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Assay Detail

CHEMBL1119458

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Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
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 metabolic inactivation: an antedrug approach.
Procopiou PA, Barrett VJ, Bevan NJ, Biggadike K, Box PC, Butchers PR, Coe DM, Conroy R, Emmons A, Ford AJ, Holmes DS, Horsley H, Kerr F, Li-Kwai-Cheung AM, Looker BE, Mann IS, McLay IM, Morrison VS, Mutch PJ, Smith CE, Tomlin P.
J Med Chem (2010) 53 : 4522 -4530
PubMed 20462258 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 8.82 9.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1085837 1 9.90
CHEMBL446840 1 9.80
CHEMBL1085399 1 9.60
CHEMBL1263 SALMETEROL 4.0 1 9.60
CHEMBL1084647 VILANTEROL ACETATE 1 9.40
CHEMBL1084648 1 9.40
CHEMBL1084891 1 9.40
CHEMBL605993 1 9.30
CHEMBL1086536 1 9.10
CHEMBL1085638 1 8.80
CHEMBL1084656 1 8.80
CHEMBL1084655 1 8.70
CHEMBL1084654 1 8.60
CHEMBL1084649 1 8.60
CHEMBL1085395 1 8.60
CHEMBL1086535 1 8.10
CHEMBL434 ISOPROTERENOL 4.0 1 7.40
CHEMBL1083884 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1085837 EC50 = 0.1259 nM 9.90
CHEMBL446840 EC50 = 0.1585 nM 9.80
CHEMBL1085399 EC50 = 0.2512 nM 9.60
CHEMBL1263 SALMETEROL EC50 = 0.2512 nM 9.60
CHEMBL1084647 VILANTEROL ACETATE EC50 = 0.3981 nM 9.40
CHEMBL1084648 EC50 = 0.3981 nM 9.40
CHEMBL1084891 EC50 = 0.3981 nM 9.40
CHEMBL605993 EC50 = 0.5012 nM 9.30
CHEMBL1086536 EC50 = 0.7943 nM 9.10
CHEMBL1085638 EC50 = 1.585 nM 8.80
CHEMBL1084656 EC50 = 1.585 nM 8.80
CHEMBL1084655 EC50 = 1.995 nM 8.70
CHEMBL1084654 EC50 = 2.512 nM 8.60
CHEMBL1084649 EC50 = 2.512 nM 8.60
CHEMBL1085395 EC50 = 2.512 nM 8.60
CHEMBL1086535 EC50 = 7.943 nM 8.10
CHEMBL434 ISOPROTERENOL EC50 = 39.81 nM 7.40
CHEMBL1083884 EC50 = 2511.89 nM 5.60