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Assay Detail

CHEMBL3607039

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 hippocampus membranes by liquid scintillation counting method
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Chemistry and Pharmacology of a Series of Unichiral Analogues of 2-(2-Pyrrolidinyl)-1,4-benzodioxane, Prolinol Phenyl Ether, and Prolinol 3-Pyridyl Ether Designed as α4β2-Nicotinic Acetylcholine Receptor Agonists.
Bolchi C, Valoti E, Gotti C, Fasoli F, Ruggeri P, Fumagalli L, Binda M, Mucchietto V, Sciaccaluga M, Budriesi R, Fucile S, Pallavicini M.
J Med Chem (2015) 58 : 6665 -6677
PubMed 26225816 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 6.01 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3603931 1 7.54
CHEMBL3603941 1 7.24
CHEMBL3603929 1 6.92
CHEMBL3603930 1 6.67
CHEMBL3 NICOTINE 4.0 1 6.63
CHEMBL3603933 1 6.49
CHEMBL3603947 1 6.41
CHEMBL3603942 1 6.13
CHEMBL3603939 1 5.94
CHEMBL3603932 1 5.92
CHEMBL3603934 1 5.46
CHEMBL3603948 1 5.21
CHEMBL3603938 1 5.05
CHEMBL3603945 1 5.03
CHEMBL3603937 1 4.82
CHEMBL3603946 1 4.67
CHEMBL3603935 1 -
CHEMBL3603936 1 -
CHEMBL3603944 1 -
CHEMBL3603940 1 -
CHEMBL3603943 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3603931 Ki = 29.0 nM 7.54
CHEMBL3603941 Ki = 57.0 nM 7.24
CHEMBL3603929 Ki = 119.0 nM 6.92
CHEMBL3603930 Ki = 212.0 nM 6.67
CHEMBL3 NICOTINE Ki = 234.0 nM 6.63
CHEMBL3603933 Ki = 321.0 nM 6.49
CHEMBL3603947 Ki = 388.0 nM 6.41
CHEMBL3603942 Ki = 743.0 nM 6.13
CHEMBL3603939 Ki = 1150.0 nM 5.94
CHEMBL3603932 Ki = 1200.0 nM 5.92
CHEMBL3603934 Ki = 3500.0 nM 5.46
CHEMBL3603948 Ki = 6100.0 nM 5.21
CHEMBL3603938 Ki = 8900.0 nM 5.05
CHEMBL3603945 Ki = 9400.0 nM 5.03
CHEMBL3603937 Ki = 15200.0 nM 4.82
CHEMBL3603946 Ki = 21500.0 nM 4.67
CHEMBL3603935 Ki - -
CHEMBL3603936 Ki - -
CHEMBL3603944 Ki - -
CHEMBL3603940 Ki - -
CHEMBL3603943 Ki - -