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Assay Detail

CHEMBL1047080

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

Binding
Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
8
Total Activities
8
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 Intermediate

Target

Alpha-2A adrenergic receptor (CHEMBL1867)
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
Ki 8 7.42 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL576623 1 7.64
CHEMBL570863 1 7.61
CHEMBL571314 1 7.57
CHEMBL576819 1 7.46
CHEMBL569933 1 7.31
CHEMBL576078 1 7.30
CHEMBL570973 1 7.24
CHEMBL13852 CIRAZOLINE 2.0 1 7.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL576623 Ki = 22.91 nM 7.64
CHEMBL570863 Ki = 24.55 nM 7.61
CHEMBL571314 Ki = 26.92 nM 7.57
CHEMBL576819 Ki = 34.67 nM 7.46
CHEMBL569933 Ki = 48.98 nM 7.31
CHEMBL576078 Ki = 50.12 nM 7.30
CHEMBL570973 Ki = 57.54 nM 7.24
CHEMBL13852 CIRAZOLINE Ki = 58.88 nM 7.23