Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

HTR3B (O95264) - Overview - Molecular Target Synopsis

Protein


HTR3B, 5-hydroxytryptamine receptor 3B
UniProt O95264

Also Known as 5HT3B_HUMAN, HTR3B

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: HTR3B is active in the following subcellular-locations: cell membrane.
GO terms: HTR3B is active in the following subcellular-locations: cell surface, integral component of plasma membrane, neuron projection, plasma membrane, postsynaptic membrane, serotonin-activated cation-selective channel complex, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project HTR3B has gain in 2 cell-lines, loss in 8 cell-lines and no signal in 995 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HL_60, SK_MEL_5, MOLT_4

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SK-N-FI, 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 HTR3B 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

HTR3B is solved in complex with the approved drug(s):

TKT/TROPISETRON (6HIS_A, 6HIS_B, 6HIS_C, 6HIS_D, 6HIS_E).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


HTR3B has been screened with 481 compounds (671 bioactivities), 219 compounds have bioactivities that show binding affinity of <= 500nM (292 bioactivities). (see details)