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Assay Detail

CHEMBL917981

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

Binding
Binding affinity to human cloned muscarinic receptor M5 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 M5 (CHEMBL2035)
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 8.95 9.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL219786 1 9.97
CHEMBL376057 1 9.70
CHEMBL376897 METHSCOPOLAMINE 4.0 1 9.68
CHEMBL375969 1 9.39
CHEMBL222259 1 9.11
CHEMBL219825 1 8.92
CHEMBL385328 1 8.87
CHEMBL376255 1 8.70
CHEMBL376870 1 8.70
CHEMBL45454 1 8.55
CHEMBL220393 1 8.49
CHEMBL375073 1 8.49
CHEMBL375851 1 8.46
CHEMBL373515 1 8.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL219786 Ki = 0.1072 nM 9.97
CHEMBL376057 Ki = 0.1995 nM 9.70
CHEMBL376897 METHSCOPOLAMINE Ki = 0.2089 nM 9.68
CHEMBL375969 Ki = 0.4074 nM 9.39
CHEMBL222259 Ki = 0.7762 nM 9.11
CHEMBL219825 Ki = 1.202 nM 8.92
CHEMBL385328 Ki = 1.349 nM 8.87
CHEMBL376255 Ki = 1.995 nM 8.70
CHEMBL376870 Ki = 1.995 nM 8.70
CHEMBL45454 Ki = 2.818 nM 8.55
CHEMBL220393 Ki = 3.236 nM 8.49
CHEMBL375073 Ki = 3.236 nM 8.49
CHEMBL375851 Ki = 3.467 nM 8.46
CHEMBL373515 Ki = 5.623 nM 8.25