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Assay Detail

CHEMBL2014883

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

Binding
Displacement of [3H]epibatidine from rat alpha7 nAChR expressed in HEK292 cells after 4 hrs by liquid scintillation counting
7
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK292
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Consequences of linker length alteration of the α7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333.
Beinat C, Banister SD, van Prehn S, Doddareddy MR, Hibbs D, Sako M, Chebib M, Tran T, Al-Muhtasib N, Xiao Y, Kassiou M.
Bioorg Med Chem Lett (2012) 22 : 2380 -2384
PubMed 22410083 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 5.86 6.30
EC50 2 5.67 5.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1084615 2 6.30
CHEMBL576234 1 5.55
CHEMBL2012935 1 5.41
CHEMBL2010825 1 -
CHEMBL2012936 1 -
CHEMBL2012937 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1084615 Ki = 500.0 nM 6.30
CHEMBL1084615 EC50 = 1650.0 nM 5.78
CHEMBL576234 EC50 = 2840.0 nM 5.55
CHEMBL2012935 Ki = 3900.0 nM 5.41
CHEMBL2010825 Ki > 10000.0 nM -
CHEMBL2012936 Ki > 10000.0 nM -
CHEMBL2012937 Ki > 10000.0 nM -