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Assay Detail

CHEMBL2188166

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Binding
Binding affinity to alpha4beta2 nAChR
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of highly potent and selective α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II.
Yu LF, Eaton JB, Fedolak A, Zhang HK, Hanania T, Brunner D, Lukas RJ, Kozikowski AP.
J Med Chem (2012) 55 : 9998 -10009
PubMed 23092294 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 9.40 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1076903 VARENICLINE 4.0 1 9.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1076903 VARENICLINE Ki = 0.4 nM 9.40