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Assay Detail

CHEMBL704479

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

Binding
Ability to displace [3H](-)-quinuclidinyl benzilate(QNB) from M2 receptor in rat heart homogenate
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biodistribution of iodine-125-labeled 1-azabicyclo[2.2.2]oct-3-yl alpha-hydroxy-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate. A new ligand for the potential imaging of muscarinic receptors by single photon emission computed tomography.
McPherson DW, DeHaven-Hudkins DL, Callahan AP, Knapp FF.
J Med Chem (1993) 36 : 848 -854
PubMed 8464039 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.80 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL558910 1 10.52
CHEMBL517712 ATROPINE 4.0 1 9.12
CHEMBL2112942 1 8.97
CHEMBL9967 PIRENZEPINE 2.0 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL558910 Ki = 0.03 nM 10.52
CHEMBL517712 ATROPINE Ki = 0.76 nM 9.12
CHEMBL2112942 Ki = 1.06 nM 8.97
CHEMBL9967 PIRENZEPINE Ki = 267.0 nM 6.57