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Assay Detail

CHEMBL648038

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

Binding
Evaluated for affinity at Alpha-1 adrenergic receptor of rat brain using [3H]prazosin as radioligand in radioligand binding assay
5
Total Activities
5
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 A-80426: A putative novel antidepressant combining -2 antagonism with 5-HT uptake inhibition
Meyer MD, Hancock AA, Tietje K, Sippy kB, Giardina WJ, Kerwin JF
Bioorg Med Chem Lett (1995) 5 : 2287 -2292
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.16 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL268258 1 6.96
CHEMBL75342 1 6.62
CHEMBL10347 RAUWOLSCINE 1 6.35
CHEMBL41 FLUOXETINE 4.0 1 5.58
CHEMBL490 PAROXETINE 4.0 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL268258 Ki = 110.0 nM 6.96
CHEMBL75342 Ki = 241.0 nM 6.62
CHEMBL10347 RAUWOLSCINE Ki = 450.0 nM 6.35
CHEMBL41 FLUOXETINE Ki = 2620.0 nM 5.58
CHEMBL490 PAROXETINE Ki = 5320.0 nM 5.27