Reaction Details |
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Target | Neuronal acetylcholine receptor subunit alpha-4 |
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Ligand | BDBM50264884 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_497115 (CHEMBL1001195) |
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EC50 | 20±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_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: | MANSGTGAPPPLLLLPLLLLLGTGLLPASSHIETRAHAEERLLKRLFSGYNKWSRPVANI
SDVVLVRFGLSIAQLIDVDEKNQMMTTNVWVKQEWHDYKLRWDPGDYENVTSIRIPSELI
WRPDIVLYNNADGDFAVTHLTKAHLFYDGRVQWTPPAIYKSSCSIDVTFFPFDQQNCTMK
FGSWTYDKAKIDLVSMHSRVDQLDFWESGEWVIVDAVGTYNTRKYECCAEIYPDITYAFI
IRRLPLFYTINLIIPCLLISCLTVLVFYLPSECGEKVTLCISVLLSLTVFLLLITEIIPS
PTSLVIPLIGEYLLFTMIFVTLSIVITVFVLNVHHRSPRTHTMPAWVRRVFLDIVPRLLF
MKRPSVVKDNCRRLIESMHKMANAPRFWPEPVGEPGILSDICNQGLSPAPTFCNPTDTAV
ETQPTCRSPPLEVPDLKTSEVEKASPCPSPGSCPPPKSSSGAPMLIKARSLSVQHVPSSQ
EAAEDGIRCRSRSIQYCVSQDGAASLADSKPTSSPTSLKARPSQLPVSDQASPCKCTCKE
PSPVSPVTVLKAGGTKAPPQHLPLSPALTRAVEGVQYIADHLKAEDTDFSVKEDWKYVAM
VIDRIFLWMFIIVCLLGTVGLFLPPWLAAC
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BDBM50264884 |
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n/a |
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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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