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Assay Detail

CHEMBL3367253

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

Binding
Displacement of [3H]EB from rat nAChR alpha7 expressed in HEK293 cell membranes by liquid scintillation counting
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Investigations of amide bond variation and biaryl modification in analogues of α7 nAChR agonist SEN12333.
Beinat C, Reekie T, Hibbs D, Xie T, Olson TT, Xiao Y, Harvey A, O'Connor S, Coles C, Tsanaktsidis J, Kassiou M.
Eur J Med Chem (2014) 84 : 200 -205
PubMed 25019477 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.63 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1084615 1 6.17
CHEMBL3318012 1 5.75
CHEMBL3318010 1 5.64
CHEMBL3318011 1 4.96
CHEMBL3318013 1 -
CHEMBL3318014 1 -
CHEMBL3318015 1 -
CHEMBL3318016 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1084615 Ki = 670.0 nM 6.17
CHEMBL3318012 Ki = 1800.0 nM 5.75
CHEMBL3318010 Ki = 2300.0 nM 5.64
CHEMBL3318011 Ki = 11000.0 nM 4.96
CHEMBL3318013 Ki = 216000.0 nM -
CHEMBL3318014 Ki = 236000.0 nM -
CHEMBL3318015 Ki = 165000.0 nM -
CHEMBL3318016 Ki = 156000.0 nM -