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

CHRNA4 (P43681) - Overview - Molecular Target Synopsis

Protein


CHRNA4, Neuronal acetylcholine receptor subunit alpha-4
UniProt P43681

Also Known as ACHA4_HUMAN, CHRNA4, NACRA4

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 permeable to sodium ions. Neuronal AChR is composed of two different types of subunits: alpha and beta. Alpha-4 subunit can be combined to beta-2 or beta-4 to give rise to functional receptors, complexes with beta-2 may be heteropentamers (PubMed:22361591). Interacts with RIC3; which is required for proper folding and assembly (PubMed:16120769). Interacts with LYPD6 (PubMed:27344019). The heteropentamer alpha-4-beta-2 interacts with alpha-conotoxins PnIA, GID and MII.

6CNJ
STRUCTURE OF THE 2ALPHA3BETA STIOCHIOMETRY OF THE HUMAN ALPHA4BETA2 NICOTINIC RECEPTOR
RCSB/PDB
Inspect Structure
See all 3D Structures for CHRNA4

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
627ENSG00000101204ENST00000370263ENSP00000359285P43681-1
556P43681-2
140ENSG00000101204ENST00000498043ENSP00000429513

Drugs


CHRNA4 is targeted by Approved Drug Varenicline. (see details)
Varenicline

Sub-cellular localization


Gene Copy Number Variation


In COSMIC - Cell Lines Project CHRNA4 has gain in 6 cell-lines, loss in 1 cell-lines and no signal in 998 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SK_OV_3, RPMI_8226, OVCAR_4

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, LN-18, SK-N-FI

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


For CHRNA4 there are:
4 structures (8 chains) solved
3 are solved in complex with at least one small molecule ligand
3 are solved with an approved drug

CHRNA4 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


CHRNA4 has been screened with 1688 compounds (4050 bioactivities), 656 compounds have bioactivities that show binding affinity of <= 500nM (1073 bioactivities). (see details)