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Assay Detail

CHEMBL1943768

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Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A multivalent approach to the discovery of long-acting β(2)-adrenoceptor agonists for the treatment of asthma and COPD.
Jacobsen JR, Choi SK, Combs J, Fournier EJ, Klein U, Pfeiffer JW, Thomas GR, Yu C, Moran EJ.
Bioorg Med Chem Lett (2012) 22 : 1213 -1218
PubMed 22178551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 8.66 10.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1940832 MILVETEROL 2.0 1 10.20
CHEMBL1940830 1 10.00
CHEMBL1940833 1 9.90
CHEMBL1940815 1 9.50
CHEMBL1940817 1 9.50
CHEMBL1263 SALMETEROL 4.0 1 9.50
CHEMBL1940831 1 9.50
CHEMBL1940834 1 9.40
CHEMBL1940816 1 9.40
CHEMBL1940820 1 8.80
CHEMBL1940821 1 8.70
CHEMBL1940818 1 8.70
CHEMBL1940825 1 8.60
CHEMBL1940819 1 8.30
CHEMBL1940823 1 8.20
CHEMBL1940824 1 8.10
CHEMBL714 ALBUTEROL 4.0 1 7.60
CHEMBL1940828 1 7.40
CHEMBL1940822 1 7.40
CHEMBL1940829 1 7.30
CHEMBL1940826 1 7.30
CHEMBL1940827 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1940832 MILVETEROL EC50 = 0.0631 nM 10.20
CHEMBL1940830 EC50 = 0.1 nM 10.00
CHEMBL1940833 EC50 = 0.1259 nM 9.90
CHEMBL1940815 EC50 = 0.3162 nM 9.50
CHEMBL1940817 EC50 = 0.3162 nM 9.50
CHEMBL1263 SALMETEROL EC50 = 0.3162 nM 9.50
CHEMBL1940831 EC50 = 0.3162 nM 9.50
CHEMBL1940834 EC50 = 0.3981 nM 9.40
CHEMBL1940816 EC50 = 0.3981 nM 9.40
CHEMBL1940820 EC50 = 1.585 nM 8.80
CHEMBL1940821 EC50 = 1.995 nM 8.70
CHEMBL1940818 EC50 = 1.995 nM 8.70
CHEMBL1940825 EC50 = 2.512 nM 8.60
CHEMBL1940819 EC50 = 5.012 nM 8.30
CHEMBL1940823 EC50 = 6.31 nM 8.20
CHEMBL1940824 EC50 = 7.943 nM 8.10
CHEMBL714 ALBUTEROL EC50 = 25.12 nM 7.60
CHEMBL1940828 EC50 = 39.81 nM 7.40
CHEMBL1940822 EC50 = 39.81 nM 7.40
CHEMBL1940829 EC50 = 50.12 nM 7.30
CHEMBL1940826 EC50 = 50.12 nM 7.30
CHEMBL1940827 EC50 = 63.1 nM 7.20