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Assay Detail

CHEMBL808120

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

Binding
Inhibition of [3H]5-HT uptake at the rat serotonin transporter.
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 serotonin transporter (CHEMBL313)
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 6.09 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281594 VANOXERINE 3.0 1 7.14
CHEMBL416409 1 6.64
CHEMBL36419 1 6.22
CHEMBL284096 1 5.99
CHEMBL33903 1 5.88
CHEMBL290799 1 5.81
CHEMBL36074 1 5.59
CHEMBL34697 1 5.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281594 VANOXERINE Ki = 73.0 nM 7.14
CHEMBL416409 Ki = 227.0 nM 6.64
CHEMBL36419 Ki = 601.0 nM 6.22
CHEMBL284096 Ki = 1020.0 nM 5.99
CHEMBL33903 Ki = 1320.0 nM 5.88
CHEMBL290799 Ki = 1560.0 nM 5.81
CHEMBL36074 Ki = 2570.0 nM 5.59
CHEMBL34697 Ki = 3580.0 nM 5.45