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Assay Detail

CHEMBL676682

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Binding
Inhibition of [3H]dopamine uptake via rat dopamine receptor.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-activity relationship studies of highly selective inhibitors of the dopamine transporter: N-benzylpiperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine.
Greiner E, Prisinzano T, Johnson EM, Dersch CM, Marcus J, Partilla JS, Rothman RB, Jacobson AE, Rice KC.
J Med Chem (2003) 46 : 1465 -1469
PubMed 12672246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.26 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34697 1 8.57
CHEMBL36419 1 8.42
CHEMBL281594 VANOXERINE 3.0 1 8.37
CHEMBL36074 1 8.29
CHEMBL33903 1 8.28
CHEMBL290799 1 8.16
CHEMBL416409 1 8.14
CHEMBL284096 1 7.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34697 Ki = 2.7 nM 8.57
CHEMBL36419 Ki = 3.8 nM 8.42
CHEMBL281594 VANOXERINE Ki = 4.3 nM 8.37
CHEMBL36074 Ki = 5.1 nM 8.29
CHEMBL33903 Ki = 5.3 nM 8.28
CHEMBL290799 Ki = 6.9 nM 8.16
CHEMBL416409 Ki = 7.2 nM 8.14
CHEMBL284096 Ki = 13.6 nM 7.87