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Assay Detail

CHEMBL672391

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

Binding
Compound was tested for binding affinity to dopamine reuptake sites in the tissue homogenates prepared from primate rat striatum using [3H]CFT as radioligand
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Papio hamadryas
Tissue Striatum
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

[123I]-2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane: high-affinity SPECT radiotracer of monoamine reuptake sites in brain.
Neumeyer JL, Wang SY, Milius RA, Baldwin RM, Zea-Ponce Y, Hoffer PB, Sybirska E, al-Tikriti M, Charney DS, Malison RT.
J Med Chem (1991) 34 : 3144 -3146
PubMed 1920365 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.59 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL311347 1 8.80
CHEMBL2079586 1 7.82
CHEMBL14391 1 7.06
CHEMBL370805 COCAINE 4.0 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL311347 IC50 = 1.6 nM 8.80
CHEMBL2079586 IC50 = 15.3 nM 7.82
CHEMBL14391 IC50 = 87.6 nM 7.06
CHEMBL370805 COCAINE IC50 = 221.0 nM 6.66