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Assay Detail

CHEMBL5737525

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

Binding
Binding Assay: ADRB2 IC50 from binding assay(nM), Determined using the Tag-lite Adrenoceptor Beta2 receptor ligand binding assay.
24
Total Activities
8
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

G protein-coupled receptor kinase 3 (CHEMBL1075166)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Adrenergic receptor modulating compounds and methods of using the same
(2021)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 10.11 10.72
kon 8 - -
k_off 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5954552 3 10.72
CHEMBL5946696 3 10.62
CHEMBL5782704 3 10.32
CHEMBL6021679 3 10.19
CHEMBL5748424 3 9.84
CHEMBL6028513 3 9.64
CHEMBL6053158 3 9.42
CHEMBL5956027 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5954552 IC50 = 0.019 nM 10.72
CHEMBL5946696 IC50 = 0.024 nM 10.62
CHEMBL5782704 IC50 = 0.048 nM 10.32
CHEMBL6021679 IC50 = 0.065 nM 10.19
CHEMBL5748424 IC50 = 0.144 nM 9.84
CHEMBL6028513 IC50 = 0.23 nM 9.64
CHEMBL6053158 IC50 = 0.38 nM 9.42
CHEMBL5956027 kon = - -
CHEMBL5956027 k_off = - s-1 -
CHEMBL5782704 kon = - -
CHEMBL5782704 k_off = - s-1 -
CHEMBL5954552 kon = - -
CHEMBL5954552 k_off = - s-1 -
CHEMBL6021679 kon = - -
CHEMBL6021679 k_off = - s-1 -
CHEMBL6028513 kon = - -
CHEMBL6028513 k_off = - s-1 -
CHEMBL5946696 kon = - -
CHEMBL5946696 k_off = - s-1 -
CHEMBL6053158 kon = - -
CHEMBL6053158 k_off = - s-1 -
CHEMBL5748424 kon = - -
CHEMBL5956027 IC50 = 0.009 nM -
CHEMBL5748424 k_off = - s-1 -