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TargetHistamine receptors

Histamine H4 receptor

H1–H4 receptor subtypes.

Measurements
2
Compounds
2
Binding constants
1
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

HRH4_HUMANHRH4Homo sapiens

Histamine H4 receptor

G protein-coupled receptor primarily expressed in immune cells such as mast cells, eosinophils, basophils, dendritic cells and neutrophils that plays a key role in immune and inflammatory responses26948974. Mediates chemotaxis of immune cells to sites of inflammation or injury by responding to histamine26948974. Activation by histamine also influences the release of proinflammatory cytokines such as TNF, CCL4, IL6 and IFN-gamma29600327,31583075. Ligand binding induces a conformation change that triggers signaling via G(i)/GNAI1 leading to decreased intracellular cAMP levels by inhibiting adenylate cyclase activity39333117. In addition, plays a role in the control of renal reabsorption processes, particularly albumin uptake (By similarity)

Quoted from UniProt’s FUNCTION annotation for Q9H3N8 (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
HDC0.7610.0000.0000.728
TPM30.7020.0000.0000.702
TRPV10.6250.0450.0000.624
HRH10.5790.0000.0000.579
IL310.5700.0000.0000.570
CD300LD0.5480.0000.0000.000
HRH30.5370.0000.0000.537
SRC0.5270.0000.5000.081
AGT0.5200.0000.5000.081
GATA10.5130.0000.0000.470

Where it sits in the cell

UniProt, curated Cell membrane

Expression by cell type

Single cell type RNA, the 10 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Mast cells9.5 nCPM
  • Retinal pigment epithelial cells8.5 nCPM
  • Hepatic stellate cells6.5 nCPM
  • Neutrophil progenitors4.6 nCPM
  • Cone photoreceptor cells4.1 nCPM
  • Retinal horizontal cells4 nCPM
  • Retinal ganglion cells3.9 nCPM
  • Late primary spermatocytes3.5 nCPM
  • Hematopoietic stem cells3.4 nCPM
  • Early spermatids3.1 nCPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 1

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
Histamine H4 receptorHistamine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2395817

Other measurements 1

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
Histamine H4 receptorHistamine receptorsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4687649