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Assay Detail

CHEMBL823923

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

Functional
Tested for functional activity against neuronal nicotinic acetylcholine receptor(nAChR) expressed in K177 cells using isotopic rubidium efflux assay.
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type K177
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Novel 2-(2-furo[3,2-b]pyridinyl) pyrrolidines: potent neuronal nicotinic acetylcholine receptor ligands
Elliott RL, Ryther KB, Anderson DJ, Piattoni-Kaplan M, Kuntzweiler TA, Donnelly-Roberts D, Arneric SP, Holladay MW
Bioorg Med Chem Lett (1997) 7 : 2703 -2708
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 5.37 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL84149 1 6.12
CHEMBL93883 1 5.50
CHEMBL3 NICOTINE 4.0 1 5.30
CHEMBL274525 ABT-418 1 4.97
CHEMBL328323 1 4.96
CHEMBL327441 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL84149 EC50 = 750.0 nM 6.12
CHEMBL93883 EC50 = 3200.0 nM 5.50
CHEMBL3 NICOTINE EC50 = 5000.0 nM 5.30
CHEMBL274525 ABT-418 EC50 = 10600.0 nM 4.97
CHEMBL328323 EC50 = 11000.0 nM 4.96
CHEMBL327441 EC50 > 1000000.0 nM -