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Assay Detail

CHEMBL744767

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Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M1
10
Total Activities
10
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

Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes.
Sagara Y, Sagara T, Mase T, Kimura T, Numazawa T, Fujikawa T, Noguchi K, Ohtake N.
J Med Chem (2002) 45 : 984 -987
PubMed 11831911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.43 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL517712 ATROPINE 4.0 1 9.60
CHEMBL1346 DARIFENACIN 4.0 1 8.26
CHEMBL2112957 1 7.85
CHEMBL2112959 1 7.44
CHEMBL369062 1 7.11
CHEMBL2112956 1 6.96
CHEMBL2112955 1 6.92
CHEMBL2112961 1 6.82
CHEMBL2112958 1 6.82
CHEMBL177040 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL517712 ATROPINE Ki = 0.25 nM 9.60
CHEMBL1346 DARIFENACIN Ki = 5.5 nM 8.26
CHEMBL2112957 Ki = 14.0 nM 7.85
CHEMBL2112959 Ki = 36.0 nM 7.44
CHEMBL369062 Ki = 77.0 nM 7.11
CHEMBL2112956 Ki = 110.0 nM 6.96
CHEMBL2112955 Ki = 120.0 nM 6.92
CHEMBL2112961 Ki = 150.0 nM 6.82
CHEMBL2112958 Ki = 150.0 nM 6.82
CHEMBL177040 Ki = 300.0 nM 6.52