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Assay Detail

CHEMBL5209600

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Functional
Inhibition of the Dopamine transporter (DAT, SLC6A3) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A3 cells (PubChem AID: 1745858)
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent dopamine transporter (CHEMBL238)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A study of the dopamine transporter using the TRACT assay, a novel in vitro tool for solute carrier drug discovery
Hubert J. Sijben; Julie J. E. van den Berg; Jeremy D. Broekhuis; Adriaan P. IJzerman; Laura H. Heitman
Sci Rep (2021) 11 : 1312
PubMed 33446713 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.46 6.70
EC50 1 4.34 4.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL543876 1 6.70
CHEMBL529437 COCAINE HYDROCHLORIDE 4.0 1 6.22
CHEMBL1557 DOPAMINE HYDROCHLORIDE 4.0 1 4.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL543876 IC50 = 200.0 nM 6.70
CHEMBL529437 COCAINE HYDROCHLORIDE IC50 = 600.0 nM 6.22
CHEMBL1557 DOPAMINE HYDROCHLORIDE EC50 = 46000.0 nM 4.34