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Assay Detail

CHEMBL900403

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

Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
18
Total Activities
18
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 Intermediate

Target

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

Publication

The discovery of indole-derived long acting beta2-adrenoceptor agonists for the treatment of asthma and COPD.
Brown AD, Bunnage ME, Glossop PA, Holbrook M, Jones RD, Lane CA, Lewthwaite RA, Mantell S, Perros-Huguet C, Price DA, Webster R.
Bioorg Med Chem Lett (2007) 17 : 6188 -6191
PubMed 17897826 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 10.00 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL236039 1 10.70
CHEMBL236041 1 10.66
CHEMBL430361 1 10.51
CHEMBL391006 1 10.42
CHEMBL236040 1 10.42
CHEMBL391946 1 10.31
CHEMBL236251 1 10.29
CHEMBL235612 1 10.28
CHEMBL237501 1 10.24
CHEMBL392056 1 10.24
CHEMBL1263 SALMETEROL 4.0 1 10.15
CHEMBL235818 1 9.91
CHEMBL394339 1 9.79
CHEMBL236042 1 9.60
CHEMBL391308 1 9.59
CHEMBL238347 1 9.16
CHEMBL428027 1 9.15
CHEMBL237709 1 8.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL236039 EC50 = 0.02 nM 10.70
CHEMBL236041 EC50 = 0.022 nM 10.66
CHEMBL430361 EC50 = 0.031 nM 10.51
CHEMBL391006 EC50 = 0.038 nM 10.42
CHEMBL236040 EC50 = 0.038 nM 10.42
CHEMBL391946 EC50 = 0.049 nM 10.31
CHEMBL236251 EC50 = 0.051 nM 10.29
CHEMBL235612 EC50 = 0.053 nM 10.28
CHEMBL237501 EC50 = 0.058 nM 10.24
CHEMBL392056 EC50 = 0.058 nM 10.24
CHEMBL1263 SALMETEROL EC50 = 0.07 nM 10.15
CHEMBL235818 EC50 = 0.122 nM 9.91
CHEMBL394339 EC50 = 0.164 nM 9.79
CHEMBL236042 EC50 = 0.254 nM 9.60
CHEMBL391308 EC50 = 0.258 nM 9.59
CHEMBL238347 EC50 = 0.687 nM 9.16
CHEMBL428027 EC50 = 0.706 nM 9.15
CHEMBL237709 EC50 = 2.55 nM 8.59