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PsychedeliaDokholyan Laboratory
TargetEnzymes

Serine/threonine-protein kinase pim-3

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

Measurements
6
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

PIM3_HUMANPIM3Homo sapiens

Serine/threonine-protein kinase pim-3

Proto-oncogene with serine/threonine kinase activity that can prevent apoptosis, promote cell survival and protein translation. May contribute to tumorigenesis through: the delivery of survival signaling through phosphorylation of BAD which induces release of the anti-apoptotic protein Bcl-X(L), the regulation of cell cycle progression, protein synthesis and by regulation of MYC transcriptional activity. Additionally to this role on tumorigenesis, can also negatively regulate insulin secretion by inhibiting the activation of MAPK1/3 (ERK1/2), through SOCS6. Involved also in the control of energy metabolism and regulation of AMPK activity in modulating MYC and PPARGC1A protein levels and cell growth

Quoted from UniProt’s FUNCTION annotation for Q86V86 (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
SHANK30.7050.1150.0000.671
RABL2B0.6200.1070.0000.572
RABL2A0.6080.1070.0000.551
ALG120.5940.0000.0000.585
BCL2L10.5860.0000.0000.578
HASPIN0.5620.0000.0000.562
IL20.5280.0000.0000.520
EWSR10.5100.0000.0000.509
SMARCB10.5010.0530.0000.495
PIM20.4630.0510.0000.403

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

Expression by cell type

Single cell type RNA, the 4 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Extravillous trophoblasts461.2 nCPM
  • Syncytiotrophoblasts458.3 nCPM
  • Prostatic club cells352.4 nCPM
  • Esophageal apical cells317.7 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

cerebral cortex — 26.5 nTPM, from PIM3cerebellum — 28.1 nTPM, from PIM3hippocampal formation — 28.4 nTPM, from PIM3amygdala — 21.3 nTPM, from PIM3hypothalamus — 29.7 nTPM, from PIM3thalamus — no resolved target expressed herebasal ganglia — 29.1 nTPM, from PIM3medulla oblongata — no resolved target expressed here

basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.

Measured but not drawn — this anatomogram has no outline for them: pituitary gland 56.6, midbrain 32.1, spinal cord 29.1, retina 2.9.

Body

heart — 73.8 nTPM, from PIM3smooth muscle — 9.2 nTPM, from PIM3lung — 117.8 nTPM, from PIM3liver — 99.4 nTPM, from PIM3kidney — 120.4 nTPM, from PIM3stomach — 129.1 nTPM, from PIM3duodenum — 22.4 nTPM, from PIM3small intestine — 55.5 nTPM, from PIM3colon — 59.9 nTPM, from PIM3adrenal gland — 54.1 nTPM, from PIM3thyroid gland — 59.9 nTPM, from PIM3pancreas — 80.2 nTPM, from PIM3urinary bladder — 82.2 nTPM, from PIM3skeletal muscle — 122.0 nTPM, from PIM3spleen — 88.0 nTPM, from PIM3salivary gland — 102.9 nTPM, from PIM3
0129 nTPM

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 PIM3 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 gland56.6 nTPM
  • midbrain32.1 nTPM
  • hypothalamus29.7 nTPM
  • basal ganglia29.1 nTPM
  • spinal cord29.1 nTPM
  • hippocampal formation28.4 nTPM
  • cerebellum28.1 nTPM
  • cerebral cortex26.5 nTPM
  • amygdala21.3 nTPM
  • retina2.9 nTPM

Peripheral and autonomic · 16

  • stomach 1129.1 nTPM
  • skeletal muscle122.0 nTPM
  • kidney120.4 nTPM
  • lung117.8 nTPM
  • salivary gland102.9 nTPM
  • liver99.4 nTPM
  • spleen88.0 nTPM
  • urinary bladder82.2 nTPM
  • pancreas80.2 nTPM
  • heart muscle73.8 nTPM
  • colon59.9 nTPM
  • thyroid gland59.9 nTPM
  • small intestine55.5 nTPM
  • adrenal gland54.1 nTPM
  • duodenum22.4 nTPM
  • smooth muscle9.2 nTPM

Transcript is not protein. These are RNA levels for PIM3, 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.

Functional readouts 2

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Serine/threonine-protein kinase pim-3EnzymesIC504,3005.37Homo sapiensCHEMBL1062887
Serine/threonine-protein kinase pim-3EnzymesIC504,3005.37Homo sapiensCHEMBL5235556

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
Serine/threonine-protein kinase pim-3EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1061912
Serine/threonine-protein kinase pim-3EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1061912
Serine/threonine-protein kinase pim-3EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1061912
Serine/threonine-protein kinase pim-3EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1061912
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