Reaction Details |
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Target | Neuronal acetylcholine receptor subunit alpha-4/beta-2 |
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Ligand | BDBM50166908 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_941644 (CHEMBL2330762) |
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EC50 | 950±n/a nM |
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Citation | Liu, Y; Richardson, J; Tran, T; Al-Muhtasib, N; Xie, T; Yenugonda, VM; Sexton, HG; Rezvani, AH; Levin, ED; Sahibzada, N; Kellar, KJ; Brown, ML; Xiao, Y; Paige, M Chemistry and pharmacological studies of 3-alkoxy-2,5-disubstituted-pyridinyl compounds as novel selectivea4ß2 nicotinic acetylcholine receptor ligands that reduce alcohol intake in rats. J Med Chem56:3000-11 (2013) [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/beta-2 |
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Name: | Neuronal acetylcholine receptor subunit alpha-4/beta-2 |
Synonyms: | Neuronal acetylcholine receptor Alpha-4/Beta-2 | Neuronal acetylcholine receptor protein alpha-4/beta-2 subunit | Neuronal acetylcholine receptor; alpha4/beta2 | nAChR subtypes alpha4 beta2 |
Type: | Protein |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
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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Component 2 |
Name: | Neuronal acetylcholine receptor subunit beta-2 |
Synonyms: | ACHB2_HUMAN | CHRNB2 | Neuronal acetylcholine receptor protein beta-2 subunit | Nicotinic acetylcholine receptor alpha3/beta2/alpha5 |
Type: | Protein |
Mol. Mass.: | 57020.50 |
Organism: | Homo sapiens (Human) |
Description: | P17787 |
Residue: | 502 |
Sequence: | MARRCGPVALLLGFGLLRLCSGVWGTDTEERLVEHLLDPSRYNKLIRPATNGSELVTVQL
MVSLAQLISVHEREQIMTTNVWLTQEWEDYRLTWKPEEFDNMKKVRLPSKHIWLPDVVLY
NNADGMYEVSFYSNAVVSYDGSIFWLPPAIYKSACKIEVKHFPFDQQNCTMKFRSWTYDR
TEIDLVLKSEVASLDDFTPSGEWDIVALPGRRNENPDDSTYVDITYDFIIRRKPLFYTIN
LIIPCVLITSLAILVFYLPSDCGEKMTLCISVLLALTVFLLLISKIVPPTSLDVPLVGKY
LMFTMVLVTFSIVTSVCVLNVHHRSPTTHTMAPWVKVVFLEKLPALLFMQQPRHHCARQR
LRLRRRQREREGAGALFFREAPGADSCTCFVNRASVQGLAGAFGAEPAPVAGPGRSGEPC
GCGLREAVDGVRFIADHMRSEDDDQSVSEDWKYVAMVIDRLFLWIFVFVCVFGTIGMFLQ
PLFQNYTTTTFLHSDHSAPSSK
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BDBM50166908 |
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n/a |
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Name | BDBM50166908 |
Synonyms: | 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2(11),3,5,7,9-pentaene; dihydrochloride | CHEMBL556954 | US9993465, Varenicline | VARENICLINE |
Type | Small organic molecule |
Emp. Form. | C13H13N3 |
Mol. Mass. | 211.2624 |
SMILES | C1C2CNCC1c1cc3nccnc3cc21 |
Structure |
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