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Assay Detail

CHEMBL747406

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

Binding
Inhibition of [3H]oxotremorine-M binding to rat brain membrane Muscarinic acetylcholine receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres.
Sauerberg P, Falch E, Meier E, Lembøl HL, Krogsgaard-Larsen P.
J Med Chem (1988) 31 : 1312 -1316
PubMed 3385727 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.74 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL540136 SULFOARECOLINE IODIDE 1 8.85
CHEMBL7303 ARECOLINE -1.0 1 8.72
CHEMBL284208 1 8.48
CHEMBL541666 1 8.04
CHEMBL278618 1 7.72
CHEMBL27384 1 7.55
CHEMBL28033 1 7.41
CHEMBL25649 1 7.37
CHEMBL285803 1 6.66
CHEMBL26932 1 6.64
CHEMBL283834 1 -
CHEMBL418022 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL540136 SULFOARECOLINE IODIDE IC50 = 1.4 nM 8.85
CHEMBL7303 ARECOLINE IC50 = 1.9 nM 8.72
CHEMBL284208 IC50 = 3.3 nM 8.48
CHEMBL541666 IC50 = 9.2 nM 8.04
CHEMBL278618 IC50 = 19.0 nM 7.72
CHEMBL27384 IC50 = 28.0 nM 7.55
CHEMBL28033 IC50 = 39.0 nM 7.41
CHEMBL25649 IC50 = 43.0 nM 7.37
CHEMBL285803 IC50 = 220.0 nM 6.66
CHEMBL26932 IC50 = 230.0 nM 6.64
CHEMBL283834 IC50 > 1000000.0 nM -
CHEMBL418022 IC50 > 1000000.0 nM -