen-activated protein kinase 3 | Enzymes | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909199 |
| Mitogen-activated protein kinase 3 | Enzymes | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909199 |
| Mitogen-activated protein kinase 3 | Enzymes | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909199 |
| Mitogen-activated protein kinase 3 | Enzymes | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909199 |
| Mitogen-activated protein kinase 3 | Enzymes | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909199 |
| Mitogen-activated protein kinase 3 | Enzymes | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909199 |
Functional readouts 7
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Mitogen-activated protein kinase 3 | Enzymes | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909199 |
| Mitogen-activated protein kinase 3 | Enzymes | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909199 |
| Mitogen-activated protein kinase 3 | Enzymes | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909199 |
| Mitogen-activated protein kinase 3 | Enzymes | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909199 |
| Mitogen-activated protein kinase 3 | Enzymes | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909199 |
| Mitogen-activated protein kinase 3 | Enzymes | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909199 |
| Mitogen-activated protein kinase 3 | Enzymes | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909199 |
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.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Mitogen-activated protein kinase 3 | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1061959 |
| Mitogen-activated protein kinase 3 | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1061959 |
| Mitogen-activated protein kinase 3 | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1061959 |
| Mitogen-activated protein kinase 3 | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1061959 |