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Assay Detail

CHEMBL1044606

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Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Studies towards topical selective beta2-adrenoceptor agonists with a long duration of action.
Bouyssou T, Rudolf K, Hoenke C, Lustenberger P, Schnapp A, Konetzki I.
Bioorg Med Chem Lett (2009) 19 : 5237 -5240
PubMed 19643607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 8.76 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1256786 FORMOTEROL 4.0 1 9.40
CHEMBL576428 1 9.30
CHEMBL568239 1 9.05
CHEMBL587197 1 9.00
CHEMBL577917 1 9.00
CHEMBL577702 1 8.96
CHEMBL583235 1 8.92
CHEMBL570834 1 8.92
CHEMBL585751 1 8.74
CHEMBL565770 1 8.39
CHEMBL565747 1 8.27
CHEMBL568667 1 8.05
CHEMBL585382 1 7.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1256786 FORMOTEROL EC50 = 0.4 nM 9.40
CHEMBL576428 EC50 = 0.5 nM 9.30
CHEMBL568239 EC50 = 0.9 nM 9.05
CHEMBL587197 EC50 = 1.0 nM 9.00
CHEMBL577917 EC50 = 1.0 nM 9.00
CHEMBL577702 EC50 = 1.1 nM 8.96
CHEMBL583235 EC50 = 1.2 nM 8.92
CHEMBL570834 EC50 = 1.2 nM 8.92
CHEMBL585751 EC50 = 1.8 nM 8.74
CHEMBL565770 EC50 = 4.1 nM 8.39
CHEMBL565747 EC50 = 5.4 nM 8.27
CHEMBL568667 EC50 = 9.0 nM 8.05
CHEMBL585382 EC50 = 11.6 nM 7.94