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PsychedeliaDokholyan Laboratory
TargetOther named receptors

Substance-K receptor

A named receptor outside the families above. The catch-all is explicit rather than silent: these are receptors, but they are not grouped.

Measurements
15
Compounds
8
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.

Protein

NK2R_HUMANTACR2Homo sapiens

Substance-K receptor

This is a receptor for the tachykinin neuropeptide substance K (neurokinin A)1659297,1848773. Is also able to bind and respond to tachynins substance P and neurokinin B/neuromedin-K (By similarity). The rank order of affinity of this receptor to tachykinins is: substance K > neuromedin-K > substance P (By similarity). Substance K binding to its receptor triggers G protein-coupled receptor signaling via activation of G(q) and phosphatidylinositol hydrolysis by phospholipase C7957923,35882833. Substance K binding also triggers signaling via activation of adenylate cyclase activity which results in increased intracellular levels of cyclic AMP (cAMP) (By similarity)

Quoted from UniProt’s FUNCTION annotation for P21452 (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.

PartnerCombinedExperimentDatabaseText mining
TAC10.9990.9940.9000.998
TAC30.9980.2920.0000.998
TAC40.9310.2920.0000.906
CHKB0.7610.0000.0000.761
GNAQ0.7080.0680.6500.177
GNA150.6780.0660.6500.096
GNA140.6740.0680.6500.075
GNA110.6640.0680.6500.053
MAS10.5930.0450.0000.586
AASDHPPT0.5740.0000.0000.574

Where it sits in the cell

  • Plasma membrane

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

UniProt, curated Cell membrane

Expression by cell type

Single cell type RNA, the 6 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Smooth muscle cells43.6 nCPM
  • Tuft cells11.5 nCPM
  • Retinal horizontal cells10 nCPM
  • Cardiomyocytes9.7 nCPM
  • Epicardial cells6.8 nCPM
  • Hepatic stellate cells6.5 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.

  • intestine134.1 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

cerebral cortex — 1.5 nTPM, from TACR2cerebellum — 0.9 nTPM, from TACR2hippocampal formation — 0.9 nTPM, from TACR2amygdala — 1.1 nTPM, from TACR2hypothalamus — 0.7 nTPM, from TACR2thalamus — no resolved target expressed herebasal ganglia — 1.3 nTPM, from TACR2medulla 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: retina 3.8, midbrain 0.6, spinal cord 0.3, pituitary gland 0.2.

Body

heart — 3.0 nTPM, from TACR2smooth muscle — 30.9 nTPM, from TACR2lung — 0.6 nTPM, from TACR2liver — 0.5 nTPM, from TACR2kidney — 0.3 nTPM, from TACR2stomach — 27.3 nTPM, from TACR2duodenum — 4.6 nTPM, from TACR2small intestine — 23.4 nTPM, from TACR2colon — 134.1 nTPM, from TACR2adrenal gland — 0.3 nTPM, from TACR2thyroid gland — 0.3 nTPM, from TACR2pancreas — 0.3 nTPM, from TACR2urinary bladder — 34.5 nTPM, from TACR2skeletal muscle — 2.6 nTPM, from TACR2spleen — 0.3 nTPM, from TACR2salivary gland — 0.4 nTPM, from TACR2
0134 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 TACR2 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

  • retina3.8 nTPM
  • cerebral cortex1.5 nTPM
  • basal ganglia1.3 nTPM
  • amygdala1.1 nTPM
  • cerebellum0.9 nTPM
  • hippocampal formation0.9 nTPM
  • hypothalamus0.7 nTPM
  • midbrain0.6 nTPM
  • spinal cord0.3 nTPM
  • pituitary gland0.2 nTPM

Peripheral and autonomic · 16

  • colon134.1 nTPM
  • urinary bladder34.5 nTPM
  • smooth muscle30.9 nTPM
  • stomach 127.3 nTPM
  • small intestine23.4 nTPM
  • duodenum4.6 nTPM
  • heart muscle3.0 nTPM
  • skeletal muscle2.6 nTPM
  • lung0.6 nTPM
  • liver0.5 nTPM
  • salivary gland0.4 nTPM
  • kidney0.3 nTPM
  • adrenal gland0.3 nTPM
  • thyroid gland0.3 nTPM
  • pancreas0.3 nTPM
  • spleen0.3 nTPM

Transcript is not protein. These are RNA levels for TACR2, 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.

TargetClassTypeValue (nM)pXOrganismAssay
Substance-K receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909114
Substance-K receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909114
Substance-K receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909114
Substance-K receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909114
Substance-K receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909114
Substance-K receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909114
Substance-K receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909114

Functional readouts 8

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

TargetClassTypeValue (nM)pXOrganismAssay
Substance-K receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909114
Substance-K receptorOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291885
Substance-K receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909114
Substance-K receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909114
Substance-K receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909114
Substance-K receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909114
Substance-K receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909114
Substance-K receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909114
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