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Assay Detail

CHEMBL1838343

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

Binding
Displacement of [3H]N-methylscopolamine from human M3 receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor M3 (CHEMBL245)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Efficient conversion of a nonselective norepinephrin reuptake inhibitor into a dual muscarinic antagonist-β₂-agonist for the treatment of chronic obstructive pulmonary disease.
Osborne R, Clarke N, Glossop P, Kenyon A, Liu H, Patel S, Summerhill S, Jones LH.
J Med Chem (2011) 54 : 6998 -7002
PubMed 21863888 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.20 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1836647 1 8.66
CHEMBL1836646 1 8.60
CHEMBL1382 TOLTERODINE 4.0 1 8.44
CHEMBL1836645 1 8.00
CHEMBL1836644 1 7.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1836647 Ki = 2.2 nM 8.66
CHEMBL1836646 Ki = 2.5 nM 8.60
CHEMBL1382 TOLTERODINE Ki = 3.6 nM 8.44
CHEMBL1836645 Ki = 10.0 nM 8.00
CHEMBL1836644 Ki = 49.0 nM 7.31