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Assay Detail

CHEMBL1804513

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Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-2 adrenergic receptor (CHEMBL3754)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Comparative molecular field analysis of fenoterol derivatives: A platform towards highly selective and effective beta(2)-adrenergic receptor agonists.
Jozwiak K, Woo AY, Tanga MJ, Toll L, Jimenez L, Kozocas JA, Plazinska A, Xiao RP, Wainer IW.
Bioorg Med Chem (2010) 18 : 728 -736
PubMed 20036561 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 6.71 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1800963 1 7.80
CHEMBL229401 1 7.23
CHEMBL388570 1 7.14
CHEMBL229614 1 6.99
CHEMBL1800961 1 6.88
CHEMBL228992 1 6.73
CHEMBL228996 1 6.30
CHEMBL229476 1 6.24
CHEMBL1800936 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1800963 EC50 = 16.0 nM 7.80
CHEMBL229401 EC50 = 59.0 nM 7.23
CHEMBL388570 EC50 = 73.0 nM 7.14
CHEMBL229614 EC50 = 103.0 nM 6.99
CHEMBL1800961 EC50 = 133.0 nM 6.88
CHEMBL228992 EC50 = 186.0 nM 6.73
CHEMBL228996 EC50 = 506.0 nM 6.30
CHEMBL229476 EC50 = 575.0 nM 6.24
CHEMBL1800936 EC50 = 8551.0 nM 5.07