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Assay Detail

CHEMBL1000461

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

Binding
Displacement of [125I]alpha-bungarotoxin from alpha7 nAChR in rat cortical membrane
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Epiboxidine and novel-related analogues: a convenient synthetic approach and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes.
Rizzi L, Dallanoce C, Matera C, Magrone P, Pucci L, Gotti C, Clementi F, De Amici M.
Bioorg Med Chem Lett (2008) 18 : 4651 -4654
PubMed 18644719 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.60 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL503604 EXO-EPIBOXIDINE 1 8.22
CHEMBL504313 ENDO-EPIBOXIDINE 1 6.64
CHEMBL525968 1 6.41
CHEMBL274525 ABT-418 1 5.92
CHEMBL449716 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL503604 EXO-EPIBOXIDINE Ki = 6.0 nM 8.22
CHEMBL504313 ENDO-EPIBOXIDINE Ki = 230.0 nM 6.64
CHEMBL525968 Ki = 394.0 nM 6.41
CHEMBL274525 ABT-418 Ki = 1200.0 nM 5.92
CHEMBL449716 Ki = 1600.0 nM 5.80