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Assay Detail

CHEMBL675907

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

Binding
Inhibitory activity in displacing [125I]- RTI-55 binding to dopamine transporter in rat striatal membranes
23
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis of 2beta-acyl-3beta-(substituted naphthyl)-8-azabicyclo[3.2.1]octanes and their binding affinities at dopamine and serotonin transport sites.
Davies HM, Gilliatt V, Kuhn LA, Saikali E, Ren P, Hammond PS, Sexton T, Childers SR.
J Med Chem (2001) 44 : 1509 -1515
PubMed 11334561 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.39 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL36720 1 10.52
CHEMBL418190 2 9.92
CHEMBL39990 1 9.89
CHEMBL34243 1 9.82
CHEMBL39589 1 9.60
CHEMBL287945 1 9.46
CHEMBL416058 1 9.41
CHEMBL435371 1 9.35
CHEMBL22930 1 8.90
CHEMBL290412 1 8.88
CHEMBL278572 1 8.28
CHEMBL23142 1 8.09
CHEMBL23672 2 8.00
CHEMBL289849 1 7.90
CHEMBL39340 1 7.60
CHEMBL287940 1 7.51
CHEMBL39764 1 7.35
CHEMBL285039 1 7.12
CHEMBL39330 1 6.83
CHEMBL290662 1 6.65
CHEMBL278122 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL36720 IC50 = 0.03 nM 10.52
CHEMBL418190 IC50 = 0.12 nM 9.92
CHEMBL39990 IC50 = 0.13 nM 9.89
CHEMBL34243 IC50 = 0.15 nM 9.82
CHEMBL39589 IC50 = 0.25 nM 9.60
CHEMBL287945 IC50 = 0.35 nM 9.46
CHEMBL416058 IC50 = 0.39 nM 9.41
CHEMBL435371 IC50 = 0.45 nM 9.35
CHEMBL22930 IC50 = 1.27 nM 8.90
CHEMBL290412 IC50 = 1.31 nM 8.88
CHEMBL418190 IC50 = 2.51 nM 8.60
CHEMBL278572 IC50 = 5.3 nM 8.28
CHEMBL23142 IC50 = 8.2 nM 8.09
CHEMBL23672 IC50 = 10.0 nM 8.00
CHEMBL289849 IC50 = 12.6 nM 7.90
CHEMBL39340 IC50 = 25.1 nM 7.60
CHEMBL287940 IC50 = 30.8 nM 7.51
CHEMBL39764 IC50 = 45.0 nM 7.35
CHEMBL285039 IC50 = 75.1 nM 7.12
CHEMBL23672 IC50 = 97.0 nM 7.01
CHEMBL39330 IC50 = 148.0 nM 6.83
CHEMBL290662 IC50 = 225.0 nM 6.65
CHEMBL278122 IC50 = 436.0 nM 6.36