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Target
Neuronal acetylcholine receptor subunit alpha-4
Ligand
BDBM50264917
Substrate
n/a
Meas. Tech.
ChEMBL_497109 (CHEMBL998587)
EC50
6±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_HUMAN | CHRNA4 | CHRNA4 protein | NACRA4 | Neuronal acetylcholine receptor protein alpha-4 subunit | Neuronal acetylcholine receptor subunit alpha 4 beta 2 | Nicotinic acetylcholine receptor alpha4/beta2/alpha5
Type:
n/a
Mol. Mass.:
69963.49
Organism:
Homo sapiens (Human)
Description:
NACHRA4
Residue:
627
Sequence:
MELGGPGAPRLLPPLLLLLGTGLLRASSHVETRAHAEERLLKKLFSGYNKWSRPVANISDVVLVRFGLSIAQLIDVDEKNQMMTTNVWVKQEWHDYKLRWDPADYENVTSIRIPSELIWRPDIVLYNNADGDFAVTHLTKAHLFHDGRVQWTPPAIYKSSCSIDVTFFPFDQQNCTMKFGSWTYDKAKIDLVNMHSRVDQLDFWESGEWVIVDAVGTYNTRKYECCAEIYPDITYAFVIRRLPLFYTINLIIPCLLISCLTVLVFYLPSECGEKITLCISVLLSLTVFLLLITEIIPSTSLVIPLIGEYLLFTMIFVTLSIVITVFVLNVHHRSPRTHTMPTWVRRVFLDIVPRLLLMKRPSVVKDNCRRLIESMHKMASAPRFWPEPEGEPPATSGTQSLHPPSPSFCVPLDVPAEPGPSCKSPSDQLPPQQPLEAEKASPHPSPGPCRPPHGTQAPGLAKARSLSVQHMSSPGEAVEGGVRCRSRSIQYCVPRDDAAPEADGQAAGALASRNTHSAELPPPDQPSPCKCTCKKEPSSVSPSATVKTRSTKAPPPHLPLSPALTRAVEGVQYIADHLKAEDTDFSVKEDWKYVAMVIDRIFLWMFIIVCLLGTVGLFLPPWLAGMI
  
Inhibitor
Name:
BDBM50264917
Synonyms:
3-(2-chloro-6-fluorophenyl)-5-(5-methyl-1-(piperidin-4-yl)-1H-pyrazol-4-yl)isoxazole | CHEMBL497162
Type:
Small organic molecule
Emp. Form.:
C18H18ClFN4O
Mol. Mass.:
360.813
SMILES:
Cc1c(cnn1C1CCNCC1)-c1cc(no1)-c1c(F)cccc1Cl
Structure:
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