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Assay Detail

CHEMBL917979

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

Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
14
Total Activities
14
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 Expert

Target

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

Publication

Synthesis, affinity profile, and functional activity of muscarinic antagonists with a 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine structure.
Dei S, Bellucci C, Buccioni M, Ferraroni M, Guandalini L, Manetti D, Martini E, Marucci G, Matucci R, Nesi M, Romanelli MN, Scapecchi S, Teodori E.
J Med Chem (2007) 50 : 1409 -1413
PubMed 17305327 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.88 9.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL376897 METHSCOPOLAMINE 4.0 1 9.87
CHEMBL219786 1 9.47
CHEMBL376057 1 9.23
CHEMBL375969 1 9.13
CHEMBL385328 1 9.05
CHEMBL222259 1 9.04
CHEMBL219825 1 8.84
CHEMBL376255 1 8.77
CHEMBL45454 1 8.75
CHEMBL376870 1 8.66
CHEMBL375073 1 8.61
CHEMBL220393 1 8.31
CHEMBL375851 1 8.30
CHEMBL373515 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL376897 METHSCOPOLAMINE Ki = 0.1349 nM 9.87
CHEMBL219786 Ki = 0.3388 nM 9.47
CHEMBL376057 Ki = 0.5888 nM 9.23
CHEMBL375969 Ki = 0.7413 nM 9.13
CHEMBL385328 Ki = 0.8913 nM 9.05
CHEMBL222259 Ki = 0.912 nM 9.04
CHEMBL219825 Ki = 1.445 nM 8.84
CHEMBL376255 Ki = 1.698 nM 8.77
CHEMBL45454 Ki = 1.778 nM 8.75
CHEMBL376870 Ki = 2.188 nM 8.66
CHEMBL375073 Ki = 2.455 nM 8.61
CHEMBL220393 Ki = 4.898 nM 8.31
CHEMBL375851 Ki = 5.012 nM 8.30
CHEMBL373515 Ki = 5.248 nM 8.28