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Assay Detail

CHEMBL750462

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

Functional
Effect on synaptosomal uptake inhibition of Noradrenaline (NA)
12
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Neuroleptic activity and dopamine-uptake inhibition in 1-piperazino-3-phenylindans.
Bøgesø KP.
J Med Chem (1983) 26 : 935 -947
PubMed 6134833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.96 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2096748 1 9.52
CHEMBL2447974 6 8.60
CHEMBL322067 1 8.27
CHEMBL273575 NOMIFENSINE 4.0 1 8.18
CHEMBL176506 1 8.17
CHEMBL2448057 2 8.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2096748 IC50 = 0.3 nM 9.52
CHEMBL2447974 IC50 = 2.5 nM 8.60
CHEMBL322067 IC50 = 5.4 nM 8.27
CHEMBL273575 NOMIFENSINE IC50 = 6.6 nM 8.18
CHEMBL176506 IC50 = 6.8 nM 8.17
CHEMBL2447974 IC50 = 7.8 nM 8.11
CHEMBL2447974 IC50 = 7.7 nM 8.11
CHEMBL2448057 IC50 = 8.2 nM 8.09
CHEMBL2448057 IC50 = 10.0 nM 8.00
CHEMBL2447974 IC50 = 32.0 nM 7.50
CHEMBL2447974 IC50 = 120.0 nM 6.92
CHEMBL2447974 IC50 = 910.0 nM 6.04