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Assay Detail

CHEMBL747778

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

Binding
The compound was tested in vitro for binding activity against M2 muscarinic receptor in homogenates of the brainstem of rat using [3H]quinuclidinyl benzilate (QNB) as radioligand
5
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and muscarinic M(2) subtype antagonistic activity of enantiomeric pairs of 3-demethylhimbacine (3-norhimbacine) and its C(4)-epimer.
Takadoi M, Yamaguchi K, Terashima S.
Bioorg Med Chem Lett (2002) 12 : 3271 -3273
PubMed 12392730 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.98 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111224 2 8.10
CHEMBL277642 HIMBACINE 1 7.90
CHEMBL324725 2 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111224 Ki = 7.943 nM 8.10
CHEMBL277642 HIMBACINE Ki = 12.59 nM 7.90
CHEMBL324725 Ki = 398.11 nM 6.40
CHEMBL324725 Ki = 398.11 nM 6.40
CHEMBL111224 Ki = 794.33 nM 6.10