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Assay Detail

CHEMBL973678

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

Binding
Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
Zhao C, Sun M, Bennani YL, Gopalakrishnan SM, Witte DG, Miller TR, Krueger KM, Browman KE, Thiffault C, Wetter J, Marsh KC, Hancock AA, Esbenshade TA, Cowart MD.
J Med Chem (2008) 51 : 5423 -5430
PubMed 18683917 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.82 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14638 CIPROXIFAN 1 7.37
CHEMBL260374 THIOPERAMIDE 1 6.90
CHEMBL191703 CONESSINE 2.0 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14638 CIPROXIFAN Ki = 42.66 nM 7.37
CHEMBL260374 THIOPERAMIDE Ki = 125.89 nM 6.90
CHEMBL191703 CONESSINE Ki = 660.69 nM 6.18