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Assay Detail

CHEMBL746417

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

Binding
Inhibition of [3H]pirenzepine binding to mouse muscarinic acetylcholine receptor M1 from cerebral cortex
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Cerebral cortex
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M1 (CHEMBL3733)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.
Valli MJ, Tang Y, Kosh JW, Chapman JM, Sowell JW.
J Med Chem (1992) 35 : 3141 -3147
PubMed 1507203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.74 6.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL107673 1 6.42
CHEMBL320291 1 6.37
CHEMBL318517 1 6.28
CHEMBL106348 1 6.17
CHEMBL106344 1 5.82
CHEMBL104681 1 5.75
CHEMBL106936 1 5.70
CHEMBL107254 1 5.68
CHEMBL106932 1 5.51
CHEMBL106782 1 5.50
CHEMBL106082 1 5.48
CHEMBL107892 1 5.42
CHEMBL321605 1 5.42
CHEMBL104355 1 5.40
CHEMBL108163 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL107673 IC50 = 380.0 nM 6.42
CHEMBL320291 IC50 = 430.0 nM 6.37
CHEMBL318517 IC50 = 530.0 nM 6.28
CHEMBL106348 IC50 = 670.0 nM 6.17
CHEMBL106344 IC50 = 1500.0 nM 5.82
CHEMBL104681 IC50 = 1800.0 nM 5.75
CHEMBL106936 IC50 = 2000.0 nM 5.70
CHEMBL107254 IC50 = 2100.0 nM 5.68
CHEMBL106932 IC50 = 3100.0 nM 5.51
CHEMBL106782 IC50 = 3200.0 nM 5.50
CHEMBL106082 IC50 = 3300.0 nM 5.48
CHEMBL107892 IC50 = 3800.0 nM 5.42
CHEMBL321605 IC50 = 3800.0 nM 5.42
CHEMBL104355 IC50 = 4000.0 nM 5.40
CHEMBL108163 IC50 = 6400.0 nM 5.19