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Assay Detail

CHEMBL1291430

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

Binding
Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

The discovery of new spirocyclic muscarinic M3 antagonists.
Stocks MJ, Alcaraz L, Bailey A, Bowers K, Donald D, Edwards H, Hunt F, Kindon N, Pairaudeau G, Theaker J, Warner DJ.
Bioorg Med Chem Lett (2010) 20 : 7458 -7461
PubMed 21036043 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 10.13 10.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545181 TIOTROPIUM BROMIDE 4.0 1 10.50
CHEMBL551466 ACLIDINIUM BROMIDE 4.0 1 10.00
CHEMBL1201027 GLYCOPYRRONIUM BROMIDE 4.0 1 9.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545181 TIOTROPIUM BROMIDE IC50 = 0.03162 nM 10.50
CHEMBL551466 ACLIDINIUM BROMIDE IC50 = 0.1 nM 10.00
CHEMBL1201027 GLYCOPYRRONIUM BROMIDE IC50 = 0.1259 nM 9.90