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Assay Detail

CHEMBL1008804

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

Binding
Displacement of [3H]WIN-35428 from DAT in rat striatum membrane
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Striatum
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Dual DAT/sigma1 receptor ligands based on 3-(4-(3-(bis(4-fluorophenyl)amino)propyl)piperazin-1-yl)-1-phenylpropan-1-ol.
Cao J, Kopajtic T, Katz JL, Newman AH.
Bioorg Med Chem Lett (2008) 18 : 5238 -5241
PubMed 18774292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.87 8.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL495519 1 8.76
CHEMBL281594 VANOXERINE 3.0 1 8.75
CHEMBL489601 1 8.49
CHEMBL314424 1 8.46
CHEMBL498600 1 8.37
CHEMBL495520 1 8.27
CHEMBL497586 1 8.25
CHEMBL496753 1 8.17
CHEMBL507255 1 8.16
CHEMBL502790 1 8.03
CHEMBL505059 1 7.83
CHEMBL490424 1 7.82
CHEMBL495726 1 7.66
CHEMBL487088 1 7.47
CHEMBL443649 1 7.44
CHEMBL444690 1 7.29
CHEMBL275707 RIMCAZOLE 2.0 1 7.01
CHEMBL521582 1 5.44
CHEMBL60542 (+)-PENTAZOCINE 1 -
CHEMBL560 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL495519 Ki = 1.72 nM 8.76
CHEMBL281594 VANOXERINE Ki = 1.77 nM 8.75
CHEMBL489601 Ki = 3.26 nM 8.49
CHEMBL314424 Ki = 3.45 nM 8.46
CHEMBL498600 Ki = 4.28 nM 8.37
CHEMBL495520 Ki = 5.36 nM 8.27
CHEMBL497586 Ki = 5.57 nM 8.25
CHEMBL496753 Ki = 6.71 nM 8.17
CHEMBL507255 Ki = 6.92 nM 8.16
CHEMBL502790 Ki = 9.36 nM 8.03
CHEMBL505059 Ki = 14.9 nM 7.83
CHEMBL490424 Ki = 15.1 nM 7.82
CHEMBL495726 Ki = 21.7 nM 7.66
CHEMBL487088 Ki = 33.5 nM 7.47
CHEMBL443649 Ki = 36.6 nM 7.44
CHEMBL444690 Ki = 51.3 nM 7.29
CHEMBL275707 RIMCAZOLE Ki = 97.7 nM 7.01
CHEMBL521582 Ki = 3620.0 nM 5.44
CHEMBL60542 (+)-PENTAZOCINE Ki - -
CHEMBL560 Ki - -