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

CHRNA1 (P02708) - Overview - Molecular Target Synopsis

Protein


CHRNA1, Acetylcholine receptor subunit alpha
UniProt P02708

Also Known as ACHA_HUMAN, CHRNA1, ACHRA, CHNRA

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. Pentamer of two alpha chains, and one each of the beta, delta, and gamma (in immature muscle) or epsilon (in mature muscle) chains. The muscle heteropentamer composed of alpha-1, beta-1, delta, epsilon subunits interacts with the alpha-conotoxin ImII (PubMed:15609996).

5HBT
COMPLEX STRUCTURE OF FAB35 AND HUMAN NACHR ALPHA1
RCSB/PDB
Inspect Structure
See all 3D Structures for CHRNA1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: CHRNA1 is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: CHRNA1 is active in the following subcellular-locations: acetylcholine-gated channel complex, cell junction, cell surface, integral component of plasma membrane, integral component of postsynaptic specialization membrane, neuromuscular junction, neuron projection, plasma membrane, postsynaptic membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CHRNA1 has gain in 1 cell-lines, loss in 2 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, CAKI_1, SK_OV_3

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: LXFL529, SJCRH30, NCI-H847

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: HSMM, HUVEC, SK-N-SH

(see details)

3D Structures


For CHRNA1 there are:
2 structures (6 chains) solved
2 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CHRNA1 has been screened with 308 compounds (495 bioactivities), 8 compounds have bioactivities that show binding affinity of <= 500nM (10 bioactivities). (see details)