Assay Detail

CHEMBL1176745

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Binding

Inhibition of [3H]dopamine reuptake at human DAT expressed in pig LLCPK cells after 1 hr

ChEMBL ↗

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Target

Sodium-dependent dopamine transporter (CHEMBL238) ↗

Open DB target context

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Sodium-dependent dopamine transporter (CHEMBL238) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Sodium-dependent dopamine transporter

CHEMBL238

Anchored from Assay target.

Protein identity Sodium-dependent dopamine transporter

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Sodium-dependent dopamine transporter (CHEMBL238) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: a new potent and selective triple reuptake inhibitor.

Micheli F, Cavanni P, Andreotti D, Arban R, Benedetti R, Bertani B, Bettati M, Bettelini L, Bonanomi G, Braggio S, Carletti R, Checchia A, Corsi M, Fazzolari E, Fontana S, Marchioro C, Merlo-Pich E, Negri M, Oliosi B, Ratti E, Read KD, Roscic M, Sartori I, Spada S, Tedesco G, Tarsi L, Terreni S, Visentini F, Zocchi A, Zonzini L, Di Fabio R.
J Med Chem (2010) 53 : 4989 -5001
PubMed 20527970 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	8.70	8.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1173532	GSK1360707	1.0	1	8.70

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1173532	GSK1360707	IC50	=	1.995	nM	8.70