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Assay Detail

CHEMBL5525959

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

Binding
Displacement of [3H]-DHA from beta-2 AR (unknown origin) overexpressed in HEK293 cell membrane assessed as dissociation constant (K) incubated for 90 mins by liquid scintillation analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Bitopic Ligands Support the Presence of a Metastable Binding Site at the β<sub>2</sub> Adrenergic Receptor.
Gaiser BI, Danielsen M, Xu X, Røpke Jørgensen K, Fronik P, Märcher-Rørsted E, Wróbel TM, Liu X, Mosolff Mathiesen J, Sejer Pedersen D.
J Med Chem (2024) 67 : 11053 -11068
PubMed 38952152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 8.19 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5564549 1 9.37
CHEMBL1160734 1 9.30
CHEMBL5557954 1 9.10
CHEMBL5562658 1 8.95
CHEMBL5568144 1 8.58
CHEMBL5561419 1 7.91
CHEMBL5562644 1 6.23
CHEMBL5561967 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5564549 Kd = 0.4266 nM 9.37
CHEMBL1160734 Kd = 0.5012 nM 9.30
CHEMBL5557954 Kd = 0.7943 nM 9.10
CHEMBL5562658 Kd = 1.122 nM 8.95
CHEMBL5568144 Kd = 2.63 nM 8.58
CHEMBL5561419 Kd = 12.3 nM 7.91
CHEMBL5562644 Kd = 588.84 nM 6.23
CHEMBL5561967 Kd = 831.76 nM 6.08