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Assay Detail

CHEMBL1047076

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Functional
Agonist activity at human alpha2B adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
7
Total Activities
7
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 Intermediate

Target

Alpha-2B adrenergic receptor (CHEMBL1942)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine?
Cardinaletti C, Mattioli L, Ghelfi F, Del Bello F, Giannella M, Bruzzone A, Paris H, Perfumi M, Piergentili A, Quaglia W, Pigini M.
J Med Chem (2009) 52 : 7319 -7322
PubMed 19886609 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 5.94 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL569933 1 7.21
CHEMBL570973 1 6.00
CHEMBL576623 1 6.00
CHEMBL13852 CIRAZOLINE 2.0 1 6.00
CHEMBL576819 1 5.60
CHEMBL576078 1 5.50
CHEMBL570863 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL569933 EC50 = 61.66 nM 7.21
CHEMBL570973 EC50 = 1000.0 nM 6.00
CHEMBL576623 EC50 = 1000.0 nM 6.00
CHEMBL13852 CIRAZOLINE EC50 = 1000.0 nM 6.00
CHEMBL576819 EC50 = 2511.89 nM 5.60
CHEMBL576078 EC50 = 3162.28 nM 5.50
CHEMBL570863 EC50 = 5011.87 nM 5.30