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Assay Detail

CHEMBL3362771

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

Binding
Antagonist activity at rat alpha3beta4 nAChR transfected in HEK293 cells by FLIPR membrane potential blue (FMP) assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907593)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Synthesis and Pharmacological Evaluation of DHβE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists.
Jepsen TH, Jensen AA, Lund MH, Glibstrup E, Kristensen JL.
ACS Med Chem Lett (2014) 5 : 766 -770
PubMed 25050162 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.00 4.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293950 1 4.00
CHEMBL3318897 1 -
CHEMBL3318902 1 -
CHEMBL3318896 1 -
CHEMBL3318892 1 -
CHEMBL3318901 1 -
CHEMBL3318889 1 -
CHEMBL3318893 1 -
CHEMBL3318894 1 -
CHEMBL3318895 1 -
CHEMBL3318890 1 -
CHEMBL3318898 1 -
CHEMBL3318899 1 -
CHEMBL3318900 1 -
CHEMBL3318891 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293950 IC50 = 100000.0 nM 4.00
CHEMBL3318897 IC50 > 300000.0 nM -
CHEMBL3318902 IC50 > 300000.0 nM -
CHEMBL3318896 IC50 > 300000.0 nM -
CHEMBL3318892 IC50 > 300000.0 nM -
CHEMBL3318901 IC50 > 300000.0 nM -
CHEMBL3318889 IC50 > 300000.0 nM -
CHEMBL3318893 IC50 > 300000.0 nM -
CHEMBL3318894 IC50 > 300000.0 nM -
CHEMBL3318895 IC50 > 300000.0 nM -
CHEMBL3318890 IC50 > 300000.0 nM -
CHEMBL3318898 IC50 > 300000.0 nM -
CHEMBL3318899 IC50 > 300000.0 nM -
CHEMBL3318900 IC50 > 300000.0 nM -
CHEMBL3318891 IC50 > 300000.0 nM -