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Assay Detail

CHEMBL1032746

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

Binding
Displacement of [3H]WIN-35428 from human dopamine transporter expressed in mouse N2A cells by scintillation counting
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type N2a
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone.
Lapinsky DJ, Aggarwal S, Huang Y, Surratt CK, Lever JR, Foster JD, Vaughan RA.
Bioorg Med Chem (2009) 17 : 3770 -3774
PubMed 19442525 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.48 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL555491 1 8.30
CHEMBL201960 PYROVALERONE 4.0 1 8.10
CHEMBL553937 1 7.55
CHEMBL558086 1 7.11
CHEMBL894 BUPROPION 4.0 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL555491 Ki = 5.0 nM 8.30
CHEMBL201960 PYROVALERONE Ki = 8.0 nM 8.10
CHEMBL553937 Ki = 28.0 nM 7.55
CHEMBL558086 Ki = 78.0 nM 7.11
CHEMBL894 BUPROPION Ki = 441.0 nM 6.36