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Assay Detail

CHEMBL2061180

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

Binding
Binding affinity to human muscle nAChR alpha1beta1gammadelta expressed in human TE-671 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type TE-671
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Acetylcholine receptor; alpha1/beta1/delta/gamma (CHEMBL1907588)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Diazaspirocyclic compounds as selective ligands for the α4β2 nicotinic acetylcholine receptor.
Strachan JP, Farias JJ, Zhang J, Caldwell WS, Bhatti BS.
Bioorg Med Chem Lett (2012) 22 : 5089 -5092
PubMed 22749278 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.36 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2057714 1 6.24
CHEMBL504652 TC-2216 1.0 1 5.24
CHEMBL2057712 1 5.00
CHEMBL2057713 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2057714 Ki = 580.0 nM 6.24
CHEMBL504652 TC-2216 Ki = 5700.0 nM 5.24
CHEMBL2057712 Ki = 9900.0 nM 5.00
CHEMBL2057713 Ki = 11000.0 nM 4.96