Target
Neuronal acetylcholine receptor subunit alpha-4
Ligand
BDBM50088454
Substrate
n/a
Meas. Tech.
Radioligand Competition Assay
Ki
0.32±0.06 nM
Citation
 Rohde, LAAhring, PKJensen, MLNielsen, EØPeters, DHelgstrand, CKrintel, CHarpsøe, KGajhede, MKastrup, JSBalle, T Intersubunit bridge formation governs agonist efficacy at nicotinic acetylcholine α4β2 receptors: unique role of halogen bonding revealed. J Biol Chem 287:4248-59 (2012) [PubMed]  Article 
Target
Name:
Neuronal acetylcholine receptor subunit alpha-4
Synonyms:
ACHA4_RAT | Acra4 | Cholinergic, Nicotinic Alpha4Beta2 | Cholinergic, Nicotinic Alpha4Beta4 | Chrna4 | Neuronal acetylcholine receptor | Neuronal acetylcholine receptor (alpha4beta2 nAChR) | Neuronal acetylcholine receptor protein alpha-4 subunit | Neuronal acetylcholine receptor subunit alpha 4 beta 2 | Neuronal acetylcholine receptor subunit alpha-4
Type:
Enzyme
Mol. Mass.:
70196.44
Organism:
Rattus norvegicus (Rat)
Description:
P09483
Residue:
630
Sequence:
MANSGTGAPPPLLLLPLLLLLGTGLLPASSHIETRAHAEERLLKRLFSGYNKWSRPVANISDVVLVRFGLSIAQLIDVDEKNQMMTTNVWVKQEWHDYKLRWDPGDYENVTSIRIPSELIWRPDIVLYNNADGDFAVTHLTKAHLFYDGRVQWTPPAIYKSSCSIDVTFFPFDQQNCTMKFGSWTYDKAKIDLVSMHSRVDQLDFWESGEWVIVDAVGTYNTRKYECCAEIYPDITYAFIIRRLPLFYTINLIIPCLLISCLTVLVFYLPSECGEKVTLCISVLLSLTVFLLLITEIIPSPTSLVIPLIGEYLLFTMIFVTLSIVITVFVLNVHHRSPRTHTMPAWVRRVFLDIVPRLLFMKRPSVVKDNCRRLIESMHKMANAPRFWPEPVGEPGILSDICNQGLSPAPTFCNPTDTAVETQPTCRSPPLEVPDLKTSEVEKASPCPSPGSCPPPKSSSGAPMLIKARSLSVQHVPSSQEAAEDGIRCRSRSIQYCVSQDGAASLADSKPTSSPTSLKARPSQLPVSDQASPCKCTCKEPSPVSPVTVLKAGGTKAPPQHLPLSPALTRAVEGVQYIADHLKAEDTDFSVKEDWKYVAMVIDRIFLWMFIIVCLLGTVGLFLPPWLAAC
  
Inhibitor
Name:
BDBM50088454
Synonyms:
1-(6-Bromo-pyridin-3-yl)-[1,4]diazepane | 1-(6-bromopyridin-3-yl)-1,4-diazepane | CHEMBL306387 | NS3920, 4
Type:
Small organic molecule
Emp. Form.:
C10H14BrN3
Mol. Mass.:
256.142
SMILES:
Brc1ccc(cn1)N1CCCNCC1
Structure:
Search PDB for entries with ligand similarity: