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BioAssay: AID 705812

Agonist activity at alpha4beta2 nAChR high sensitivity form

The potential for nicotinic ligands with affinity for the alpha4beta2 or alpha7 subtypes to treat such diverse diseases as nicotine addiction, neuropathic pain, and neurodegenerative and cognitive disorders has been exhibited clinically for several compounds while preclinical activity in relevant in vivo models has been demonstrated for many more. For several therapeutic programs, we sought more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 705812
Data Source: ChEMBL (873555)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-06-29
Modify Date: 2013-11-18

Data Table ( Complete ):           Active    All
BioActive Compound: 1
Description:
Title: Structure-activity studies of 7-heteroaryl-3-azabicyclo[3.3.1]non-6-enes: a novel class of highly potent nicotinic receptor ligands.

Abstract: The potential for nicotinic ligands with affinity for the alpha4beta2 or alpha7 subtypes to treat such diverse diseases as nicotine addiction, neuropathic pain, and neurodegenerative and cognitive disorders has been exhibited clinically for several compounds while preclinical activity in relevant in vivo models has been demonstrated for many more. For several therapeutic programs, we sought nicotinic ligands with various combinations of affinity and function across both subtypes, with an emphasis on dual alpha4beta2-alpha7 ligands, to explore the possibility of synergistic effects. We report here the structure-activity relationships (SAR) for a novel series of 7-heteroaryl-3-azabicyclo[3.3.1]non-6-enes and characterize many of the analogues for activity at multiple nicotinic subtypes.
(PMID: 23025891)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Putative Target:

ChEMBL Target ID: 104283
Target Type: PROTEIN COMPLEX
Pref Name: Neuronal acetylcholine receptor; alpha4/beta2
Synonyms: Neuronal acetylcholine receptor subunit alpha-4;Neuronal acetylcholine receptor subunit beta-2;
Gene Name: CHRNA4;NACRA4;CHRNB2;
Protein Accession: P43681;P17787;
Protein GI: 1351848;113105;
Organism: Homo sapiens
Tax ID: 9606
Target Classification 1: ion channel lgic cys_loop ach cationic ns chrn alpha
Target Classification 2: ion channel lgic cys_loop ach cationic ns chrn beta
Confidence: Homologous protein complex subunits assigned
Relationship Type: Homologous protein target assigned
Categorized Comment
ChEMBL Assay Type: Functional

ChEMBL Assay Data Source: Scientific Literature

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50*EC50 PubChem standard valueFloatμM
2EC50 activity commentEC50 activity commentString
3EC50 standard flagEC50 standard flagInteger
4EC50 qualifierEC50 qualifierString
5EC50 published valueEC50 published valueFloatμM
6EC50 standard valueEC50 standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
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