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Assay Detail

CHEMBL3367783

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

Binding
Displacement of [3H]NMS from human muscarinic M2 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
9
Total Activities
9
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 Autocuration

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites.
Del Bello F, Bonifazi A, Quaglia W, Mazzolari A, Barocelli E, Bertoni S, Matucci R, Nesi M, Piergentili A, Vistoli G.
Bioorg Med Chem Lett (2014) 24 : 3255 -3259
PubMed 24980056 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.81 6.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL168815 CEVIMELINE 4.0 1 6.07
CHEMBL387632 1 5.92
CHEMBL14 CARBACHOL 4.0 1 5.91
CHEMBL3309718 1 5.76
CHEMBL390842 1 5.68
CHEMBL74300 1 5.49
CHEMBL3309715 1 -
CHEMBL3359597 1 -
CHEMBL3309717 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL168815 CEVIMELINE Ki = 851.14 nM 6.07
CHEMBL387632 Ki = 1202.26 nM 5.92
CHEMBL14 CARBACHOL Ki = 1230.27 nM 5.91
CHEMBL3309718 Ki = 1737.8 nM 5.76
CHEMBL390842 Ki = 2089.3 nM 5.68
CHEMBL74300 Ki = 3235.94 nM 5.49
CHEMBL3309715 Ki > 100000.0 nM -
CHEMBL3359597 Ki > 100000.0 nM -
CHEMBL3309717 Ki > 100000.0 nM -