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Assay Detail

CHEMBL1775311

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Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Beta-2 adrenergic receptor (CHEMBL210)
Type SINGLE PROTEIN
Organism Homo sapiens

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 11 7.82 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL230490 1 8.96
CHEMBL1773267 1 8.62
CHEMBL1773266 1 8.24
CHEMBL1773197 1 8.09
CHEMBL1773262 1 8.00
CHEMBL1773264 1 7.89
CHEMBL1773198 1 7.82
CHEMBL1773196 1 7.77
CHEMBL1773263 1 6.94
CHEMBL1773074 1 6.89
CHEMBL1773265 1 6.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL230490 EC50 = 1.1 nM 8.96
CHEMBL1773267 EC50 = 2.4 nM 8.62
CHEMBL1773266 EC50 = 5.7 nM 8.24
CHEMBL1773197 EC50 = 8.1 nM 8.09
CHEMBL1773262 EC50 = 10.0 nM 8.00
CHEMBL1773264 EC50 = 13.0 nM 7.89
CHEMBL1773198 EC50 = 15.0 nM 7.82
CHEMBL1773196 EC50 = 17.0 nM 7.77
CHEMBL1773263 EC50 = 116.0 nM 6.94
CHEMBL1773074 EC50 = 129.0 nM 6.89
CHEMBL1773265 EC50 = 173.0 nM 6.76