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Assay Detail

CHEMBL671629

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

Binding
In vitro inhibitory activity against radioligand [3H]-WN 35,428 binding to dopamine transporter (DAT) in rat striatal tissue
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Striatum
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium-dependent dopamine transporter (CHEMBL338)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3 Beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester as a high-affinity selective ligand for the serotonin transporter.
Blough BE, Abraham P, Mills AC, Lewin AH, Boja JW, Scheffel U, Kuhar MJ, Carroll FI.
J Med Chem (1997) 40 : 3861 -3864
PubMed 9397165 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.70 9.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81525 1 9.21
CHEMBL306208 1 8.95
CHEMBL2079586 1 7.86
CHEMBL1790051 1 7.64
CHEMBL67387 1 7.58
CHEMBL340523 1 7.30
CHEMBL334546 1 7.26
CHEMBL370805 COCAINE 4.0 1 7.05
CHEMBL127623 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81525 IC50 = 0.62 nM 9.21
CHEMBL306208 IC50 = 1.12 nM 8.95
CHEMBL2079586 IC50 = 13.9 nM 7.86
CHEMBL1790051 IC50 = 23.0 nM 7.64
CHEMBL67387 IC50 = 26.0 nM 7.58
CHEMBL340523 IC50 = 49.9 nM 7.30
CHEMBL334546 IC50 = 55.0 nM 7.26
CHEMBL370805 COCAINE IC50 = 89.1 nM 7.05
CHEMBL127623 IC50 = 329.0 nM 6.48