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Assay Detail

CHEMBL642945

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

Binding
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Alpha-1A adrenergic receptor (CHEMBL319)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
Quiñones-Torrelo C, Sagrado S, Villanueva-Camañas RM, Medina-Hernández MJ.
J Med Chem (1999) 42 : 3154 -3162
PubMed 10447960 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 10.38 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1628227 DOXEPIN 4.0 1 11.00
CHEMBL629 AMITRIPTYLINE 4.0 1 10.70
CHEMBL445 NORTRIPTYLINE 4.0 1 10.40
CHEMBL415 CLOMIPRAMINE 4.0 1 10.40
CHEMBL6437 MIANSERIN 4.0 1 10.15
CHEMBL72 DESIPRAMINE 4.0 1 9.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1628227 DOXEPIN IC50 = 0.01 nM 11.00
CHEMBL629 AMITRIPTYLINE IC50 = 0.02 nM 10.70
CHEMBL445 NORTRIPTYLINE IC50 = 0.04 nM 10.40
CHEMBL415 CLOMIPRAMINE IC50 = 0.04 nM 10.40
CHEMBL6437 MIANSERIN IC50 = 0.07 nM 10.15
CHEMBL72 DESIPRAMINE IC50 = 0.25 nM 9.60