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PsychedeliaDokholyan Laboratory
TargetOther named receptors

Substance-P 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
17
Compounds
9
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

NK1R_HUMANTACR1Homo sapiens

Substance-P receptor

Receptor for the tachykinin substance P, also able to bind and respond to tachynins neurokinin A/substance K and neurokinin B/neuromedin-K1718267,15452552. The rank order of affinity of this receptor to tachykinins is: substance P > neurokinin A/substance K > neurokinin B/neuromedin-K1718267. Substance P binding to its receptor triggers G protein-coupled receptor signaling via activation of phosphatidylinositol hydrolysis by phospholipase C. Substance P 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 P25103 (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
TAC10.9990.9940.9000.999
TAC30.9960.0000.0000.996
TAC40.9950.2920.9000.941
ARRB10.9570.0000.5000.918
ARRB20.9570.0000.5000.918
GNB10.9070.9020.0000.091
GNAS0.9050.9000.0000.091
NALCN0.8740.0000.0000.874
UNC800.8540.0000.0000.853
NTS0.8490.0000.0000.849

Where it sits in the cell

  • Plasma membrane
  • Centrosome
  • Basal body

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

UniProt, curated Cell membrane · Early endosome

Expression by cell type

Single cell type RNA, the 7 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Epicardial cells341.1 nCPM
  • Rod photoreceptor cells271.4 nCPM
  • Other brain neurons176.7 nCPM
  • Cone photoreceptor cells161.5 nCPM
  • Vascular endothelial cells153.6 nCPM
  • Retinal amacrine cells96.6 nCPM
  • Brain inhibitory neurons60.4 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.

  • adipose tissue6.2 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 — 1.7 nTPM, from TACR1cerebellum — no resolved target expressed herehippocampal formation — 0.6 nTPM, from TACR1amygdala — 0.8 nTPM, from TACR1hypothalamus — 1.1 nTPM, from TACR1thalamus — no resolved target expressed herebasal ganglia — 3.9 nTPM, from TACR1medulla 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 0.9, midbrain 0.2, spinal cord 0.2, pituitary gland 0.1.

Body

heart — 0.1 nTPM, from TACR1smooth muscle — 2.6 nTPM, from TACR1lung — 0.8 nTPM, from TACR1liver — no resolved target expressed herekidney — 0.7 nTPM, from TACR1stomach — 0.5 nTPM, from TACR1duodenum — 0.2 nTPM, from TACR1small intestine — 0.7 nTPM, from TACR1colon — 1.0 nTPM, from TACR1adrenal gland — 0.2 nTPM, from TACR1thyroid gland — 0.5 nTPM, from TACR1pancreas — 0.1 nTPM, from TACR1urinary bladder — 1.9 nTPM, from TACR1skeletal muscle — 0.3 nTPM, from TACR1spleen — no resolved target expressed heresalivary gland — 1.5 nTPM, from TACR1
04 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 TACR1 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 · 9

  • basal ganglia3.9 nTPM
  • cerebral cortex1.7 nTPM
  • hypothalamus1.1 nTPM
  • retina0.9 nTPM
  • amygdala0.8 nTPM
  • hippocampal formation0.6 nTPM
  • midbrain0.2 nTPM
  • spinal cord0.2 nTPM
  • pituitary gland0.1 nTPM

Peripheral and autonomic · 14

  • smooth muscle2.6 nTPM
  • urinary bladder1.9 nTPM
  • salivary gland1.5 nTPM
  • colon1.0 nTPM
  • lung0.8 nTPM
  • kidney0.7 nTPM
  • small intestine0.7 nTPM
  • stomach 10.5 nTPM
  • thyroid gland0.5 nTPM
  • skeletal muscle0.3 nTPM
  • duodenum0.2 nTPM
  • adrenal gland0.2 nTPM
  • heart muscle0.1 nTPM
  • pancreas0.1 nTPM

Transcript is not protein. These are RNA levels for TACR1, 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-P receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909113
Substance-P receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909113
Substance-P receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909113
Substance-P receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909113
Substance-P receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909113
Substance-P receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909113
Substance-P receptorOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909113

Functional readouts 10

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

TargetClassTypeValue (nM)pXOrganismAssay
Substance-P receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909113
Substance-P receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909113
Substance-P receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909113
Substance-P receptorOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291884
Substance-P receptorOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291884
Substance-P receptorOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291884
Substance-P receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909113
Substance-P receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909113
Substance-P receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909113
Substance-P receptorOther named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909113
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