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Assay Detail

CHEMBL4148421

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 cortex after 30 mins by Microbeta scintillation counting method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HT7 receptor agents with antidepressant activity.
Kucwaj-Brysz K, Kurczab R, Jastrzębska-Więsek M, Żesławska E, Satała G, Nitek W, Partyka A, Siwek A, Jankowska A, Wesołowska A, Kieć-Kononowicz K, Handzlik J.
Eur J Med Chem (2018) 147 : 102 -114
PubMed 29425815 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.82 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL762 OXYMETAZOLINE 4.0 1 8.82
CHEMBL4166804 1 -
CHEMBL4163778 1 -
CHEMBL4171652 1 -
CHEMBL4163626 1 -
CHEMBL4176588 1 -
CHEMBL4160262 1 -
CHEMBL4174681 1 -
CHEMBL4170484 1 -
CHEMBL4162548 1 -
CHEMBL4170657 1 -
CHEMBL4176950 1 -
CHEMBL4174055 1 -
CHEMBL4159967 1 -
CHEMBL4170613 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL762 OXYMETAZOLINE Ki = 1.5 nM 8.82
CHEMBL4166804 Ki > 10000.0 nM -
CHEMBL4163778 Ki > 10000.0 nM -
CHEMBL4171652 Ki - -
CHEMBL4163626 Ki - -
CHEMBL4176588 Ki - -
CHEMBL4160262 Ki - -
CHEMBL4174681 Ki - -
CHEMBL4170484 Ki - -
CHEMBL4162548 Ki - -
CHEMBL4170657 Ki > 5000.0 nM -
CHEMBL4176950 Ki > 5000.0 nM -
CHEMBL4174055 Ki > 10000.0 nM -
CHEMBL4159967 Ki > 10000.0 nM -
CHEMBL4170613 Ki > 5000.0 nM -