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Assay Detail

CHEMBL861933

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

Binding
Inhibition of [3H]NMS dissociation from porcine heart muscarinic receptor M2
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M2 (CHEMBL4781)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Design, synthesis, and action of oxotremorine-related hybrid-type allosteric modulators of muscarinic acetylcholine receptors.
Disingrini T, Muth M, Dallanoce C, Barocelli E, Bertoni S, Kellershohn K, Mohr K, De Amici M, Holzgrabe U.
J Med Chem (2006) 49 : 366 -372
PubMed 16392821 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 8.07 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274413 NAPHMETHONIUM 1 9.29
CHEMBL380572 1 8.96
CHEMBL381913 1 8.63
CHEMBL199636 1 8.61
CHEMBL266295 1 7.87
CHEMBL382659 1 7.67
CHEMBL382846 1 7.30
CHEMBL197604 1 7.22
CHEMBL201016 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274413 NAPHMETHONIUM EC50 = 0.5129 nM 9.29
CHEMBL380572 EC50 = 1.096 nM 8.96
CHEMBL381913 EC50 = 2.344 nM 8.63
CHEMBL199636 EC50 = 2.455 nM 8.61
CHEMBL266295 EC50 = 13.49 nM 7.87
CHEMBL382659 EC50 = 21.38 nM 7.67
CHEMBL382846 EC50 = 50.12 nM 7.30
CHEMBL197604 EC50 = 60.26 nM 7.22
CHEMBL201016 EC50 = 83.18 nM 7.08