Reaction Details Report a problem with these data
Target
Neuronal acetylcholine receptor subunit alpha-4
Ligand
BDBM50264884
Substrate
n/a
Meas. Tech.
ChEMBL_497115 (CHEMBL1001195)
EC50
20±n/a nM
Citation
 Albrecht, BK; Berry, V; Boezio, AA; Cao, L; Clarkin, K; Guo, W; Harmange, JC; Hierl, M; Huang, L; Janosky, B; Knop, J; Malmberg, A; McDermott, JS; Nguyen, HQ; Springer, SK; Waldon, D; Woodin, K; McDonough, SI Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant alpha4beta2 nicotinic acetylcholine receptor potentiators. Bioorg Med Chem Lett 18:5209-12 (2008) [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:
BDBM50264884
Synonyms:
3-(2-chlorophenyl)-5-(5-methyl-1-(piperidin-4-yl)-1H-pyrazol-4-yl)isoxazole | CHEMBL504947
Type:
Small organic molecule
Emp. Form.:
C18H19ClN4O
Mol. Mass.:
342.823
SMILES:
Cc1c(cnn1C1CCNCC1)-c1cc(no1)-c1ccccc1Cl
Structure:
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