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Assay Detail

CHEMBL746585

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Binding
Affinity versus [3H]oxotremorine M (agonist) binding to Muscarinic acetylcholine receptor M1 in Rat Cerebral Cortical Membranes, (Kd=0.75 nM)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M1 (CHEMBL276)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.
Pei XF, Gupta TH, Badio B, Padgett WL, Daly JW.
J Med Chem (1998) 41 : 2047 -2055
PubMed 9622546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.71 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64000 1 8.25
CHEMBL12587 MUSCARINE 1 7.57
CHEMBL14 CARBACHOL 4.0 1 7.51
CHEMBL64788 1 6.58
CHEMBL294273 1 5.58
CHEMBL2115494 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64000 Ki = 5.6 nM 8.25
CHEMBL12587 MUSCARINE Ki = 27.0 nM 7.57
CHEMBL14 CARBACHOL Ki = 31.0 nM 7.51
CHEMBL64788 Ki = 260.0 nM 6.58
CHEMBL294273 Ki = 2600.0 nM 5.58
CHEMBL2115494 Ki = 18000.0 nM 4.75