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Assay Detail

CHEMBL649641

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

Binding
In vitro binding affinity was measured as the inhibition of [3H]idazoxan to alpha-2 adrenergic receptors of rat cortical membranes
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.
Guérémy C, Audiau F, Renault C, Benavides J, Uzan A, Le Fur G.
J Med Chem (1986) 29 : 1394 -1398
PubMed 3016265 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.19 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29001 1 7.85
CHEMBL31548 1 7.01
CHEMBL28448 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29001 Ki = 14.0 nM 7.85
CHEMBL31548 Ki = 97.0 nM 7.01
CHEMBL28448 Ki = 200.0 nM 6.70