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Target
Neuronal acetylcholine receptor subunit alpha-3
Ligand
BDBM50420604
Substrate
n/a
Meas. Tech.
ChEMBL_842058 (CHEMBL2091475)
IC50
3250±n/a nM
Citation
 Zanaletti, R; Bettinetti, L; Castaldo, C; Cocconcelli, G; Comery, T; Dunlop, J; Gaviraghi, G; Ghiron, C; Haydar, SN; Jow, F; Maccari, L; Micco, I; Nencini, A; Scali, C; Turlizzi, E; Valacchi, M Discovery of a novel alpha-7 nicotinic acetylcholine receptor agonist series and characterization of the potent, selective, and orally efficacious agonist 5-(4-acetyl[1,4]diazepan-1-yl)pentanoic acid [5-(4-methoxyphenyl)-1H-pyrazol-3-yl] amide (SEN15924, WAY-361789). J Med Chem 55:4806-23 (2012) [PubMed]  Article 
Target
Name:
Neuronal acetylcholine receptor subunit alpha-3
Synonyms:
ACHA3_HUMAN | CHRNA3 | Cholinergic, Nicotinic Alpha3Beta2 | Cholinergic, Nicotinic Alpha3Beta4 | Cholinergic, Nicotinic Alpha3Beta4x | Integrin alpha-5/Neuronal acetylcholine receptor subunit alpha-3/Neuronal acetylcholine receptor subunit beta-2/Neuronal acetylcholine receptor subunit beta-4 | NACHRA3 | Neuronal acetylcholine receptor protein alpha-3 subunit | Neuronal acetylcholine receptor subunit alpha-3 | Nicotinic acetylcholine receptor alpha6/alpha3/beta4 | nicotinic central
Type:
Enzyme Catalytic Domain
Mol. Mass.:
57479.03
Organism:
Homo sapiens (Human)
Description:
Cholinergic, Nicotinic Alpha3Beta2 0 HUMAN::P32297
Residue:
505
Sequence:
MGSGPLSLPLALSPPRLLLLLLLSLLPVARASEAEHRLFERLFEDYNEIIRPVANVSDPVIIHFEVSMSQLVKVDEVNQIMETNLWLKQIWNDYKLKWNPSDYGGAEFMRVPAQKIWKPDIVLYNNAVGDFQVDDKTKALLKYTGEVTWIPPAIFKSSCKIDVTYFPFDYQNCTMKFGSWSYDKAKIDLVLIGSSMNLKDYWESGEWAIIKAPGYKHDIKYNCCEEIYPDITYSLYIRRLPLFYTINLIIPCLLISFLTVLVFYLPSDCGEKVTLCISVLLSLTVFLLVITETIPSTSLVIPLIGEYLLFTMIFVTLSIVITVFVLNVHYRTPTTHTMPSWVKTVFLNLLPRVMFMTRPTSNEGNAQKPRPLYGAELSNLNCFSRAESKGCKEGYPCQDGMCGYCHHRRIKISNFSANLTRSSSSESVDAVLSLSALSPEIKEAIQSVKYIAENMKAQNEAKEIQDDWKYVAMVIDRIFLWVFTLVCILGTAGLFLQPLMAREDA
  
Inhibitor
Name:
BDBM50420604
Synonyms:
CHEMBL2087443
Type:
Small organic molecule
Emp. Form.:
C20H28N4O2
Mol. Mass.:
356.4619
SMILES:
COc1ccc(cc1)-c1cc(NC(=O)CCCCN2CCCCC2)[nH]n1
Structure:
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