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Assay Detail

CHEMBL4432469

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

Binding
Inhibition of [3H]dofetilide binding to human ERG expressed in HEK293 cell membranes after 60 mins by liquid scintillation spectrometric analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Synthesis and in vitro evaluation of water-soluble 1,4-diphenethylpiperazine analogs as novel inhibitors of the vesicular monoamine transporter-2.
Nickell JR, Culver JP, Janganati V, Zheng G, Dwoskin LP, Crooks PA.
Bioorg Med Chem Lett (2016) 26 : 4441 -4445
PubMed 27524311 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.03 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122425 1 6.62
CHEMBL4443407 1 5.99
CHEMBL4442303 1 5.97
CHEMBL4519939 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122425 Ki = 238.0 nM 6.62
CHEMBL4443407 Ki = 1020.0 nM 5.99
CHEMBL4442303 Ki = 1080.0 nM 5.97
CHEMBL4519939 Ki = 2940.0 nM 5.53