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Assay Detail

CHEMBL744901

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

Binding
Compound was evaluated for its affinity towards Muscarinic acetylcholine receptor M2, using [3H]- N-methyl-scopolamine, a radioligand displacement assay in rat heart membranes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Heart
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M2 (CHEMBL309)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological activity of enantiomers of a conformationally restricted muscarone analog
Wu ES, Mack RA, Kover A, Loch JT, Mullen G, Murray RJ, Gordon JC, Machulskis AC, McCreedy SA, Blosser JC
Bioorg Med Chem Lett (1995) 5 : 1813 -1818
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.08 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50898 1 5.60
CHEMBL40121 1 5.28
CHEMBL550 PILOCARPINE 4.0 1 5.01
CHEMBL50831 1 4.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50898 Ki = 2500.0 nM 5.60
CHEMBL40121 Ki = 5300.0 nM 5.28
CHEMBL550 PILOCARPINE Ki = 9800.0 nM 5.01
CHEMBL50831 Ki = 37000.0 nM 4.43