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Assay Detail

CHEMBL1071508

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

Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
21
Total Activities
21
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

Discovery of olodaterol, a novel inhaled beta2-adrenoceptor agonist with a 24 h bronchodilatory efficacy.
Bouyssou T, Hoenke C, Rudolf K, Lustenberger P, Pestel S, Sieger P, Lotz R, Heine C, Büttner FH, Schnapp A, Konetzki I.
Bioorg Med Chem Lett (2010) 20 : 1410 -1414
PubMed 20096576 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 8.05 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2133469 FORMOTEROL FUMARATE HYDRATE 1 9.40
CHEMBL601036 1 9.15
CHEMBL603274 1 8.89
CHEMBL603271 1 8.85
CHEMBL600617 1 8.85
CHEMBL592879 1 8.62
CHEMBL566973 1 8.54
CHEMBL604333 1 8.47
CHEMBL600401 1 8.47
CHEMBL602257 1 8.39
CHEMBL600616 1 7.97
CHEMBL600400 1 7.92
CHEMBL601429 1 7.92
CHEMBL601430 1 7.91
CHEMBL604125 1 7.84
CHEMBL600007 1 7.81
CHEMBL602258 1 7.30
CHEMBL605372 1 7.24
CHEMBL601858 1 7.17
CHEMBL600817 1 7.01
CHEMBL606208 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2133469 FORMOTEROL FUMARATE HYDRATE EC50 = 0.4 nM 9.40
CHEMBL601036 EC50 = 0.7 nM 9.15
CHEMBL603274 EC50 = 1.3 nM 8.89
CHEMBL603271 EC50 = 1.4 nM 8.85
CHEMBL600617 EC50 = 1.4 nM 8.85
CHEMBL592879 EC50 = 2.4 nM 8.62
CHEMBL566973 EC50 = 2.9 nM 8.54
CHEMBL604333 EC50 = 3.4 nM 8.47
CHEMBL600401 EC50 = 3.4 nM 8.47
CHEMBL602257 EC50 = 4.1 nM 8.39
CHEMBL600616 EC50 = 10.7 nM 7.97
CHEMBL600400 EC50 = 11.9 nM 7.92
CHEMBL601429 EC50 = 12.1 nM 7.92
CHEMBL601430 EC50 = 12.4 nM 7.91
CHEMBL604125 EC50 = 14.3 nM 7.84
CHEMBL600007 EC50 = 15.4 nM 7.81
CHEMBL602258 EC50 = 49.7 nM 7.30
CHEMBL605372 EC50 = 58.0 nM 7.24
CHEMBL601858 EC50 = 68.0 nM 7.17
CHEMBL600817 EC50 = 97.7 nM 7.01
CHEMBL606208 EC50 = 5167.0 nM 5.29