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Assay Detail

CHEMBL4048900

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

Binding
Displacement of [3H]WIN 35,428 from DAT in Sprague-Dawley rat striatum after 120 mins by scintillation counting method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D4 Receptor.
Del Bello F, Bonifazi A, Giorgioni G, Cifani C, Micioni Di Bonaventura MV, Petrelli R, Piergentili A, Fontana S, Mammoli V, Yano H, Matucci R, Vistoli G, Quaglia W.
J Med Chem (2018) 61 : 3712 -3725
PubMed 29589445 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.63 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4072818 1 6.35
CHEMBL3354065 1 5.47
CHEMBL4085780 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4072818 Ki = 446.68 nM 6.35
CHEMBL3354065 Ki = 3388.44 nM 5.47
CHEMBL4085780 Ki = 8709.64 nM 5.06