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Target
Neuronal acetylcholine receptor subunit alpha-7
Ligand
BDBM50250184
Substrate
n/a
Meas. Tech.
ChEMBL_498620 (CHEMBL966966)
EC50
10500±n/a nM
Citation
 Faghih, R; Gopalakrishnan, SM; Gronlien, JH; Malysz, J; Briggs, CA; Wetterstrand, C; Ween, H; Curtis, MP; Sarris, KA; Gfesser, GA; El-Kouhen, R; Robb, HM; Radek, RJ; Marsh, KC; Bunnelle, WH; Gopalakrishnan, M Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. J Med Chem 52:3377-84 (2009) [PubMed]  Article 
Target
Name:
Neuronal acetylcholine receptor subunit alpha-7
Synonyms:
ACHA7_HUMAN | CHRNA7 | Cholinergic, Nicotinic Alpha7 | NACHRA7 | Neuronal acetylcholine receptor protein alpha-7 subunit | Neuronal acetylcholine receptor subunit alpha-7 (nAChR-alpha 7) | Nicotinic acetylcholine receptor alpha-7 (alpha7 nAChR)
Type:
n/a
Mol. Mass.:
56448.33
Organism:
Homo sapiens (Human)
Description:
CHRNA7 (NACHRA7)
Residue:
502
Sequence:
MRCSPGGVWLALAASLLHVSLQGEFQRKLYKELVKNYNPLERPVANDSQPLTVYFSLSLLQIMDVDEKNQVLTTNIWLQMSWTDHYLQWNVSEYPGVKTVRFPDGQIWKPDILLYNSADERFDATFHTNVLVNSSGHCQYLPPGIFKSSCYIDVRWFPFDVQHCKLKFGSWSYGGWSLDLQMQEADISGYIPNGEWDLVGIPGKRSERFYECCKEPYPDVTFTVTMRRRTLYYGLNLLIPCVLISALALLVFLLPADSGEKISLGITVLLSLTVFMLLVAEIMPATSDSVPLIAQYFASTMIIVGLSVVVTVIVLQYHHHDPDGGKMPKWTRVILLNWCAWFLRMKRPGEDKVRPACQHKQRRCSLASVEMSAVAPPPASNGNLLYIGFRGLDGVHCVPTPDSGVVCGRMACSPTHDEHLLHGGQPPEGDPDLAKILEEVRYIANRFRCQDESEAVCSEWKFAACVVDRLCLMAFSVFTIICTIGILMSAPNFVEAVSKDFA
  
Inhibitor
Name:
BDBM50250184
Synonyms:
4-(5-(4-Chlorophenyl)-3-(5-fluoro-2-methoxybenzoyl)-2-methyl-1H-pyrrol-1-yl)benzenesulfonamide | CHEMBL492176
Type:
Small organic molecule
Emp. Form.:
C25H20ClFN2O4S
Mol. Mass.:
498.954
SMILES:
COc1ccc(F)cc1C(=O)c1cc(-c2ccc(Cl)cc2)n(c1C)-c1ccc(cc1)S(N)(=O)=O
Structure:
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