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Assay Detail

CHEMBL4183544

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

Binding
Displacement of [3H]NMS from muscarinic receptor in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 5 — Multiple protein complex / RNA
Curated By Intermediate

Target

Muscarinic acetylcholine receptor (CHEMBL1907609)
Type PROTEIN FAMILY
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
IC50 8 7.97 8.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4215958 1 8.53
CHEMBL4216478 1 8.49
CHEMBL1382 TOLTERODINE 4.0 1 8.20
CHEMBL4204282 1 8.15
CHEMBL4211510 1 7.88
CHEMBL4206276 1 7.86
CHEMBL4208614 1 7.74
CHEMBL4207504 1 6.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4215958 IC50 = 2.951 nM 8.53
CHEMBL4216478 IC50 = 3.236 nM 8.49
CHEMBL1382 TOLTERODINE IC50 = 6.31 nM 8.20
CHEMBL4204282 IC50 = 7.079 nM 8.15
CHEMBL4211510 IC50 = 13.18 nM 7.88
CHEMBL4206276 IC50 = 13.8 nM 7.86
CHEMBL4208614 IC50 = 18.2 nM 7.74
CHEMBL4207504 IC50 = 123.03 nM 6.91