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Assay Detail

CHEMBL1010734

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

Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
12
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol.
Kern C, Meyer T, Droux S, Schollmeyer D, Miculka C.
J Med Chem (2009) 52 : 1773 -1777
PubMed 19245211 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.51 8.52
Ki 6 6.84 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL513389 ZENIDOLOL 2.0 2 9.00
CHEMBL509336 RACTOPAMINE 2.0 2 6.75
CHEMBL462313 2 6.50
CHEMBL714 ALBUTEROL 4.0 2 6.29
CHEMBL2218907 ZILPATEROL 2.0 2 6.24
CHEMBL49080 CLENBUTEROL 2.0 2 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL513389 ZENIDOLOL Ki = 1.0 nM 9.00
CHEMBL513389 ZENIDOLOL IC50 = 3.0 nM 8.52
CHEMBL509336 RACTOPAMINE Ki = 180.0 nM 6.75
CHEMBL462313 Ki = 320.0 nM 6.50
CHEMBL509336 RACTOPAMINE IC50 = 330.0 nM 6.48
CHEMBL714 ALBUTEROL Ki = 510.0 nM 6.29
CHEMBL2218907 ZILPATEROL Ki = 580.0 nM 6.24
CHEMBL49080 CLENBUTEROL Ki = 570.0 nM 6.24
CHEMBL462313 IC50 = 620.0 nM 6.21
CHEMBL714 ALBUTEROL IC50 = 980.0 nM 6.01
CHEMBL2218907 ZILPATEROL IC50 = 1100.0 nM 5.96
CHEMBL49080 CLENBUTEROL IC50 = 1300.0 nM 5.89