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Assay Detail

CHEMBL838689

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

Binding
Displacement of [3H]CIT from dopamine transporter of rat striatal homogenate
14
Total Activities
14
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 amine transporter affinities of novel phenyltropane derivatives as potential positron emission tomography (PET) imaging agents.
Peng X, Zhang A, Kula NS, Baldessarini RJ, Neumeyer JL.
Bioorg Med Chem Lett (2004) 14 : 5635 -5639
PubMed 15482938 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.73 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL97887 1 9.52
CHEMBL187299 1 9.28
CHEMBL365623 1 9.28
CHEMBL186119 1 9.24
CHEMBL184807 1 9.14
CHEMBL186306 1 9.07
CHEMBL318961 1 9.03
CHEMBL362565 1 8.91
CHEMBL365649 1 8.72
CHEMBL185608 1 8.63
CHEMBL433159 1 8.48
CHEMBL184123 1 7.97
CHEMBL365413 1 7.59
CHEMBL183259 1 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL97887 Ki = 0.3 nM 9.52
CHEMBL187299 Ki = 0.52 nM 9.28
CHEMBL365623 Ki = 0.52 nM 9.28
CHEMBL186119 Ki = 0.57 nM 9.24
CHEMBL184807 Ki = 0.72 nM 9.14
CHEMBL186306 Ki = 0.85 nM 9.07
CHEMBL318961 Ki = 0.93 nM 9.03
CHEMBL362565 Ki = 1.23 nM 8.91
CHEMBL365649 Ki = 1.91 nM 8.72
CHEMBL185608 Ki = 2.33 nM 8.63
CHEMBL433159 Ki = 3.33 nM 8.48
CHEMBL184123 Ki = 10.6 nM 7.97
CHEMBL365413 Ki = 25.7 nM 7.59
CHEMBL183259 Ki = 44.5 nM 7.35