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Assay Detail

CHEMBL3095630

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

Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M3 (CHEMBL245)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Molecular basis for the long duration of action and kinetic selectivity of tiotropium for the muscarinic M3 receptor.
Tautermann CS, Kiechle T, Seeliger D, Diehl S, Wex E, Banholzer R, Gantner F, Pieper MP, Casarosa P.
J Med Chem (2013) 56 : 8746 -8756
PubMed 24088171 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 10.80 10.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545181 TIOTROPIUM BROMIDE 4.0 1 10.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545181 TIOTROPIUM BROMIDE Ki = 0.01585 nM 10.80