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Assay Detail

CHEMBL1937030

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

Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
12
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Cell-based and in-silico studies on the high intrinsic activity of two boron-containing salbutamol derivatives at the human β₂-adrenoceptor.
Soriano-Ursúa MA, McNaught-Flores DA, Nieto-Alamilla G, Segura-Cabrera A, Correa-Basurto J, Arias-Montaño JA, Trujillo-Ferrara JG.
Bioorg Med Chem (2012) 20 : 933 -941
PubMed 22182578 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.54 6.30
Inhibition 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1711 ISOPROTERENOL HYDROCHLORIDE 4.0 3 6.30
CHEMBL2068576 3 5.41
CHEMBL1002 LEVOSALBUTAMOL 4.0 3 5.25
CHEMBL2068577 3 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1711 ISOPROTERENOL HYDROCHLORIDE Ki = 501.0 nM 6.30
CHEMBL1711 ISOPROTERENOL HYDROCHLORIDE Ki = 501.19 nM 6.30
CHEMBL2068576 Ki = 3890.0 nM 5.41
CHEMBL2068576 Ki = 3890.45 nM 5.41
CHEMBL1002 LEVOSALBUTAMOL Ki = 5623.0 nM 5.25
CHEMBL1002 LEVOSALBUTAMOL Ki = 5623.41 nM 5.25
CHEMBL2068577 Ki = 6607.0 nM 5.18
CHEMBL2068577 Ki = 6606.93 nM 5.18
CHEMBL1711 ISOPROTERENOL HYDROCHLORIDE Inhibition - % -
CHEMBL2068577 Inhibition - % -
CHEMBL2068576 Inhibition - % -
CHEMBL1002 LEVOSALBUTAMOL Inhibition - % -