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Assay Detail

CHEMBL746581

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

Binding
In vitro binding affinity towards Muscarinic acetylcholine receptor M1 using [3H]QNB as radioligand from rat heart tissue
5
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor M1 (CHEMBL276)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Resolution and in vitro and initial in vivo evaluation of isomers of iodine-125-labeled 1-azabicyclo[2.2.2]oct-3-yl alpha-hydroxy-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate: a high-affinity ligand for the muscarinic receptor.
McPherson DW, Lambert CR, Jahn K, Sood V, McRee RC, Zeeberg B, Reba RC, Knapp FF.
J Med Chem (1995) 38 : 3908 -3917
PubMed 7562924 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 9.32 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2111842 2 9.89
CHEMBL558910 1 9.49
CHEMBL127587 2 9.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2111842 Kd = 0.13 nM 9.89
CHEMBL2111842 Kd = 0.23 nM 9.64
CHEMBL558910 Kd = 0.32 nM 9.49
CHEMBL127587 Kd = 0.383 nM 9.42
CHEMBL127587 Kd = 6.83 nM 8.17