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Assay Detail

CHEMBL929018

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

Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
8
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Rapid novel divergent synthesis and muscarinic agonist profile of all four optical isomers of N,N,N-trimethyl(6-methyl-1,4-dioxan-2-yl)methanaminium iodide.
Piergentili A, Quaglia W, Giannella M, Del Bello F, Buccioni M, Nesi M, Matucci R.
Bioorg Med Chem Lett (2008) 18 : 614 -618
PubMed 18077164 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 4.73 5.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL390842 1 5.47
CHEMBL667 ACETYLCHOLINE 4.0 1 5.15
CHEMBL228144 2 5.12
CHEMBL227429 1 4.63
CHEMBL227378 1 4.44
CHEMBL14 CARBACHOL 4.0 1 4.36
CHEMBL404557 1 4.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL390842 Ki = 3388.44 nM 5.47
CHEMBL667 ACETYLCHOLINE Ki = 7079.46 nM 5.15
CHEMBL228144 Ki = 7585.78 nM 5.12
CHEMBL227429 Ki = 23442.29 nM 4.63
CHEMBL228144 Ki = 35481.34 nM 4.45
CHEMBL227378 Ki = 36307.81 nM 4.44
CHEMBL14 CARBACHOL Ki = 43651.58 nM 4.36
CHEMBL404557 Ki = 61659.5 nM 4.21