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Assay Detail

CHEMBL3855953

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

Binding
Agonist activity at human alpha2b-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Combined Interactions with I1-, I2-Imidazoline Binding Sites and α2-Adrenoceptors To Manage Opioid Addiction.
Giusepponi ME, Cifani C, Micioni Di Bonaventura MV, Mattioli L, Hudson A, Diamanti E, Del Bello F, Giannella M, Mammoli V, Paoletti CD, Piergentili A, Pigini M, Quaglia W.
ACS Med Chem Lett (2016) 7 : 956 -961
PubMed 27774136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 5.71 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51358 1 6.11
CHEMBL337862 1 6.02
CHEMBL3961335 1 5.60
CHEMBL3904276 1 5.50
CHEMBL3892351 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51358 EC50 = 776.25 nM 6.11
CHEMBL337862 EC50 = 954.99 nM 6.02
CHEMBL3961335 EC50 = 2511.89 nM 5.60
CHEMBL3904276 EC50 = 3162.28 nM 5.50
CHEMBL3892351 EC50 = 4570.88 nM 5.34