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

CHEMBL746900

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

Binding
The binding affinity at the Norepinephrine transporter reuptake sites determined using competition binding assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine.
Wikström HV, Mensonides-Harsema MM, Cremers TI, Moltzen EK, Arnt J.
J Med Chem (2002) 45 : 3280 -3285
PubMed 12109911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.29 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6437 MIANSERIN 4.0 1 7.66
CHEMBL654 MIRTAZAPINE 4.0 1 6.58
CHEMBL111184 1 5.91
CHEMBL324270 1 5.75
CHEMBL113238 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6437 MIANSERIN IC50 = 22.0 nM 7.66
CHEMBL654 MIRTAZAPINE IC50 = 260.0 nM 6.58
CHEMBL111184 IC50 = 1240.0 nM 5.91
CHEMBL324270 IC50 = 1780.0 nM 5.75
CHEMBL113238 IC50 = 2860.0 nM 5.54