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Assay Detail

CHEMBL714427

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

Binding
Ability to displace [3H]pirenzepine (PZ) from M1 receptor in rat cortex homogenate
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor M1 (CHEMBL276)
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 9.20 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL558910 1 9.82
CHEMBL517712 ATROPINE 4.0 1 9.59
CHEMBL2112942 1 9.11
CHEMBL9967 PIRENZEPINE 2.0 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL558910 Ki = 0.15 nM 9.82
CHEMBL517712 ATROPINE Ki = 0.26 nM 9.59
CHEMBL2112942 Ki = 0.78 nM 9.11
CHEMBL9967 PIRENZEPINE Ki = 5.21 nM 8.28