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Assay Detail

CHEMBL643683

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

Binding
binding affinity towards alpha-2 adrenergic receptor, using [3H]- atipamezole as radioligand from rat frontal cortex membranes
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and in vitro evaluation of 2,3-dimethoxy-5-(fluoroalkyl)-substituted benzamides: high-affinity ligands for CNS dopamine D2 receptors.
Bishop JE, Mathis CA, Gerdes JM, Whitney JM, Eaton AM, Mailman RB.
J Med Chem (1991) 34 : 1612 -1624
PubMed 1827843 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.09 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL44237 EPIDEPRIDE 1 8.30
CHEMBL43506 1 8.02
CHEMBL42448 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL44237 EPIDEPRIDE Ki = 5.0 nM 8.30
CHEMBL43506 Ki = 9.5 nM 8.02
CHEMBL42448 Ki = 11.1 nM 7.96