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Assay Detail

CHEMBL648048

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

Binding
In vitro binding affinity at Alpha-1 adrenergic receptor by radioligand binding assay using [3H]prazosin
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-1 (CHEMBL1907610)
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 6.97 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11 IMIPRAMINE 4.0 1 7.34
CHEMBL25014 1 7.32
CHEMBL27926 NAPITANE 2.0 3 7.12
CHEMBL285367 1 6.98
CHEMBL433033 1 6.72
CHEMBL10316 IDAZOXAN 3.0 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11 IMIPRAMINE Ki = 46.0 nM 7.34
CHEMBL25014 Ki = 47.4 nM 7.32
CHEMBL27926 NAPITANE Ki = 75.9 nM 7.12
CHEMBL285367 Ki = 104.0 nM 6.98
CHEMBL27926 NAPITANE Ki = 106.0 nM 6.97
CHEMBL27926 NAPITANE Ki = 112.0 nM 6.95
CHEMBL433033 Ki = 189.0 nM 6.72
CHEMBL10316 IDAZOXAN Ki = 403.0 nM 6.39