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Assay Detail

CHEMBL863115

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

Binding
Displacement of [3H]beta-CIT from DAT in rat caudate homogenate
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis and monoamine transporter affinity of 2beta-carbomethoxy-3beta-(4'-p-substituted phenyl)-piperidine analogs of cocaine.
Bois F, Baldwin RM, Kula NS, Baldessarini RJ, Al Tikriti M, Innis RB, Tamagnan GD.
Bioorg Med Chem Lett (2006) 16 : 5222 -5225
PubMed 16908151 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.11 9.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215376 1 9.02
CHEMBL213921 1 6.91
CHEMBL215988 1 6.71
CHEMBL214567 1 6.69
CHEMBL213823 1 6.22
CHEMBL386244 1 -
CHEMBL385645 1 -
CHEMBL214618 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215376 Ki = 0.96 nM 9.02
CHEMBL213921 Ki = 123.0 nM 6.91
CHEMBL215988 Ki = 195.0 nM 6.71
CHEMBL214567 Ki = 205.0 nM 6.69
CHEMBL213823 Ki = 598.0 nM 6.22
CHEMBL386244 Ki > 10000.0 nM -
CHEMBL385645 Ki > 10000.0 nM -
CHEMBL214618 Ki >= 5000.0 nM -