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Assay Detail

CHEMBL931446

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

Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M2 receptor expressed in CHO cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Alkyne-quinuclidine derivatives as potent and selective muscarinic antagonists for the treatment of COPD.
Starck JP, Provins L, Christophe B, Gillard M, Jadot S, Lo Brutto P, Quéré L, Talaga P, Guyaux M.
Bioorg Med Chem Lett (2008) 18 : 2675 -2678
PubMed 18359633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.22 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545181 TIOTROPIUM BROMIDE 4.0 1 9.50
CHEMBL381623 1 9.10
CHEMBL1908368 1 8.90
CHEMBL428962 1 8.80
CHEMBL409151 1 8.60
CHEMBL264676 1 8.50
CHEMBL258959 1 8.20
CHEMBL264414 1 7.70
CHEMBL371734 1 7.60
CHEMBL260228 1 7.50
CHEMBL410061 1 7.40
CHEMBL411514 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545181 TIOTROPIUM BROMIDE Ki = 0.3162 nM 9.50
CHEMBL381623 Ki = 0.7943 nM 9.10
CHEMBL1908368 Ki = 1.259 nM 8.90
CHEMBL428962 Ki = 1.585 nM 8.80
CHEMBL409151 Ki = 2.512 nM 8.60
CHEMBL264676 Ki = 3.162 nM 8.50
CHEMBL258959 Ki = 6.31 nM 8.20
CHEMBL264414 Ki = 19.95 nM 7.70
CHEMBL371734 Ki = 25.12 nM 7.60
CHEMBL260228 Ki = 31.62 nM 7.50
CHEMBL410061 Ki = 39.81 nM 7.40
CHEMBL411514 Ki = 158.49 nM 6.80