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Assay Detail

CHEMBL1019681

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Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
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 Autocuration

Target

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

Publication

Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
Procopiou PA, Barrett VJ, Bevan NJ, Biggadike K, Butchers PR, Coe DM, Conroy R, Edney DD, Field RN, Ford AJ, Guntrip SB, Looker BE, McLay IM, Monteith MJ, Morrison VS, Mutch PJ, Richards SA, Sasse R, Smith CE.
J Med Chem (2009) 52 : 2280 -2288
PubMed 19317397 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 8.75 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL443435 1 9.80
CHEMBL446840 1 9.80
CHEMBL500782 1 9.70
CHEMBL1263 SALMETEROL 4.0 1 9.60
CHEMBL475389 1 9.30
CHEMBL514032 1 9.30
CHEMBL1256786 FORMOTEROL 4.0 1 9.30
CHEMBL516056 1 9.20
CHEMBL520313 1 9.10
CHEMBL474393 1 9.00
CHEMBL506518 1 9.00
CHEMBL456485 1 8.90
CHEMBL475237 1 8.80
CHEMBL485847 1 8.60
CHEMBL483202 1 8.10
CHEMBL475236 1 8.00
CHEMBL434 ISOPROTERENOL 4.0 1 7.40
CHEMBL483407 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL443435 EC50 = 0.1585 nM 9.80
CHEMBL446840 EC50 = 0.1585 nM 9.80
CHEMBL500782 EC50 = 0.1995 nM 9.70
CHEMBL1263 SALMETEROL EC50 = 0.2512 nM 9.60
CHEMBL475389 EC50 = 0.5012 nM 9.30
CHEMBL514032 EC50 = 0.5012 nM 9.30
CHEMBL1256786 FORMOTEROL EC50 = 0.5012 nM 9.30
CHEMBL516056 EC50 = 0.631 nM 9.20
CHEMBL520313 EC50 = 0.7943 nM 9.10
CHEMBL474393 EC50 = 1.0 nM 9.00
CHEMBL506518 EC50 = 1.0 nM 9.00
CHEMBL456485 EC50 = 1.259 nM 8.90
CHEMBL475237 EC50 = 1.585 nM 8.80
CHEMBL485847 EC50 = 2.512 nM 8.60
CHEMBL483202 EC50 = 7.943 nM 8.10
CHEMBL475236 EC50 = 10.0 nM 8.00
CHEMBL434 ISOPROTERENOL EC50 = 39.81 nM 7.40
CHEMBL483407 EC50 = 25118.86 nM 4.60