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PsychedeliaDokholyan Laboratory
TargetOther named receptors

C-X-C chemokine receptor type 2

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

CXCR2_HUMANCXCR2Homo sapiens

C-X-C chemokine receptor type 2

Receptor for interleukin-8 which is a powerful neutrophil chemotactic factor1891716. Binding of IL-8 to the receptor causes activation of neutrophils. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system8662698. Binds to IL-8 with high affinity. Also binds with high affinity to CXCL3, GRO/MGSA and NAP-21891716. Involved in the homeostatic wound healing response to tissue injury, a multistep cascade that guides neutrophil migration to necrotic sites while avoiding collateral damage of healthy tissues. Signals intravascular neutrophil chemotaxis to the injury site

Quoted from UniProt’s FUNCTION annotation for P25025 (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
CXCL80.9990.9990.9000.999
CXCL10.9990.2870.9000.999
CXCL30.9990.2870.9000.997
PPBP0.9990.2870.9000.996
CXCL50.9990.2870.9000.998
CXCR10.9990.0000.9000.980
CXCL60.9990.0000.9000.996
CXCL20.9990.2870.9000.998
CXCL120.9980.0460.6500.996
CXCL130.9970.0000.6500.992

Where it sits in the cell

  • Plasma membrane
  • Vesiclesadditional
  • Microtubulesadditional
  • Mitotic spindleadditional
  • Primary ciliumadditional
  • Primary cilium tipadditional
  • Basal bodyadditional

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

  • Neutrophils1,412.1 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 tissue40.8 nTPM
  • esophagus25.7 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 — 0.3 nTPM, from CXCR2cerebellum — 0.1 nTPM, from CXCR2hippocampal formation — 0.3 nTPM, from CXCR2amygdala — 0.3 nTPM, from CXCR2hypothalamus — 0.3 nTPM, from CXCR2thalamus — no resolved target expressed herebasal ganglia — 0.4 nTPM, from CXCR2medulla 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: midbrain 0.5, spinal cord 0.4, pituitary gland 0.1.

Body

heart — 0.9 nTPM, from CXCR2smooth muscle — 2.3 nTPM, from CXCR2lung — 6.3 nTPM, from CXCR2liver — 6.1 nTPM, from CXCR2kidney — 0.4 nTPM, from CXCR2stomach — 0.6 nTPM, from CXCR2duodenum — 0.7 nTPM, from CXCR2small intestine — 1.6 nTPM, from CXCR2colon — 1.3 nTPM, from CXCR2adrenal gland — 1.4 nTPM, from CXCR2thyroid gland — 0.6 nTPM, from CXCR2pancreas — 2.7 nTPM, from CXCR2urinary bladder — 7.4 nTPM, from CXCR2skeletal muscle — 0.5 nTPM, from CXCR2spleen — 40.8 nTPM, from CXCR2salivary gland — 2.6 nTPM, from CXCR2
041 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 CXCR2 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

  • midbrain0.5 nTPM
  • basal ganglia0.4 nTPM
  • spinal cord0.4 nTPM
  • cerebral cortex0.3 nTPM
  • hippocampal formation0.3 nTPM
  • amygdala0.3 nTPM
  • hypothalamus0.3 nTPM
  • cerebellum0.1 nTPM
  • pituitary gland0.1 nTPM

Peripheral and autonomic · 16

  • spleen40.8 nTPM
  • urinary bladder7.4 nTPM
  • lung6.3 nTPM
  • liver6.1 nTPM
  • pancreas2.7 nTPM
  • salivary gland2.6 nTPM
  • smooth muscle2.3 nTPM
  • small intestine1.6 nTPM
  • adrenal gland1.4 nTPM
  • colon1.3 nTPM
  • heart muscle0.9 nTPM
  • duodenum0.7 nTPM
  • stomach 10.6 nTPM
  • thyroid gland0.6 nTPM
  • skeletal muscle0.5 nTPM
  • kidney0.4 nTPM

Transcript is not protein. These are RNA levels for CXCR2, 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
C-X-C chemokine receptor type 2Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909128
C-X-C chemokine receptor type 2Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909128
C-X-C chemokine receptor type 2Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909128
C-X-C chemokine receptor type 2Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909128
C-X-C chemokine receptor type 2Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909128
C-X-C chemokine receptor type 2Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909128
C-X-C chemokine receptor type 2Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909128

Functional readouts 7

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

TargetClassTypeValue (nM)pXOrganismAssay
C-X-C chemokine receptor type 2Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909128
C-X-C chemokine receptor type 2Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909128
C-X-C chemokine receptor type 2Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909128
C-X-C chemokine receptor type 2Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909128
C-X-C chemokine receptor type 2Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909128
C-X-C chemokine receptor type 2Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909128
C-X-C chemokine receptor type 2Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909128
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