Tclin HRH3 Histamine H3 receptor

Protein Summary

Description

The H3 subclass of histamine receptors could mediate the histamine signals in CNS and peripheral nervous system. Signals through the inhibition of adenylate cyclase and displays high constitutive activity (spontaneous activity in the absence of agonist). Agonist stimulation of isoform 3 neither modified adenylate cyclase activity nor induced intracellular calcium mobilization. Histamine is a ubiquitous messenger molecule released from mast cells, enterochromaffin-like cells, and neurons. Its various actions are mediated by histamine receptors H1, H2, H3 and H4. This gene encodes one of the histamine receptors (H3) which belongs to the family 1 of G protein-coupled receptors. It is an integral membrane protein and can regulate neurotransmitter release. This receptor can also increase voltage-dependent calcium current in smooth muscles and innervates the blood vessels and the heart in cardiovascular system. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• Q9Y5N1
• Q4QRI7
• Q9GZX2
• Q9H4K8
• H3R

Gene Name

• HRH3

Ensembl ID

• ENST00000340177
• ENSP00000342560
• ENSG00000101180

Symbol

• GPCR97
• HH3R
• GPCR97

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
ligand (chemical)	0.98
biological process	0.95
disease perturbation	0.74
chemical	0.64
molecular function	0.63

Protein Classes

PANTHER Classes

Protein / Receptor / G-protein Coupled Receptor / Histamine H3 Receptor

DTO Classes

Protein / G-protein Coupled Receptor / Class A Rhodopsin Like / Histamine Receptor / Histamine H3 Receptor

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 699.92   (req: < 5)

Gene RIFs: 45   (req: <= 3)

Antibodies: 434   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 699.92   (req: >= 5)

Gene RIFs: 45   (req: > 3)

Antibodies: 434   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 14

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 3093

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 5