Reaction Details |
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Target | Neuronal acetylcholine receptor subunit alpha-4 |
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Ligand | BDBM50264799 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_497109 (CHEMBL998587) |
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EC50 | 12±n/a nM |
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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 Lett18:5209-12 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Neuronal acetylcholine receptor subunit alpha-4 |
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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: | MELGGPGAPRLLPPLLLLLGTGLLRASSHVETRAHAEERLLKKLFSGYNKWSRPVANISD
VVLVRFGLSIAQLIDVDEKNQMMTTNVWVKQEWHDYKLRWDPADYENVTSIRIPSELIWR
PDIVLYNNADGDFAVTHLTKAHLFHDGRVQWTPPAIYKSSCSIDVTFFPFDQQNCTMKFG
SWTYDKAKIDLVNMHSRVDQLDFWESGEWVIVDAVGTYNTRKYECCAEIYPDITYAFVIR
RLPLFYTINLIIPCLLISCLTVLVFYLPSECGEKITLCISVLLSLTVFLLLITEIIPSTS
LVIPLIGEYLLFTMIFVTLSIVITVFVLNVHHRSPRTHTMPTWVRRVFLDIVPRLLLMKR
PSVVKDNCRRLIESMHKMASAPRFWPEPEGEPPATSGTQSLHPPSPSFCVPLDVPAEPGP
SCKSPSDQLPPQQPLEAEKASPHPSPGPCRPPHGTQAPGLAKARSLSVQHMSSPGEAVEG
GVRCRSRSIQYCVPRDDAAPEADGQAAGALASRNTHSAELPPPDQPSPCKCTCKKEPSSV
SPSATVKTRSTKAPPPHLPLSPALTRAVEGVQYIADHLKAEDTDFSVKEDWKYVAMVIDR
IFLWMFIIVCLLGTVGLFLPPWLAGMI
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BDBM50264799 |
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n/a |
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Name | BDBM50264799 |
Synonyms: | 3-(2-chloro-6-fluorophenyl)-5-(1-methyl-2-(piperidin-4-yl)-1H-imidazol-5-yl)isoxazole | CHEMBL491847 |
Type | Small organic molecule |
Emp. Form. | C18H18ClFN4O |
Mol. Mass. | 360.813 |
SMILES | Cn1c(cnc1C1CCNCC1)-c1cc(no1)-c1c(F)cccc1Cl |
Structure |
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