Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4229769

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

Binding
Inhibition of human DAT expressed in CHOK1 cells assessed as decrease in [3H]-dopamine reuptake after 10 mins by scintillation counting method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.
Ramesh R, Reddy DS.
J Med Chem (2018) 61 : 3779 -3798
PubMed 29039662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.24 6.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2311600 1 6.15
CHEMBL2204341 1 5.58
CHEMBL637 VENLAFAXINE 4.0 1 5.35
CHEMBL427215 1 5.28
CHEMBL252720 (S)-VENLAFAXINE 1 5.18
CHEMBL251694 1 4.71
CHEMBL2204342 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2311600 IC50 = 707.0 nM 6.15
CHEMBL2204341 IC50 = 2630.0 nM 5.58
CHEMBL637 VENLAFAXINE IC50 = 4430.0 nM 5.35
CHEMBL427215 IC50 = 5270.0 nM 5.28
CHEMBL252720 (S)-VENLAFAXINE IC50 = 6670.0 nM 5.18
CHEMBL251694 IC50 = 19600.0 nM 4.71
CHEMBL2204342 IC50 = 36350.0 nM 4.44