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Assay Detail

CHEMBL3293104

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

Binding
Displacement of [3H]NMS from human M2R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
6
Total Activities
3
Compounds Tested
2
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 M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological comparison of enantiomers of mepenzolate bromide, a muscarinic receptor antagonist with bronchodilatory and anti-inflammatory activities.
Yamashita Y, Tanaka K, Asano T, Yamakawa N, Kobayashi D, Ishihara T, Hanaya K, Shoji M, Sugai T, Wada M, Mashimo T, Fukunishi Y, Mizushima T.
Bioorg Med Chem (2014) 22 : 3488 -3497
PubMed 24844758 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 9.04 9.35
Inhibition 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3289390 2 9.35
CHEMBL1724 MEPENZOLATE BROMIDE 4.0 2 9.17
CHEMBL3289391 2 8.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3289390 Ki = 0.45 nM 9.35
CHEMBL1724 MEPENZOLATE BROMIDE Ki = 0.68 nM 9.17
CHEMBL3289391 Ki = 2.52 nM 8.60
CHEMBL3289390 Inhibition - % -
CHEMBL3289391 Inhibition - % -
CHEMBL1724 MEPENZOLATE BROMIDE Inhibition - % -