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TargetOther named receptors

Sphingosine 1-phosphate 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
7
Compounds
2
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

S1PR1_HUMANS1PR1Homo sapiens

Sphingosine 1-phosphate receptor 1

G protein-coupled receptor for the bioactive lysosphingolipid sphingosine 1-phosphate (S1P) that seems to be coupled to the G(i) subclass of heteromeric G proteins. Signaling leads to the activation of RAC1, SRC, PTK2/FAK1 and MAP kinases. Plays an important role in cell migration, probably via its role in the reorganization of the actin cytoskeleton and the formation of lamellipodia in response to stimuli that increase the activity of the sphingosine kinase SPHK1. Required for normal chemotaxis toward sphingosine 1-phosphate. Required for normal embryonic heart development and normal cardiac morphogenesis. Plays an important role in the regulation of sprouting angiogenesis and vascular maturation. Inhibits sprouting angiogenesis to prevent excessive sprouting during blood vessel development. Required for normal egress of mature T-cells from the thymus into the blood stream and into peripheral lymphoid organs. Plays a role in the migration of osteoclast precursor cells, the regulation of bone mineralization and bone homeostasis (By similarity). Plays a role in responses to oxidized 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine by pulmonary endothelial cells and in the protection against ventilator-induced lung injury

Quoted from UniProt’s FUNCTION annotation for P21453 (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
CD690.9950.3010.0000.993
GNAI10.9930.9320.9000.166
GNAI30.9630.3560.9000.482
S1PR40.9480.0000.9000.448
GNAI20.9220.1280.9000.163
GNB10.9200.9200.0000.000
SPHK10.9180.0000.0000.918
SPHK20.8700.0000.0000.870
KLF20.8560.0000.0000.822
GNG20.8420.8270.0000.000

Where it sits in the cell

  • Vesicles

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

UniProt, curated Cell membrane · Endosome · Membrane raft

Expression by cell type

Single cell type RNA, the 11 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Vascular endothelial cells164.5 nCPM
  • Lymphatic endothelial cells102.1 nCPM
  • Bergmann glia71.3 nCPM
  • Astrocytes40.7 nCPM
  • Müller glia36.6 nCPM
  • Hofbauer cells28.1 nCPM
  • Innate lymphoid cells23.5 nCPM
  • Granulosa cells22.7 nCPM
  • NK-cells20.7 nCPM
  • Thymocytes20.3 nCPM
  • B-cells19.9 nCPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Other measurements 7

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
Sphingosine 1-phosphate receptor 1Other named receptors%Max (Mean)— no normalized value— value does not convert to pXHomo sapiensCHEMBL5209836
Sphingosine 1-phosphate receptor 1Other named receptors%Inhib (Mean)— no normalized value— value does not convert to pXHomo sapiensCHEMBL5209836
Sphingosine 1-phosphate receptor 1Other named receptors%Inhib (Mean)— no normalized value— value does not convert to pXHomo sapiensCHEMBL5209836
Sphingosine 1-phosphate receptor 1Other named receptors%Max (Mean)— no normalized value— value does not convert to pXHomo sapiensCHEMBL5209836
Sphingosine 1-phosphate receptor 1Other named receptors%Inhib (Mean)— no normalized value— value does not convert to pXHomo sapiensCHEMBL5209836
Sphingosine 1-phosphate receptor 1Other named receptors%Inhib (Mean)— no normalized value— value does not convert to pXHomo sapiensCHEMBL5209837
Sphingosine 1-phosphate receptor 1Other named receptors%Inhib (Mean)— no normalized value— value does not convert to pXHomo sapiensCHEMBL5209838