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Assay Detail

CHEMBL2343549

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

Binding
Inhibition of human alpha3beta4 nAChR expressed in CHO cells assessed as inhibition of calcium influx by calcium-4 based FLIPR analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Pharmacological properties and predicted binding mode of arylmethylene quinuclidine-like derivatives at the α3β4 nicotinic acetylcholine receptor (nAChR).
Kombo DC, Hauser TA, Grinevich VP, Melvin MS, Strachan JP, Sidach SS, Chewning J, Fedorov N, Tallapragada K, Breining SR, Miller CH.
Bioorg Med Chem Lett (2013) 23 : 1450 -1455
PubMed 23352509 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.78 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2332278 1 7.10
CHEMBL2332280 1 7.00
CHEMBL2332279 1 6.70
CHEMBL478358 1 5.22
CHEMBL2179959 1 5.00
CHEMBL2332276 1 4.82
CHEMBL2332277 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2332278 IC50 = 80.0 nM 7.10
CHEMBL2332280 IC50 = 100.0 nM 7.00
CHEMBL2332279 IC50 = 200.0 nM 6.70
CHEMBL478358 IC50 = 6000.0 nM 5.22
CHEMBL2179959 IC50 = 10000.0 nM 5.00
CHEMBL2332276 IC50 = 15000.0 nM 4.82
CHEMBL2332277 IC50 = 23000.0 nM 4.64