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Assay Detail

CHEMBL4183541

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Binding
Displacement of [3H]NMS from muscarinic receptor M2 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M2 (CHEMBL309)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Ligand-Phospholipid Conjugation: A Versatile Strategy for Developing Long-Acting Ligands That Bind to Membrane Proteins by Restricting the Subcellular Localization of the Ligand.
Kawamura S, Ito Y, Hirokawa T, Hikiyama E, Yamada S, Shuto S.
J Med Chem (2018) 61 : 4020 -4029
PubMed 29652494 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.31 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1382 TOLTERODINE 4.0 1 8.57
CHEMBL271108 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1382 TOLTERODINE Ki = 2.7 nM 8.57
CHEMBL271108 Ki = 9.0 nM 8.05