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Assay Detail

CHEMBL918562

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

Binding
Binding affinity to human cloned muscarinic receptor M1 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 M1 (CHEMBL216)
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 9.16 9.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL219786 1 9.93
CHEMBL376057 1 9.60
CHEMBL375969 1 9.53
CHEMBL376897 METHSCOPOLAMINE 4.0 1 9.49
CHEMBL376870 1 9.46
CHEMBL222259 1 9.30
CHEMBL375073 1 9.12
CHEMBL219825 1 9.04
CHEMBL220393 1 9.02
CHEMBL45454 1 8.96
CHEMBL385328 1 8.86
CHEMBL376255 1 8.83
CHEMBL375851 1 8.63
CHEMBL373515 1 8.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL219786 Ki = 0.1175 nM 9.93
CHEMBL376057 Ki = 0.2512 nM 9.60
CHEMBL375969 Ki = 0.2951 nM 9.53
CHEMBL376897 METHSCOPOLAMINE Ki = 0.3236 nM 9.49
CHEMBL376870 Ki = 0.3467 nM 9.46
CHEMBL222259 Ki = 0.5012 nM 9.30
CHEMBL375073 Ki = 0.7586 nM 9.12
CHEMBL219825 Ki = 0.912 nM 9.04
CHEMBL220393 Ki = 0.955 nM 9.02
CHEMBL45454 Ki = 1.096 nM 8.96
CHEMBL385328 Ki = 1.38 nM 8.86
CHEMBL376255 Ki = 1.479 nM 8.83
CHEMBL375851 Ki = 2.344 nM 8.63
CHEMBL373515 Ki = 3.467 nM 8.46