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Assay Detail

CHEMBL1272633

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 brain cell membrane
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of 9-fluoro substituted (-)-cytisine derivatives as ligands with high affinity for nicotinic receptors.
Houllier N, Gopisetti J, Lestage P, Lasne MC, Rouden J.
Bioorg Med Chem Lett (2010) 20 : 6667 -6670
PubMed 20880707 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.13 6.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL599685 1 6.95
CHEMBL365956 1 6.40
CHEMBL497939 CYTISINICLINE 3.0 1 6.00
CHEMBL1269417 1 6.00
CHEMBL1269418 1 5.70
CHEMBL1269456 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL599685 Ki = 112.0 nM 6.95
CHEMBL365956 Ki = 401.1 nM 6.40
CHEMBL497939 CYTISINICLINE Ki = 1000.0 nM 6.00
CHEMBL1269417 Ki = 1000.0 nM 6.00
CHEMBL1269418 Ki = 2000.0 nM 5.70
CHEMBL1269456 Ki = 2000.0 nM 5.70