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Assay Detail

CHEMBL3855981

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

Binding
Displacement of [3H]-clonidine from alpha2-AR in rat brain cortical membranes after 45 mins by liquid scintillation counting
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

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
Ki 2 7.14 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13881 PHENAMAZOLINE 2.0 1 7.14
CHEMBL275970 TRACIZOLINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13881 PHENAMAZOLINE Ki = 72.44 nM 7.14
CHEMBL275970 TRACIZOLINE Ki > 1000.0 nM -