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Assay Detail

CHEMBL1840217

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

Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulation
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Beta-1 adrenergic receptor (CHEMBL213)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
Procopiou PA, Barrett VJ, Ford AJ, Looker BE, Lunniss GE, Needham D, Smith CE, Somers G.
Bioorg Med Chem (2011) 19 : 6026 -6032
PubMed 21925889 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.44 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1835857 1 8.10
CHEMBL1835855 1 8.10
CHEMBL434 ISOPROTERENOL 4.0 1 8.10
CHEMBL1835860 1 8.00
CHEMBL1835856 1 7.50
CHEMBL1835858 1 7.50
CHEMBL1835859 1 7.50
CHEMBL1835854 1 7.50
CHEMBL1835862 1 7.40
CHEMBL1200811 ARFORMOTEROL FUMARATE 1 7.40
CHEMBL1835861 1 7.30
CHEMBL1835853 1 7.20
CHEMBL1084647 VILANTEROL ACETATE 1 6.40
CHEMBL1263 SALMETEROL 4.0 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1835857 EC50 = 7.943 nM 8.10
CHEMBL1835855 EC50 = 7.943 nM 8.10
CHEMBL434 ISOPROTERENOL EC50 = 7.943 nM 8.10
CHEMBL1835860 EC50 = 10.0 nM 8.00
CHEMBL1835856 EC50 = 31.62 nM 7.50
CHEMBL1835858 EC50 = 31.62 nM 7.50
CHEMBL1835859 EC50 = 31.62 nM 7.50
CHEMBL1835854 EC50 = 31.62 nM 7.50
CHEMBL1835862 EC50 = 39.81 nM 7.40
CHEMBL1200811 ARFORMOTEROL FUMARATE EC50 = 39.81 nM 7.40
CHEMBL1835861 EC50 = 50.12 nM 7.30
CHEMBL1835853 EC50 = 63.1 nM 7.20
CHEMBL1084647 VILANTEROL ACETATE EC50 = 398.11 nM 6.40
CHEMBL1263 SALMETEROL EC50 = 794.33 nM 6.10