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Assay Detail

CHEMBL4051395

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

Binding
Binding affinity to human muscarinic acetylcholine receptor M2 expressed in CHOK9 cell homogenate after 2 hrs by liquid scintillation counting assay
4
Total Activities
2
Compounds Tested
2
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 M2 (CHEMBL211)
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
Bmax 2 - -
Kd 2 9.09 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4089543 2 9.66
CHEMBL4068393 2 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4089543 Kd = 0.22 nM 9.66
CHEMBL4068393 Kd = 3.0 nM 8.52
CHEMBL4068393 Bmax = 4900.0 disintegrations/minute -
CHEMBL4089543 Bmax = 620.0 disintegrations/minute -