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Assay Detail

CHEMBL670585

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

Binding
Compound was tested for binding against Dopamine transporter using radioligand as [3H]-RTI 55
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909).
Matecka D, Rothman RB, Radesca L, de Costa BR, Dersch CM, Partilla JS, Pert A, Glowa JR, Wojnicki FH, Rice KC.
J Med Chem (1996) 39 : 4704 -4716
PubMed 8941383 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.08 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL102119 1 8.96
CHEMBL143612 1 8.80
CHEMBL370805 COCAINE 4.0 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL102119 IC50 = 1.1 nM 8.96
CHEMBL143612 IC50 = 1.6 nM 8.80
CHEMBL370805 COCAINE IC50 = 341.0 nM 6.47