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Assay Detail

CHEMBL895077

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

Binding
Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed in CHO cells
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 Expert

Target

Alpha-2A adrenergic receptor (CHEMBL1867)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Alpha2-adrenoreceptors profile modulation. 3.1 (R)-(+)-m-nitrobiphenyline, a new efficient and alpha2C-subtype selective agonist.
Crassous PA, Cardinaletti C, Carrieri A, Bruni B, Di Vaira M, Gentili F, Ghelfi F, Giannella M, Paris H, Piergentili A, Quaglia W, Schaak S, Vesprini C, Pigini M.
J Med Chem (2007) 50 : 3964 -3968
PubMed 17630725 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.20 7.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223836 1 7.83
CHEMBL374584 1 7.56
CHEMBL128168 BIPHENYLINE 1 7.32
CHEMBL222928 1 7.22
CHEMBL397753 1 7.14
CHEMBL242693 1 7.09
CHEMBL396013 1 7.04
CHEMBL373535 1 6.86
CHEMBL242265 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223836 Ki = 14.79 nM 7.83
CHEMBL374584 Ki = 27.54 nM 7.56
CHEMBL128168 BIPHENYLINE Ki = 47.86 nM 7.32
CHEMBL222928 Ki = 60.26 nM 7.22
CHEMBL397753 Ki = 72.44 nM 7.14
CHEMBL242693 Ki = 81.28 nM 7.09
CHEMBL396013 Ki = 91.2 nM 7.04
CHEMBL373535 Ki = 138.04 nM 6.86
CHEMBL242265 Ki = 186.21 nM 6.73