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Assay Detail

CHEMBL649633

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

Binding
In vitro binding affinity at Alpha-2 adrenergic receptor in rat cortex by radioligand binding assay using [3H]rauwolscine
8
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

Synthesis and pharmacological characterization of ABT-200: a putative novel antidepressant combining potent -2 antagonism with moderate NE uptake inhibition
Zelle RE, Hancock AA, Buckner SA, Basha FZ, Tietje K, DeBernardis JF, Meyer MD
Bioorg Med Chem Lett (1994) 4 : 1319 -1322
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.64 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27926 NAPITANE 2.0 3 9.37
CHEMBL25014 1 9.30
CHEMBL10316 IDAZOXAN 3.0 1 8.76
CHEMBL285367 1 8.68
CHEMBL433033 1 8.34
CHEMBL11 IMIPRAMINE 4.0 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27926 NAPITANE Ki = 0.428 nM 9.37
CHEMBL25014 Ki = 0.5 nM 9.30
CHEMBL27926 NAPITANE Ki = 0.708 nM 9.15
CHEMBL27926 NAPITANE Ki = 1.23 nM 8.91
CHEMBL10316 IDAZOXAN Ki = 1.72 nM 8.76
CHEMBL285367 Ki = 2.08 nM 8.68
CHEMBL433033 Ki = 4.56 nM 8.34
CHEMBL11 IMIPRAMINE Ki = 255.0 nM 6.59