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Assay Detail

CHEMBL647973

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

Binding
Alpha-2 adrenergic receptor binding affinity was tested against membrane preparations of rat brain using 0.2 nM [3H]rauwolscine as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
Zhang X, Yao XT, Dalton JT, Shams G, Lei L, Patil PN, Feller DR, Hsu FL, George C, Miller DD.
J Med Chem (1996) 39 : 3001 -3013
PubMed 8709134 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.77 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL306751 1 7.89
CHEMBL105328 1 7.48
CHEMBL105487 1 6.91
CHEMBL102076 1 6.78
CHEMBL102669 1 5.83
CHEMBL322844 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL306751 Ki = 13.0 nM 7.89
CHEMBL105328 Ki = 33.0 nM 7.48
CHEMBL105487 Ki = 122.0 nM 6.91
CHEMBL102076 Ki = 165.0 nM 6.78
CHEMBL102669 Ki = 1474.0 nM 5.83
CHEMBL322844 Ki = 1890.0 nM 5.72