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

CHRNA5 (P30532) - Overview - Molecular Target Synopsis

Protein


CHRNA5, Neuronal acetylcholine receptor subunit alpha-5
UniProt P30532

Also Known as ACHA5_HUMAN, CHRNA5, NACHRA5

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 non-alpha (beta). Interacts with LYPD6 (PubMed:27344019).

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: CHRNA5 is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: CHRNA5 is active in the following subcellular-locations: acetylcholine-gated channel complex, cell junction, dopaminergic synapse, integral component of plasma membrane, neuron projection, plasma membrane, postsynaptic membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CHRNA5 has gain in 0 cell-lines, loss in 2 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: T47D, NCI_H460, NCI_H522

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

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: MCF-7, SK-N-SH, NHLF

(see details)

3D Structures


At greater than 50% identity similarity to CHRNA5 there are:
10 structures (18 chains) solved
7 are solved in complex with at least one small molecule ligand
3 are solved with an approved drug

CHRNA5 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


CHRNA5 has been screened with 68 compounds (164 bioactivities), 1 compounds have bioactivities that show binding affinity of <= 500nM (1 bioactivities). (see details)