Target
Neuronal acetylcholine receptor subunit alpha-7
Ligand
BDBM50309883
Substrate
n/a
Meas. Tech.
ChEMBL_611542 (CHEMBL1066386)
Ki
23±n/a nM
Citation
 O'Donnell, CJRogers, BNBronk, BSBryce, DKCoe, JWCook, KKDuplantier, AJEvrard, EHajós, MHoffmann, WEHurst, RSMaklad, NMather, RJMcLean, SNedza, FMO'Neill, BTPeng, LQian, WRottas, MMSands, SBSchmidt, AWShrikhande, AVSpracklin, DKWong, DFZhang, AZhang, L Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models. J Med Chem 53:1222-37 (2010) [PubMed]  Article
Target
Name:
Neuronal acetylcholine receptor subunit alpha-7
Synonyms:
ACHA7_RAT | Acra7 | Cholinergic, Nicotinic Alpha7 | Cholinergic, Nicotinic Alpha7/5-HT3 | Chrna7 | Neuronal acetylcholine receptor | Neuronal acetylcholine receptor (alpha7 nAChR) | Neuronal acetylcholine receptor subunit alpha 7 | Neuronal acetylcholine receptor subunit alpha-7 | Neuronal acetylcholine receptor subunit alpha-7 (nAChR alpha7) | Neuronal acetylcholine receptor subunit alpha-7 (nAChR)
Type:
Enzyme
Mol. Mass.:
56502.44
Organism:
Rattus norvegicus (Rat)
Description:
Q05941
Residue:
502
Sequence:
MCGGRGGIWLALAAALLHVSLQGEFQRRLYKELVKNYNPLERPVANDSQPLTVYFSLSLLQIMDVDEKNQVLTTNIWLQMSWTDHYLQWNMSEYPGVKNVRFPDGQIWKPDILLYNSADERFDATFHTNVLVNASGHCQYLPPGIFKSSCYIDVRWFPFDVQQCKLKFGSWSYGGWSLDLQMQEADISSYIPNGEWDLMGIPGKRNEKFYECCKEPYPDVTYTVTMRRRTLYYGLNLLIPCVLISALALLVFLLPADSGEKISLGITVLLSLTVFMLLVAEIMPATSDSVPLIAQYFASTMIIVGLSVVVTVIVLRYHHHDPDGGKMPKWTRIILLNWCAWFLRMKRPGEDKVRPACQHKPRRCSLASVELSAGAGPPTSNGNLLYIGFRGLEGMHCAPTPDSGVVCGRLACSPTHDEHLMHGAHPSDGDPDLAKILEEVRYIANRFRCQDESEVICSEWKFAACVVDRLCLMAFSVFTIICTIGILMSAPNFVEAVSKDFA
  
Inhibitor
Name:
BDBM50309883
Synonyms:
2-(6-(1H-Pyrazol-3-yl)oxazolo[4,5-b]pyridin-2-yl)-2,5-diazabicyclo[3.2.2]nonane | CHEMBL605840
Type:
Small organic molecule
Emp. Form.:
C16H18N6O
Mol. Mass.:
310.3537
SMILES:
C1CN2CCC1N(CC2)c1nc2ncc(cc2o1)-c1cc[nH]n1 |TLB:9:6:0.1:4.3,(22.19,-41.04,;21.57,-42.18,;21.65,-43.89,;20.66,-44.59,;20.96,-43.15,;22.25,-42.45,;23.66,-43.07,;24.03,-44.54,;23.02,-43.82,;24.99,-42.3,;26.48,-42.71,;27.33,-41.43,;28.86,-41.2,;29.42,-39.76,;28.45,-38.55,;26.92,-38.79,;26.37,-40.22,;24.93,-40.77,;28.93,-37.07,;30.39,-36.6,;30.41,-35.04,;28.93,-34.55,;28.01,-35.81,)|
Structure:
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