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

CHEMBL1959312

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

Binding
Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
9
Total Activities
9
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-2A adrenergic receptor (CHEMBL1867)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Favourable involvement of α2A-adrenoreceptor antagonism in the I₂-imidazoline binding sites-mediated morphine analgesia enhancement.
Mammoli V, Bonifazi A, Del Bello F, Diamanti E, Giannella M, Hudson AL, Mattioli L, Perfumi M, Piergentili A, Quaglia W, Titomanlio F, Pigini M.
Bioorg Med Chem (2012) 20 : 2259 -2265
PubMed 22370341 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.98 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10316 IDAZOXAN 3.0 1 8.15
CHEMBL1956902 1 6.40
CHEMBL1956900 1 6.30
CHEMBL1956906 1 5.42
CHEMBL1956903 1 5.27
CHEMBL1956904 1 5.20
CHEMBL1956901 1 5.10
CHEMBL1956899 1 -
CHEMBL1956905 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10316 IDAZOXAN Ki = 7.079 nM 8.15
CHEMBL1956902 Ki = 398.11 nM 6.40
CHEMBL1956900 Ki = 501.19 nM 6.30
CHEMBL1956906 Ki = 3801.89 nM 5.42
CHEMBL1956903 Ki = 5370.32 nM 5.27
CHEMBL1956904 Ki = 6309.57 nM 5.20
CHEMBL1956901 Ki = 7943.28 nM 5.10
CHEMBL1956899 Ki > 10000.0 nM -
CHEMBL1956905 Ki > 10000.0 nM -