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

CHRNB3 (Q05901) - Overview - Molecular Target Synopsis

Protein


CHRNB3, Neuronal acetylcholine receptor subunit beta-3
UniProt Q05901

Also Known as ACHB3_HUMAN, CHRNB3

After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. Neuronal AChR seems to be composed of two different type of subunits: alpha and beta.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
458ENSG00000147432ENST00000289957ENSP00000289957Q05901-1, Q5IS75-1
15ENSG00000147432ENST00000534391ENSP00000433913

Sub-cellular localization


UniProt: CHRNB3 is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: CHRNB3 is active in the following subcellular-locations: acetylcholine-gated channel complex, cell junction, dopaminergic synapse, integral component of membrane, integral component of plasma membrane, neuron projection, plasma membrane, postsynaptic membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CHRNB3 has gain in 7 cell-lines, loss in 6 cell-lines and no signal in 992 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, LOXIMVI, HL_60

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Pfeiffer, 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 50% identity similarity to CHRNB3 there are:
10 structures (19 chains) solved
4 are solved in complex with at least one small molecule ligand
3 are solved with an approved drug

CHRNB3 is solved in complex with the approved drug(s):

NCT/NICOTINE (5KXI_A, 5KXI_D, 6CNJ_A, 6CNJ_D, 6CNK_A, 6CNK_B, 6CNK_D).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CHRNB3 has been screened with 55 compounds (74 bioactivities), 13 compounds have bioactivities that show binding affinity of <= 500nM (18 bioactivities). (see details)