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Assay Detail

CHEMBL744134

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

Binding
In vitro binding affinity to the Muscarinic acetylcholine receptor by displacing [3H]-QNB from the rat heart tissues
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Heart
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Muscarinic acetylcholine receptor (CHEMBL1907609)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.
Bräuner-Osborne H, Ebert B, Brann MR, Falch E, Krogsgaard-Larsen P.
J Med Chem (1995) 38 : 2188 -2195
PubMed 7783150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.62 7.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69306 1 7.09
CHEMBL7634 OXOTREMORINE 1 7.08
CHEMBL69305 1 6.85
CHEMBL304142 1 6.46
CHEMBL305264 1 6.44
CHEMBL7303 ARECOLINE -1.0 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69306 IC50 = 82.0 nM 7.09
CHEMBL7634 OXOTREMORINE IC50 = 84.0 nM 7.08
CHEMBL69305 IC50 = 140.0 nM 6.85
CHEMBL304142 IC50 = 350.0 nM 6.46
CHEMBL305264 IC50 = 360.0 nM 6.44
CHEMBL7303 ARECOLINE IC50 = 1700.0 nM 5.77