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Assay Detail

CHEMBL752536

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

Binding
Binding affinity towards alpha3-beta4 subtype of neuronal nicotinic acetylcholine receptor (nAChR) using [3H]epibatidine as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha3/beta2 (CHEMBL2109234)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha7 selectivity.
Karig G, Large JM, Sharples CG, Sutherland A, Gallagher T, Wonnacott S.
Bioorg Med Chem Lett (2003) 13 : 2825 -2828
PubMed 14611837 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.02 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1086655 1 8.19
CHEMBL444572 1 7.65
CHEMBL329084 1 7.25
CHEMBL96828 1 6.33
CHEMBL93983 1 5.70
CHEMBL419700 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1086655 Ki = 6.5 nM 8.19
CHEMBL444572 Ki = 22.5 nM 7.65
CHEMBL329084 Ki = 56.3 nM 7.25
CHEMBL96828 Ki = 468.0 nM 6.33
CHEMBL93983 Ki = 1990.0 nM 5.70
CHEMBL419700 Ki > 50000.0 nM -