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Assay Detail

CHEMBL744059

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

Binding
Compound was evaluated for displacement of [3H]QNB from human Muscarinic m1 receptor in CHO cells.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor M1 (CHEMBL216)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The N4 nitrogen of pirenzepine is responsible for selective binding of the M1 subtype human muscarinic receptor
Murgolo NJ, Kozlowski J, Tice MA, Hollinger FP, Brown JE, Zhou G, Taylor LA, McQuade RD
Bioorg Med Chem Lett (1996) 6 : 785 -788
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.52 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9967 PIRENZEPINE 2.0 1 8.34
CHEMBL279453 1 7.91
CHEMBL611476 1 7.08
CHEMBL17045 OTENZEPAD 2.0 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9967 PIRENZEPINE Ki = 4.6 nM 8.34
CHEMBL279453 Ki = 12.4 nM 7.91
CHEMBL611476 Ki = 82.4 nM 7.08
CHEMBL17045 OTENZEPAD Ki = 179.0 nM 6.75