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Assay Detail

CHEMBL641048

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

Functional
Evaluated for its postsynaptic Alpha-2 adrenergic receptor antagonist activity against dog saphenous vein using norepinephrine as the control expressed as slope
7
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Canis lupus familiaris
Tissue Saphenous vein
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2095158)
Type PROTEIN FAMILY
Organism Homo sapiens

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
Kd 7 7.64 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27926 NAPITANE 2.0 3 8.25
CHEMBL25014 1 8.15
CHEMBL10316 IDAZOXAN 3.0 1 7.28
CHEMBL285367 1 6.80
CHEMBL433033 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27926 NAPITANE Kd = 5.623 nM 8.25
CHEMBL27926 NAPITANE Kd = 6.761 nM 8.17
CHEMBL27926 NAPITANE Kd = 7.079 nM 8.15
CHEMBL25014 Kd = 7.079 nM 8.15
CHEMBL10316 IDAZOXAN Kd = 52.48 nM 7.28
CHEMBL285367 Kd = 158.49 nM 6.80
CHEMBL433033 Kd = 208.93 nM 6.68