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Assay Detail

CHEMBL1804511

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Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
14
Total Activities
14
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: 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 14 8.53 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388570 1 9.52
CHEMBL228992 1 9.52
CHEMBL1800961 1 9.40
CHEMBL228996 1 8.70
CHEMBL229614 1 8.57
CHEMBL1800936 1 8.55
CHEMBL1800963 1 8.41
CHEMBL1800934 1 8.40
CHEMBL229476 1 8.33
CHEMBL228998 1 8.14
CHEMBL1800962 1 8.12
CHEMBL229477 1 8.07
CHEMBL229401 1 7.90
CHEMBL1800960 1 7.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388570 EC50 = 0.3 nM 9.52
CHEMBL228992 EC50 = 0.3 nM 9.52
CHEMBL1800961 EC50 = 0.4 nM 9.40
CHEMBL228996 EC50 = 2.0 nM 8.70
CHEMBL229614 EC50 = 2.7 nM 8.57
CHEMBL1800936 EC50 = 2.8 nM 8.55
CHEMBL1800963 EC50 = 3.9 nM 8.41
CHEMBL1800934 EC50 = 4.0 nM 8.40
CHEMBL229476 EC50 = 4.7 nM 8.33
CHEMBL228998 EC50 = 7.2 nM 8.14
CHEMBL1800962 EC50 = 7.6 nM 8.12
CHEMBL229477 EC50 = 8.5 nM 8.07
CHEMBL229401 EC50 = 12.5 nM 7.90
CHEMBL1800960 EC50 = 16.6 nM 7.78