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PsychedeliaDokholyan Laboratory
TargetOther named receptors

Cysteinyl leukotriene receptor 1

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

Measurements
14
Compounds
7
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

CLTR1_HUMANCYSLTR1Homo sapiens

Cysteinyl leukotriene receptor 1

Receptor for cysteinyl leukotrienes mediating bronchoconstriction of individuals with and without asthma. Stimulation by LTD4 results in the contraction and proliferation of smooth muscle, edema, eosinophil migration and damage to the mucus layer in the lung. This response is mediated via a G protein that activates a phosphatidylinositol-calcium second messenger system. The rank order of affinities for the leukotrienes is LTD4 >> LTE4 = LTC4 >> LTB4

Quoted from UniProt’s FUNCTION annotation for Q9Y271 (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
CYSLTR20.9760.5410.9000.495
LTC4S0.9460.0000.0000.946
GNAQ0.8400.1150.6500.525
ALOX5AP0.7870.0000.0000.784
GGT10.7870.0000.7500.183
ALOX50.7820.0000.0000.762
TBXA2R0.7500.0000.4000.601
GNA150.7330.1150.6500.208
LTB4R20.7210.0000.4000.555
GNA110.7110.1150.6500.144

Where it sits in the cell

UniProt, curated Cell membrane

Expression by cell type

Single cell type RNA, the 12 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Innate lymphoid cells129.5 nCPM
  • pDCs128.7 nCPM
  • B-cells89.8 nCPM
  • Plasma cells89.5 nCPM
  • Microglia82.2 nCPM
  • Hofbauer cells67.7 nCPM
  • Thymocytes66.1 nCPM
  • Mast cells61.9 nCPM
  • Kupffer cells61.5 nCPM
  • Hematopoietic stem cells46.1 nCPM
  • Macrophages35.6 nCPM
  • Thymic myoid cells34 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.

  • lymphoid tissue10.9 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 — 0.6 nTPM, from CYSLTR1cerebellum — no resolved target expressed herehippocampal formation — 0.4 nTPM, from CYSLTR1amygdala — 0.4 nTPM, from CYSLTR1hypothalamus — 0.4 nTPM, from CYSLTR1thalamus — no resolved target expressed herebasal ganglia — 0.4 nTPM, from CYSLTR1medulla 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: spinal cord 0.8, midbrain 0.6, pituitary gland 0.3, retina 0.3.

Body

heart — 1.6 nTPM, from CYSLTR1smooth muscle — 4.2 nTPM, from CYSLTR1lung — 6.9 nTPM, from CYSLTR1liver — 1.5 nTPM, from CYSLTR1kidney — 0.9 nTPM, from CYSLTR1stomach — 2.7 nTPM, from CYSLTR1duodenum — 2.3 nTPM, from CYSLTR1small intestine — 3.7 nTPM, from CYSLTR1colon — 3.3 nTPM, from CYSLTR1adrenal gland — 1.6 nTPM, from CYSLTR1thyroid gland — 1.9 nTPM, from CYSLTR1pancreas — 0.5 nTPM, from CYSLTR1urinary bladder — 6.5 nTPM, from CYSLTR1skeletal muscle — 0.4 nTPM, from CYSLTR1spleen — 10.0 nTPM, from CYSLTR1salivary gland — 1.7 nTPM, from CYSLTR1
010 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 CYSLTR1 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

  • spinal cord0.8 nTPM
  • cerebral cortex0.6 nTPM
  • midbrain0.6 nTPM
  • hippocampal formation0.4 nTPM
  • amygdala0.4 nTPM
  • hypothalamus0.4 nTPM
  • basal ganglia0.4 nTPM
  • pituitary gland0.3 nTPM
  • retina0.3 nTPM

Peripheral and autonomic · 16

  • spleen10.0 nTPM
  • lung6.9 nTPM
  • urinary bladder6.5 nTPM
  • smooth muscle4.2 nTPM
  • small intestine3.7 nTPM
  • colon3.3 nTPM
  • stomach 12.7 nTPM
  • duodenum2.3 nTPM
  • thyroid gland1.9 nTPM
  • salivary gland1.7 nTPM
  • heart muscle1.6 nTPM
  • adrenal gland1.6 nTPM
  • liver1.5 nTPM
  • kidney0.9 nTPM
  • pancreas0.5 nTPM
  • skeletal muscle0.4 nTPM

Transcript is not protein. These are RNA levels for CYSLTR1, 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
Cysteinyl leukotriene receptor 1Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909164
Cysteinyl leukotriene receptor 1Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909164
Cysteinyl leukotriene receptor 1Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909164
Cysteinyl leukotriene receptor 1Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909164
Cysteinyl leukotriene receptor 1Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909164
Cysteinyl leukotriene receptor 1Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909164
Cysteinyl leukotriene receptor 1Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909164

Functional readouts 7

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

TargetClassTypeValue (nM)pXOrganismAssay
Cysteinyl leukotriene receptor 1Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909164
Cysteinyl leukotriene receptor 1Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909164
Cysteinyl leukotriene receptor 1Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909164
Cysteinyl leukotriene receptor 1Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909164
Cysteinyl leukotriene receptor 1Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909164
Cysteinyl leukotriene receptor 1Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909164
Cysteinyl leukotriene receptor 1Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909164
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