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Assay Detail

CHEMBL753703

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

Binding
In vitro binding affinity against human norepinephrine transporter in human embryonic kidney cell line by using [125I]-RTI-55 radioligand
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent noradrenaline transporter (CHEMBL222)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, radiosynthesis, and biological evaluation of carbon-11 and iodine-123 labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-haloethenyl)phenyl]tropanes: candidate radioligands for in vivo imaging of the serotonin transporter.
Plisson C, McConathy J, Martarello L, Malveaux EJ, Camp VM, Williams L, Votaw JR, Goodman MM.
J Med Chem (2004) 47 : 1122 -1135
PubMed 14971892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.39 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14531 1 8.60
CHEMBL14257 1 8.25
CHEMBL14305 1 6.96
CHEMBL14924 1 6.79
CHEMBL275212 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14531 Ki = 2.5 nM 8.60
CHEMBL14257 Ki = 5.6 nM 8.25
CHEMBL14305 Ki = 111.0 nM 6.96
CHEMBL14924 Ki = 161.0 nM 6.79
CHEMBL275212 Ki = 450.0 nM 6.35