Reaction Details |
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Target | Neuronal acetylcholine receptor subunit alpha-3 |
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Ligand | BDBM50264882 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_497110 (CHEMBL998588) |
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EC50 | >100000±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-3 |
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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: | MGSGPLSLPLALSPPRLLLLLLLSLLPVARASEAEHRLFERLFEDYNEIIRPVANVSDPV
IIHFEVSMSQLVKVDEVNQIMETNLWLKQIWNDYKLKWNPSDYGGAEFMRVPAQKIWKPD
IVLYNNAVGDFQVDDKTKALLKYTGEVTWIPPAIFKSSCKIDVTYFPFDYQNCTMKFGSW
SYDKAKIDLVLIGSSMNLKDYWESGEWAIIKAPGYKHDIKYNCCEEIYPDITYSLYIRRL
PLFYTINLIIPCLLISFLTVLVFYLPSDCGEKVTLCISVLLSLTVFLLVITETIPSTSLV
IPLIGEYLLFTMIFVTLSIVITVFVLNVHYRTPTTHTMPSWVKTVFLNLLPRVMFMTRPT
SNEGNAQKPRPLYGAELSNLNCFSRAESKGCKEGYPCQDGMCGYCHHRRIKISNFSANLT
RSSSSESVDAVLSLSALSPEIKEAIQSVKYIAENMKAQNEAKEIQDDWKYVAMVIDRIFL
WVFTLVCILGTAGLFLQPLMAREDA
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BDBM50264882 |
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n/a |
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Name | BDBM50264882 |
Synonyms: | CHEMBL497990 | N-((3-(2-chlorophenyl)isoxazol-5-yl)methyl)-N-methylpiperidine-4-carboxamide |
Type | Small organic molecule |
Emp. Form. | C17H20ClN3O2 |
Mol. Mass. | 333.813 |
SMILES | CN(Cc1cc(no1)-c1ccccc1Cl)C(=O)C1CCNCC1 |
Structure |
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