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Assay Detail

CHEMBL4397572

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

Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
Stanek M, Picard LP, Schmidt MF, Kaindl JM, Hübner H, Bouvier M, Weikert D, Gmeiner P.
J Med Chem (2019) 62 : 5111 -5131
PubMed 31042379 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.10 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1263 SALMETEROL 4.0 1 10.10
CHEMBL1160723 LEVISOPRENALINE 2.0 1 7.70
CHEMBL3797876 1 7.00
CHEMBL1160694 1 6.60
CHEMBL3800303 1 6.38
CHEMBL4435895 1 6.20
CHEMBL4593181 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1263 SALMETEROL EC50 = 0.07943 nM 10.10
CHEMBL1160723 LEVISOPRENALINE EC50 = 19.95 nM 7.70
CHEMBL3797876 EC50 = 100.0 nM 7.00
CHEMBL1160694 EC50 = 251.19 nM 6.60
CHEMBL3800303 EC50 = 416.87 nM 6.38
CHEMBL4435895 EC50 = 630.96 nM 6.20
CHEMBL4593181 EC50 = 1995.26 nM 5.70