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Assay Detail

CHEMBL879860

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

Binding
Displacement of [125I]RTI-55 from dopamine transporter of rat brain membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis of 3 beta-aryl-8-azabicyclo[3.2.1]octanes with high binding affinities and selectivities for the serotonin transporter site.
Davies HM, Kuhn LA, Thornley C, Matasi JJ, Sexton T, Childers SR.
J Med Chem (1996) 39 : 2554 -2558
PubMed 8691453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.59 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418190 1 9.92
CHEMBL314361 1 9.05
CHEMBL85492 1 8.82
CHEMBL87983 1 8.33
CHEMBL82807 1 8.14
CHEMBL23142 1 8.09
CHEMBL85877 1 7.80
CHEMBL36720 1 7.44
CHEMBL87678 1 6.72
CHEMBL314919 1 6.57
CHEMBL87739 1 6.50
CHEMBL278122 1 6.36
CHEMBL84899 1 6.31
CHEMBL85256 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418190 IC50 = 0.12 nM 9.92
CHEMBL314361 IC50 = 0.9 nM 9.05
CHEMBL85492 IC50 = 1.5 nM 8.82
CHEMBL87983 IC50 = 4.7 nM 8.33
CHEMBL82807 IC50 = 7.2 nM 8.14
CHEMBL23142 IC50 = 8.2 nM 8.09
CHEMBL85877 IC50 = 16.0 nM 7.80
CHEMBL36720 IC50 = 36.0 nM 7.44
CHEMBL87678 IC50 = 190.0 nM 6.72
CHEMBL314919 IC50 = 270.0 nM 6.57
CHEMBL87739 IC50 = 320.0 nM 6.50
CHEMBL278122 IC50 = 440.0 nM 6.36
CHEMBL84899 IC50 = 490.0 nM 6.31
CHEMBL85256 IC50 = 540.0 nM 6.27