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Assay Detail

CHEMBL747117

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

Functional
Antagonistic potency against Muscarinic acetylcholine receptor M2
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.
Melchiorre C, Andrisano V, Bolognesi ML, Budriesi R, Cavalli A, Cavrini V, Rosini M, Tumiatti V, Recanatini M.
J Med Chem (1998) 41 : 4186 -4189
PubMed 9784091 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 6.94 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27673 METHOCTRAMINE 1 7.92
CHEMBL422977 1 7.64
CHEMBL302179 1 6.98
CHEMBL132377 1 6.67
CHEMBL134382 1 6.67
CHEMBL11805 CAPROCTAMINE 1 6.39
CHEMBL134488 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27673 METHOCTRAMINE Kd = 12.02 nM 7.92
CHEMBL422977 Kd = 22.91 nM 7.64
CHEMBL302179 Kd = 104.71 nM 6.98
CHEMBL132377 Kd = 213.8 nM 6.67
CHEMBL134382 Kd = 213.8 nM 6.67
CHEMBL11805 CAPROCTAMINE Kd = 407.38 nM 6.39
CHEMBL134488 Kd = 501.19 nM 6.30