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Assay Detail

CHEMBL3861570

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

Binding
Displacement of [3H]clonidine from alpha2 adrenergic receptor in rat brain cerebral cortex after 25 mins by microbeta scintillation counting method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Synthesis and activity of newly designed aroxyalkyl or aroxyethoxyethyl derivatives of piperazine on the cardiovascular and the central nervous systems.
Waszkielewicz AM, Kubacka M, Pańczyk K, Mogilski S, Siwek A, Głuch-Lutwin M, Gryboś A, Filipek B.
Bioorg Med Chem Lett (2016) 26 : 5315 -5321
PubMed 27692547 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.66 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134 CLONIDINE 4.0 1 8.57
CHEMBL3949348 1 6.54
CHEMBL3958008 1 6.43
CHEMBL3979966 1 6.30
CHEMBL3921558 1 6.09
CHEMBL3971078 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134 CLONIDINE Ki = 2.7 nM 8.57
CHEMBL3949348 Ki = 289.0 nM 6.54
CHEMBL3958008 Ki = 370.5 nM 6.43
CHEMBL3979966 Ki = 505.7 nM 6.30
CHEMBL3921558 Ki = 810.0 nM 6.09
CHEMBL3971078 Ki = 893.0 nM 6.05