Reaction Details |
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Target | Neuronal acetylcholine receptor subunit alpha-3 |
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Ligand | BDBM50420604 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_842058 (CHEMBL2091475) |
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IC50 | 3250±n/a nM |
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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 Chem55:4806-23 (2012) [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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BDBM50420604 |
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n/a |
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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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