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Assay Detail

CHEMBL4051385

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

Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the M2 Muscarinic Acetylcholine Receptor.
Pegoli A, She X, Wifling D, Hübner H, Bernhardt G, Gmeiner P, Keller M.
J Med Chem (2017) 60 : 3314 -3334
PubMed 28388054 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.26 7.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4097258 1 7.81
CHEMBL4079233 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4097258 Ki = 15.49 nM 7.81
CHEMBL4079233 Ki = 199.53 nM 6.70