Reaction Details Report a problem with these data
Target
Neuronal acetylcholine receptor subunit alpha-4
Ligand
BDBM50088453
Substrate
n/a
Meas. Tech.
Radioligand Competition Assay
Ki
0.25±0.05 nM
Citation
 Rohde, LA; Ahring, PK; Jensen, ML; Nielsen, EØ; Peters, D; Helgstrand, C; Krintel, C; Harpsøe, K; Gajhede, M; Kastrup, JS; Balle, 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:
BDBM50088453
Synonyms:
1-(6-Bromo-5-ethoxy-pyridin-3-yl)-[1,4]diazepane | 1-(6-bromo-5-ethoxypyridin-3-yl)-1,4-diazepane | CHEMBL72433 | NS3570, 5
Type:
Small organic molecule
Emp. Form.:
C12H18BrN3O
Mol. Mass.:
300.195
SMILES:
CCOc1cc(cnc1Br)N1CCCNCC1
Structure:
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