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Assay Detail

CHEMBL3429938

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

Functional
Bronchoprotection in male Duncan Hartley guinea pig bronchoconstriction einthoven model assessed as inhibition of methacholine-induced bronchoconstriction treated inhalation after 24 hrs by in vivo muscarinic antagonist and beta2 agonist activity assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 1 — Organism
Curated By Autocuration

Target

Cavia porcellus (CHEMBL369)
Type ORGANISM
Organism Cavia porcellus

Publication

Discovery of (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate (TD-5959, GSK961081, batefenterol): first-in-class dual pharmacology multivalent muscarinic antagonist and β₂ agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD).
Hughes AD, Chen Y, Hegde SS, Jasper JR, Jaw-Tsai S, Lee TW, McNamara A, Pulido-Rios MT, Steinfeld T, Mammen M.
J Med Chem (2015) 58 : 2609 -2622
PubMed 25629394 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 8.00 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3039518 BATEFENTEROL 2.0 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3039518 BATEFENTEROL EC50 = 10.0 nM 8.00