Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3855949

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

Binding
Displacement of [3H]-RX 821002 from alpha2-AR in Sprague-Dawley rat brain membranes after 30 mins by liquid scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
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 9 7.12 7.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3904276 1 7.73
CHEMBL51358 1 7.59
CHEMBL3961335 1 6.79
CHEMBL3892351 1 6.75
CHEMBL337862 1 6.75
CHEMBL1439667 1 -
CHEMBL3920069 1 -
CHEMBL3939078 1 -
CHEMBL3911124 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3904276 Ki = 18.62 nM 7.73
CHEMBL51358 Ki = 25.7 nM 7.59
CHEMBL3961335 Ki = 162.18 nM 6.79
CHEMBL3892351 Ki = 177.83 nM 6.75
CHEMBL337862 Ki = 177.83 nM 6.75
CHEMBL1439667 Ki > 1000.0 nM -
CHEMBL3920069 Ki > 1000.0 nM -
CHEMBL3939078 Ki > 1000.0 nM -
CHEMBL3911124 Ki > 1000.0 nM -