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Assay Detail

CHEMBL2188609

Review assay metadata, readout intent, target linkage, and publication context from the same page.

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

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Brain
Confidence 7 — Homologous single protein target
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 10.40 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59986 1 10.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59986 Ki = 0.04 nM 10.40