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Assay Detail

CHEMBL750055

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

Functional
Stimulation of cation efflux in Nicotinic acetylcholine receptor alpha3-betaX subtype expressing IMR-32 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type IMR-32
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Nicotinic acetylcholine receptor alpha3/betaX (CHEMBL2111384)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist.
Lin NH, Gunn DE, Li Y, He Y, Bai H, Ryther KB, Kuntzweiler T, Donnelly-Roberts DL, Anderson DJ, Campbell JE, Sullivan JP, Arneric SP, Holladay MW.
Bioorg Med Chem Lett (1998) 8 : 249 -254
PubMed 9871663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 4.89 5.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83473 1 5.54
CHEMBL86162 1 4.87
CHEMBL84692 1 4.74
CHEMBL84149 1 4.71
CHEMBL84887 1 4.57
CHEMBL86079 1 -
CHEMBL85998 1 -
CHEMBL84827 1 -
CHEMBL312964 1 -
CHEMBL315212 1 -
CHEMBL85956 1 -
CHEMBL312962 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83473 EC50 = 2900.0 nM 5.54
CHEMBL86162 EC50 = 13400.0 nM 4.87
CHEMBL84692 EC50 = 18200.0 nM 4.74
CHEMBL84149 EC50 = 19400.0 nM 4.71
CHEMBL84887 EC50 = 27100.0 nM 4.57
CHEMBL86079 EC50 > 1000000.0 nM -
CHEMBL85998 EC50 > 1000000.0 nM -
CHEMBL84827 EC50 > 1000000.0 nM -
CHEMBL312964 EC50 > 1000000.0 nM -
CHEMBL315212 EC50 > 1000000.0 nM -
CHEMBL85956 EC50 > 1000000.0 nM -
CHEMBL312962 EC50 > 1000000.0 nM -