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Assay Detail

CHEMBL5239848

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

Binding
Binding affinity to human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin recruitment preincubated for 30 mins followed by carbachol stimulation and measured after 90 mins by PathHunter assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis, Characterization, and Application of Muscarinergic M<sub>3</sub> Receptor Ligands Linked to Fluorescent Dyes.
Köckenberger J, Fischer O, Konopa A, Bergwinkl S, Mühlich S, Gmeiner P, Kutta RJ, Hübner H, Keller M, Heinrich MR.
J Med Chem (2022) 65 : 16494 -16509
PubMed 36484801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.36 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5285607 1 6.37
CHEMBL5271406 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5285607 IC50 = 430.0 nM 6.37
CHEMBL5271406 IC50 = 450.0 nM 6.35