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

CHEMBL4024875

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

Binding
Inhibition of [3H]dopamine uptake at DAT in rat brain striatal synaptosomes by liquid scintillation counting analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions.
Jackson PA, Widen JC, Harki DA, Brummond KM.
J Med Chem (2017) 60 : 839 -885
PubMed 27996267 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.31 4.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8211 N-ETHYLMALEIMIDE 1 4.33
CHEMBL721 ACROLEIN 1 4.28
CHEMBL1600824 1 -
CHEMBL9019 ACRYLIC ACID METHYL ESTER 1 -
CHEMBL348107 ACRYLAMIDE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8211 N-ETHYLMALEIMIDE IC50 = 46773.51 nM 4.33
CHEMBL721 ACROLEIN IC50 = 52480.75 nM 4.28
CHEMBL1600824 IC50 = 331131.12 nM -
CHEMBL9019 ACRYLIC ACID METHYL ESTER IC50 = 461317574.56 nM -
CHEMBL348107 ACRYLAMIDE IC50 = 437522105.16 nM -