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Assay Detail

CHEMBL3362769

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

Binding
Displacement of [3H]epibatidine from rat alpha3beta4 nAChR transfected in HEK293 cells after 4 hrs by scintillation count analysis
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
Ki 15 4.00 4.00

Compounds Tested

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

Activity Data

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