Target
Neuronal acetylcholine receptor subunit alpha-4
Ligand
BDBM50143314
Substrate
n/a
Meas. Tech.
Radioligand Competition Assay
Ki
0.33±0.21 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:
BDBM50143314
Synonyms:
(+)-Epibatidine | (-)-epibatidine | (1R,2R,4S)-2-(6-Chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane | 2-(6-Chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]heptane (epibatidine) | CHEMBL298826 | EPIBATIDINE
Type:
Small organic molecule
Emp. Form.:
C11H13ClN2
Mol. Mass.:
208.687
SMILES:
Clc1ccc(cn1)[C@H]1C[C@@H]2CC[C@H]1N2 |THB:4:7:13:11.10|
Structure:
Search PDB for entries with ligand similarity: