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Assay Detail

CHEMBL3292795

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Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.
Jacobsen JR, Aggen JB, Church TJ, Klein U, Pfeiffer JW, Pulido-Rios TM, Thomas GR, Yu C, Moran EJ.
Bioorg Med Chem Lett (2014) 24 : 2625 -2630
PubMed 24813741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 8.96 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3290999 1 9.40
CHEMBL1263 SALMETEROL 4.0 1 9.30
CHEMBL3290998 1 9.10
CHEMBL1256786 FORMOTEROL 4.0 1 8.60
CHEMBL3290997 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3290999 EC50 = 0.3981 nM 9.40
CHEMBL1263 SALMETEROL EC50 = 0.5012 nM 9.30
CHEMBL3290998 EC50 = 0.7943 nM 9.10
CHEMBL1256786 FORMOTEROL EC50 = 2.512 nM 8.60
CHEMBL3290997 EC50 = 3.981 nM 8.40