Target
Neuronal acetylcholine receptor subunit alpha-4
Ligand
BDBM50279369
Substrate
n/a
Meas. Tech.
ChEMBL_546021 (CHEMBL1028499)
EC50
40±n/a nM
Citation
 Bunnelle, WHTietje, KRFrost, JMPeters, DJi, JLi, TScanio, MJShi, LAnderson, DJDyhring, TGrønlien, JHWeen, HThorin-Hagene, KMeyer, MD Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. Substitutions that switch subtype selectivity. J Med Chem 52:4126-41 (2009) [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:
BDBM50279369
Synonyms:
CHEMBL460562 | cis-2-(3-Pyridinyl)octahydropyrrolo[3,4-c]pyrrole Dihydrochloride
Type:
Small organic molecule
Emp. Form.:
C11H15N3
Mol. Mass.:
189.2569
SMILES:
C1NC[C@@H]2CN(C[C@H]12)c1cccnc1 |r|
Structure:
Search PDB for entries with ligand similarity: