1137 |
CHOLINERGIC RECEPTOR NICOTINIC ALPHA 4 SUBUNIT |
CHRNA4 |
BFNC |
EBN |
EBN1 |
NACHR |
NACHRA4 |
NACRA4 |
118504 |
1958 |
ENSG00000101204 |
OTTHUMG00000033080 |
P43681 |
ACHA4_HUMAN |
465 |
nicotinic acetylcholine receptor α4 subunit |
NICOTINIC ACETYLCHOLINE RECEPTOR |
BE0000849 |
NEURONAL ACETYLCHOLINE RECEPTOR SUBUNIT ALPHA-4 |
NEURONAL ACETYLCHOLINE RECEPTOR PROTEIN, ALPHA-4 SUBUNIT PRECURSOR. [SOURCE:UNIPROT/SWISSPROT;ACC:P43681] |
PA26490 |
T78111 |
Neuronal acetylcholine receptor alpha-4 |
T70967 |
NM_000744 |
NP_000735 |
Target Class | Receptors |
Target Subclass | TC:1.A.9 |
Uniprot Status | Swiss-Prot |
Interpro Type | Domain |
Interpro Name | Neurotransmitter-gated ion-channel ligand-binding |
Human Readable Name | DRUGGABLE GENOME |
Interpro Short Name | Neur_chan_lig-bd |
Interpro Name | Neurotransmitter-gated ion-channel |
Interpro Type | Family |
Uniprot Evidence | 1: Evidence at protein level |
Interpro Acc | IPR006202 |
Interpro Short Name | Neur_channel |
Human Readable Name | ION CHANNEL |
Interpro Acc | IPR006201 |
Transmembrane Helix Count | 4 |
Target Subclass | Ligand_gated_ion_channels |
Target Subclass | Channels |
Target Subclass | cys-loop |
Target Main Class | Receptors |
Gene Biotype | PROTEIN_CODING |
GuideToPharmacology Gene Category Name | Nicotinic acetylcholine receptors |
GuideToPharmacology Gene Category ID | 76 |
DNA REPAIR |
ION CHANNEL |
EXTERNAL SIDE OF PLASMA MEMBRANE |
DRUGGABLE GENOME |
partial agonist (activating) |
agonist (activating) |
Trial Name | varenicline, CP-526 |
Novel drug target | Established target |
Details of the Assay for Interaction | <i>In vitro</i> affinity for recombinant human α4β2 receptors in membranes from transfected CHO-K1 cells, determined by displacement of [<sup>3</sup>H]-(−)-cytisine. |
partial agonist (activating) |
Novel drug target | Established target |
Trial Name | TC-1734, AZD-3480, ispronicline |
Mechanism of Interaction | Neuronal acetylcholine receptor; alpha4/beta2 partial agonist |
antagonist (inhibitory) |
Novel drug target | Established target |
Trial Name | TC-5214 |
Mechanism of Interaction | Neuronal acetylcholine receptor; alpha4/beta2 antagonist |
partial agonist (activating) |
Direct Interaction | yes |
Mechanism of Interaction | Nicotinic acetylcholine receptor alpha4/beta2/alpha5 partial agonist |
Trial Name | pozanicline , ABT-089 |
agonist (activating) |
Mechanism of Interaction | Neuronal acetylcholine receptor; alpha4/beta2 agonist |
Direct Interaction | yes |
agonist (activating) |
Mechanism of Interaction | Neuronal acetylcholine receptor; alpha4/beta2 agonist |
Direct Interaction | yes |
agonist (activating) |
Mechanism of Interaction | Neuronal acetylcholine receptor; alpha4/beta2 agonist |
Direct Interaction | yes |
modulator |
Mechanism of Interaction | Neuronal acetylcholine receptor; alpha4/beta2 modulator |
Direct Interaction | yes |
agonist (activating) |
Mechanism of Interaction | Neuronal acetylcholine receptor; alpha4/beta2 agonist |
Direct Interaction | yes |
antagonist (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Neuronal acetylcholine receptor; alpha4/beta2 antagonist |
agonist (activating) |
Direct Interaction | yes |
Mechanism of Interaction | Neuronal acetylcholine receptor; alpha4/beta2 agonist |
agonist (activating) |
Direct Interaction | yes |
Mechanism of Interaction | Neuronal acetylcholine receptor; alpha4/beta2 agonist |
agonist (activating) |
Trial Name | TC-6499 |
Novel drug target | Established target |
Mechanism of Interaction | Neuronal acetylcholine receptor; alpha4/beta2 agonist |
agonist (activating) |
Details of the Assay for Interaction | <i>In vitro</i> affinity for recombinant human α4β2 receptors in membranes from transfected CHO-K1 cells, determined by displacement of [<sup>3</sup>H]-(−)-cytisine. |
Specific Action of the Ligand | Agonist |
Details of Interaction | α4β2 |
antagonist (inhibitory) |
Details of the Assay for Interaction | Antagonism of ACh activation of human α4β2 nACh receptors expressed in <i>Xenopus</i> oocytes, at different ACh concentrations. |
Specific Action of the Ligand | Antagonist |
Endogenous Drug? | False |
blocker (inhibitory) |
Specific Action of the Ligand | None |
Details of Interaction | α4β4 |
Endogenous Drug? | False |
partial agonist (activating) |
Mechanism of Interaction | Neuronal acetylcholine receptor; alpha4/beta2 partial agonist |
Direct Interaction | yes |
blocker (inhibitory) |
Specific Action of the Ligand | None |
Details of Interaction | α4β2 |
Endogenous Drug? | False |
agonist (activating) |
Direct Interaction? | False |
Endogenous Drug? | False |
Specific Action of the Ligand | Agonist |
antagonist (inhibitory) |
Trial Name | - |
Novel drug target | Established target |
blocker (inhibitory) |
Specific Action of the Ligand | None |
Details of Interaction | α4β2 |
Endogenous Drug? | False |
CHRNA4 | Ensembl Gene Name |
Gene Biotype | PROTEIN_CODING |
CHRNA4 | Gene Symbol |
Target Class | Receptors |
Target Subclass | TC:1.A.9 |
ENSG00000101204 | Ensembl Gene Id |
CHRNA4 | Display Id |
NEURONAL ACETYLCHOLINE RECEPTOR PROTEIN, ALPHA-4 SUBUNIT PRECURSOR. [SOURCE:UNIPROT/SWISSPROT;ACC:P43681] | Description |
Human Readable Name | DRUGGABLE GENOME |
DRUGGABLE GENOME |
ACHA4_HUMAN | Uniprot Id |
CHRNA4 | Uniprot Gene Name |
ENSG00000101204 | Ensembl Gene Id |
Uniprot Status | Swiss-Prot |
Interpro Type | Domain |
Interpro Name | Neurotransmitter-gated ion-channel ligand-binding |
ION CHANNEL, DRUGGABLE GENOME |
ACHA4_HUMAN | Uniprot Id |
ENSG00000101204 | Ensembl Gene Id |
1137 | Entrez Gene Id |
Transmembrane Helix Count | 4 |
Target Subclass | Ligand_gated_ion_channels |
Target Subclass | Channels |
1958 | HUGO Gene ID |
1958 | HUGO Gene Symbol |
cholinergic receptor nicotinic alpha 4 subunit | HUGO Gene Name |
GuideToPharmacology Gene Category Name | Nicotinic acetylcholine receptors |
GuideToPharmacology Gene Category ID | 76 |
ION CHANNEL |
PA26490 | PharmGKB ID |
CHRNA4 | DrugBank Gene Name |
P43681 | UniProt Accession |
1137 | Entrez Gene Id |
nAChR | TTD Gene Abbreviation |
T78111 | TTD Target ID |
ENSG00000101204 | Gene Symbol |
CHRNA4 | Ensembl Id |
DRUGGABLE GENOME |
NACRA4 | GENE_SYMBOL |
CHRNA4 | GENE_SYMBOL |
Neuronal acetylcholine receptor subunit alpha-4 | UNIPROT |
Neuronal acetylcholine receptor subunit alpha-4 | Gene Name |
P43681 | UniProt ID |
ION CHANNEL |
NACRA4 | GO Gene Synonym |
DNA REPAIR, EXTERNAL SIDE OF PLASMA MEMBRANE |
CHRNA4 | TTD Gene Abbreviation |
T70967 | TTD Target ID |