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Assay Detail

CHEMBL1775317

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Functional
Agonist activity at muscarinic M3 receptor in guinea pig trachea assessed as bronchorelaxation activity in presence of propranolol
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Trachea
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M3 (CHEMBL5498)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Inhalation by design: dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD.
Jones LH, Baldock H, Bunnage ME, Burrows J, Clarke N, Coghlan M, Entwistle D, Fairman D, Feeder N, Fulton C, Hilton L, James K, Jones RM, Kenyon AS, Marshall S, Newman SD, Osborne R, Patel S, Selby MD, Stuart EF, Trevethick MA, Wright KN, Price DA.
Bioorg Med Chem Lett (2011) 21 : 2759 -2763
PubMed 21075627 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.34 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1773267 1 8.40
CHEMBL1773197 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1773267 EC50 = 4.0 nM 8.40
CHEMBL1773197 EC50 = 5.3 nM 8.28