Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL641371

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

Functional
Evaluated for its presynaptic Alpha-2 adrenergic receptor antagonistic activity against rat vas deferens using clonidine as the control expressed as slope
7
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Vas deferens
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
Kd 7 7.51 7.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10316 IDAZOXAN 3.0 1 7.93
CHEMBL25014 1 7.91
CHEMBL27926 NAPITANE 2.0 3 7.84
CHEMBL285367 1 6.78
CHEMBL433033 1 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10316 IDAZOXAN Kd = 11.75 nM 7.93
CHEMBL25014 Kd = 12.3 nM 7.91
CHEMBL27926 NAPITANE Kd = 14.45 nM 7.84
CHEMBL27926 NAPITANE Kd = 16.6 nM 7.78
CHEMBL27926 NAPITANE Kd = 20.89 nM 7.68
CHEMBL285367 Kd = 165.96 nM 6.78
CHEMBL433033 Kd = 223.87 nM 6.65