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Assay Detail

CHEMBL748254

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

Binding
Affinity for human muscarinic acetylcholine receptor M2 expressed in CHO-K1 cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.
Melchiorre C, Bolognesi ML, Budriesi R, Ghelardini C, Chiarini A, Minarini A, Rosini M, Tumiatti V, Wade EJ.
J Med Chem (2001) 44 : 4035 -4038
PubMed 11708906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.94 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130835 PIPERTRAMINE AMIDE 1 8.04
CHEMBL27673 METHOCTRAMINE 1 7.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130835 PIPERTRAMINE AMIDE Ki = 9.2 nM 8.04
CHEMBL27673 METHOCTRAMINE Ki = 14.3 nM 7.84