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Assay Detail

CHEMBL4361684

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

Binding
Displacement of [125I]alpha-bungarotoxin from alpha7nAChR in rat hippocampus membrane
17
Total Activities
17
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

Novel N-aryl nicotinamide derivatives: Taking stock on 3,6-diazabicyclo[3.1.1]heptanes as ligands for neuronal acetylcholine receptors.
Murineddu G, Gotti C, Asproni B, Corona P, Martinello K, Plutino S, Fucile S, Temml V, Moretti M, Viani P, Schuster D, Piras S, Deligia F, Pinna GA.
Eur J Med Chem (2019) 180 : 51 -61
PubMed 31299587 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 5.11 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4543232 1 6.00
CHEMBL4472986 1 5.97
CHEMBL4462607 1 5.64
CHEMBL4571320 1 5.62
CHEMBL4453342 1 5.47
CHEMBL4444866 1 5.08
CHEMBL4447564 1 4.89
CHEMBL4441630 1 4.64
CHEMBL4435435 1 4.63
CHEMBL4565381 1 4.55
CHEMBL4460815 1 4.48
CHEMBL4530364 1 4.37
CHEMBL4532589 1 -
CHEMBL4556523 1 -
CHEMBL4581470 1 -
CHEMBL4476500 1 -
CHEMBL298826 (-)-EPIBATIDINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4543232 Ki = 1000.0 nM 6.00
CHEMBL4472986 Ki = 1070.0 nM 5.97
CHEMBL4462607 Ki = 2300.0 nM 5.64
CHEMBL4571320 Ki = 2400.0 nM 5.62
CHEMBL4453342 Ki = 3400.0 nM 5.47
CHEMBL4444866 Ki = 8400.0 nM 5.08
CHEMBL4447564 Ki = 13000.0 nM 4.89
CHEMBL4441630 Ki = 22900.0 nM 4.64
CHEMBL4435435 Ki = 23400.0 nM 4.63
CHEMBL4565381 Ki = 27900.0 nM 4.55
CHEMBL4460815 Ki = 33200.0 nM 4.48
CHEMBL4530364 Ki = 43100.0 nM 4.37
CHEMBL4532589 Ki > 50000.0 nM -
CHEMBL4556523 Ki > 50000.0 nM -
CHEMBL4581470 Ki > 50000.0 nM -
CHEMBL4476500 Ki > 50000.0 nM -
CHEMBL298826 (-)-EPIBATIDINE Ki - -