Serine/threonine-protein kinase pim-1
Named enzymes, including the metabolising cytochromes and the monoamine oxidases.
- Measurements
- 8
- Compounds
- 5
- Binding constants
- 1
- 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.
Serine/threonine-protein kinase pim-1
Proto-oncogene with serine/threonine kinase activity involved in cell survival and cell proliferation and thus providing a selective advantage in tumorigenesis15528381,1825810,31548394. Exerts its oncogenic activity through: the regulation of MYC transcriptional activity, the regulation of cell cycle progression and by phosphorylation and inhibition of proapoptotic proteins (BAD, MAP3K5, FOXO3)18593906. Phosphorylation of MYC leads to an increase of MYC protein stability and thereby an increase of transcriptional activity (By similarity). The stabilization of MYC exerted by PIM1 might explain partly the strong synergism between these two oncogenes in tumorigenesis (By similarity). Mediates survival signaling through phosphorylation of BAD, which induces release of the anti-apoptotic protein Bcl-X(L)/BCL2L1 (By similarity). Phosphorylation of MAP3K5, another proapoptotic protein, by PIM1, significantly decreases MAP3K5 kinase activity and inhibits MAP3K5-mediated phosphorylation of JNK and JNK/p38MAPK subsequently reducing caspase-3 activation and cell apoptosis19749799. Stimulates cell cycle progression at the G1-S and G2-M transitions by phosphorylation of CDC25A and CDC25C16356754. Phosphorylation of CDKN1A, a regulator of cell cycle progression at G1, results in the relocation of CDKN1A to the cytoplasm and enhanced CDKN1A protein stability12431783. Promotes cell cycle progression and tumorigenesis by down-regulating expression of a regulator of cell cycle progression, CDKN1B, at both transcriptional and post-translational levels18593906. Phosphorylation of CDKN1B, induces 14-3-3 proteins binding, nuclear export and proteasome-dependent degradation18593906. May affect the structure or silencing of chromatin by phosphorylating HP1 gamma/CBX310664448. Also acts as a regulator of homing and migration of bone marrow cells involving functional interaction with the CXCL12-CXCR4 signaling axis (By similarity). Acts as a positive regulator of mTORC1 signaling by mediating phosphorylation and inhibition of DEPDC5 component of the GATOR1 complex31548394. Acts as a negative regulator of innate immunity by mediating phosphorylation and inactivation of GBP1 in absence of infection: phosphorylation of GBP1 induces interaction with 14-3-3 protein sigma (SFN) and retention in the cytosol37797010. Also phosphorylates and activates the ATP-binding cassette transporter ABCG2, allowing resistance to drugs through their excretion from cells18056989. Promotes brown adipocyte differentiation (By similarity)
Quoted from UniProt’s FUNCTION annotation for P11309 (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
- Cytosol
- Nucleoplasmadditional
- Nucleoliadditional
Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.
UniProt, curated Cytoplasm · Nucleus · Cell membrane
Expression by cell type
Single cell type RNA, the 1 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.
- Esophageal apical cells1,769.1 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.
- bone marrow206.5 nTPM
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: pituitary gland 13.8, spinal cord 11.0, midbrain 10.3, retina 7.6.
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 PIM1 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
- pituitary gland13.8 nTPM
- cerebellum11.8 nTPM
- spinal cord11.0 nTPM
- midbrain10.3 nTPM
- hypothalamus9.8 nTPM
- hippocampal formation7.8 nTPM
- retina7.6 nTPM
- amygdala7.5 nTPM
- basal ganglia7.5 nTPM
- cerebral cortex7.2 nTPM
Peripheral and autonomic · 16
- urinary bladder94.7 nTPM
- heart muscle61.5 nTPM
- spleen58.1 nTPM
- liver55.9 nTPM
- lung47.1 nTPM
- colon42.6 nTPM
- small intestine40.9 nTPM
- salivary gland37.5 nTPM
- stomach 136.9 nTPM
- duodenum36.9 nTPM
- smooth muscle35.5 nTPM
- skeletal muscle34.0 nTPM
- kidney24.7 nTPM
- thyroid gland21.4 nTPM
- pancreas19.2 nTPM
- adrenal gland13.6 nTPM
Transcript is not protein. These are RNA levels for PIM1, 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 1
Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Serine/threonine-protein kinase pim-1 | Enzymes | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1963726 |
Functional readouts 2
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Serine/threonine-protein kinase pim-1 | Enzymes | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5235555 |
| Serine/threonine-protein kinase pim-1 | Enzymes | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL2187125 |
Other measurements 5
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 |
|---|---|---|---|---|---|---|
| Serine/threonine-protein kinase pim-1 | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1063736 |
| Serine/threonine-protein kinase pim-1 | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1063736 |
| Serine/threonine-protein kinase pim-1 | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1063736 |
| Serine/threonine-protein kinase pim-1 | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1063736 |
| Serine/threonine-protein kinase pim-1 | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4151471 |