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Assay Detail

CHEMBL700295

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

Functional
Ability to stimulate Rb+ efflux from human IMR-32 cell preparations containing human alpha3-betaX receptors
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type IMR-32
Confidence 1 — Organism
Curated By Intermediate

Target

IMR-32 (CHEMBL614585)
Type CELL-LINE
Organism Homo sapiens

Publication

Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors.
Abreo MA, Lin NH, Garvey DS, Gunn DE, Hettinger AM, Wasicak JT, Pavlik PA, Martin YC, Donnelly-roberts DL, Anderson DJ, Sullivan JP, Williams M, Arneric SP, Holladay MW.
J Med Chem (1996) 39 : 817 -825
PubMed 8632405 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 5.36 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 1 8.15
CHEMBL59986 1 6.16
CHEMBL262769 1 5.96
CHEMBL440195 1 5.24
CHEMBL84149 2 4.92
CHEMBL3 NICOTINE 4.0 1 4.68
CHEMBL293435 1 4.52
CHEMBL168780 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE EC50 = 7.0 nM 8.15
CHEMBL59986 EC50 = 700.0 nM 6.16
CHEMBL262769 EC50 = 1100.0 nM 5.96
CHEMBL440195 EC50 = 5800.0 nM 5.24
CHEMBL84149 EC50 = 12000.0 nM 4.92
CHEMBL3 NICOTINE EC50 = 21000.0 nM 4.68
CHEMBL293435 EC50 = 30000.0 nM 4.52
CHEMBL168780 EC50 = 38000.0 nM 4.42
CHEMBL84149 EC50 = 63000.0 nM 4.20