Molecular Target Synopsis
Domains and Structures
Drugs and Clinical Candidates
Ligand Efficiency Plot
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
Germline Genetics

HTR3E (A5X5Y0) - Overview - Molecular Target Synopsis


HTR3E, 5-hydroxytryptamine receptor 3E
UniProt A5X5Y0

Also Known as 5HT3E_HUMAN, HTR3E

This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses. It is a cation-specific, but otherwise relatively nonselective, ion channel. Forms a pentaheteromeric complex with HTR3A. Not functional as a homomeric complex.

Isoforms / Transcripts (Protein Coding)

Sub-cellular localization

UniProt: HTR3E is active in the following subcellular-locations: cell membrane.
GO terms: HTR3E is active in the following subcellular-locations: integral component of plasma membrane, neuron projection, plasma membrane, synapse.

GO terms

Gene Copy Number Variation

In COSMIC - Cell Lines Project HTR3E has gain in 11 cell-lines, loss in 1 cell-lines and no signal in 993 cell-lines. (see details)

Gene Expression

In NCI60, the highest expressing cell lines are:

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SJCRH30, Hs 746T, NCI-H209

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, NHLF, HSMM

(see details)

3D Structures

At greater than 35% identity similarity to HTR3E there are:
8 structures (40 chains) solved
8 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

HTR3E is solved in complex with the approved drug(s):


(see details)
Molecular Target 3D Synopsis

Screening and Chemistry

HTR3E has been screened with 480 compounds (667 bioactivities), 218 compounds have bioactivities that show binding affinity of <= 500nM (288 bioactivities). (see details)