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Assay Detail

CHEMBL3100636

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

Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Comparative molecular field analysis of fenoterol derivatives interacting with an agonist-stabilized form of the β₂-adrenergic receptor.
Plazinska A, Pajak K, Rutkowska E, Jimenez L, Kozocas J, Koolpe G, Tanga M, Toll L, Wainer IW, Jozwiak K.
Bioorg Med Chem (2014) 22 : 234 -246
PubMed 24326276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 7.26 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434 ISOPROTERENOL 4.0 1 9.70
CHEMBL228992 1 9.52
CHEMBL3099659 1 8.79
CHEMBL228996 1 8.70
CHEMBL228998 1 8.14
CHEMBL3099657 1 7.99
CHEMBL228417 1 7.48
CHEMBL3099658 1 6.68
CHEMBL3099663 1 6.33
CHEMBL3099660 1 6.00
CHEMBL3099664 1 5.21
CHEMBL3099662 1 5.21
CHEMBL3099661 1 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434 ISOPROTERENOL EC50 = 0.2 nM 9.70
CHEMBL228992 EC50 = 0.3 nM 9.52
CHEMBL3099659 EC50 = 1.63 nM 8.79
CHEMBL228996 EC50 = 2.0 nM 8.70
CHEMBL228998 EC50 = 7.2 nM 8.14
CHEMBL3099657 EC50 = 10.19 nM 7.99
CHEMBL228417 EC50 = 33.2 nM 7.48
CHEMBL3099658 EC50 = 210.0 nM 6.68
CHEMBL3099663 EC50 = 462.0 nM 6.33
CHEMBL3099660 EC50 = 1010.0 nM 6.00
CHEMBL3099664 EC50 = 6100.0 nM 5.21
CHEMBL3099662 EC50 = 6100.0 nM 5.21
CHEMBL3099661 EC50 = 26200.0 nM 4.58