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Assay Detail

CHEMBL805629

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

Binding
50% Inhibition against Serotonin transporter in rat midbrain tissue by displacing [3H]paroxetine radioligand
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Midbrain
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and transporter binding properties of 3beta-[4'-(phenylalkyl, -phenylalkenyl, and -phenylalkynyl)phenyl]tropane-2beta-carboxylic acid methyl esters: evidence of a remote phenyl binding domain on the dopamine transporter.
Blough BE, Keverline KI, Nie Z, Navarro H, Kuhar MJ, Carroll FI.
J Med Chem (2002) 45 : 4029 -4037
PubMed 12190324 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.82 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2310867 1 9.10
CHEMBL3350431 1 8.36
CHEMBL2310868 1 8.02
CHEMBL2310874 1 7.94
CHEMBL2310884 1 7.94
CHEMBL2310871 1 7.88
CHEMBL2310869 1 7.80
CHEMBL50157 1 7.55
CHEMBL2310872 1 7.33
CHEMBL2310866 1 7.15
CHEMBL2310876 1 7.02
CHEMBL2310877 1 6.63
CHEMBL2373962 1 6.62
CHEMBL2310883 1 6.47
CHEMBL84680 1 6.46
CHEMBL2310881 1 6.11
CHEMBL2310870 1 6.08
CHEMBL2310878 1 5.91
CHEMBL2310875 1 5.87
CHEMBL1790051 1 5.71
CHEMBL2310873 1 5.66
CHEMBL2310879 1 5.57
CHEMBL2310865 1 5.32
CHEMBL2310880 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2310867 IC50 = 0.8 nM 9.10
CHEMBL3350431 IC50 = 4.4 nM 8.36
CHEMBL2310868 IC50 = 9.5 nM 8.02
CHEMBL2310874 IC50 = 11.4 nM 7.94
CHEMBL2310884 IC50 = 11.4 nM 7.94
CHEMBL2310871 IC50 = 13.1 nM 7.88
CHEMBL2310869 IC50 = 15.7 nM 7.80
CHEMBL50157 IC50 = 28.4 nM 7.55
CHEMBL2310872 IC50 = 46.8 nM 7.33
CHEMBL2310866 IC50 = 70.4 nM 7.15
CHEMBL2310876 IC50 = 95.8 nM 7.02
CHEMBL2310877 IC50 = 234.0 nM 6.63
CHEMBL2373962 IC50 = 240.0 nM 6.62
CHEMBL2310883 IC50 = 335.0 nM 6.47
CHEMBL84680 IC50 = 345.0 nM 6.46
CHEMBL2310881 IC50 = 781.0 nM 6.11
CHEMBL2310870 IC50 = 828.0 nM 6.08
CHEMBL2310878 IC50 = 1243.0 nM 5.91
CHEMBL2310875 IC50 = 1340.0 nM 5.87
CHEMBL1790051 IC50 = 1960.0 nM 5.71
CHEMBL2310873 IC50 = 2180.0 nM 5.66
CHEMBL2310879 IC50 = 2710.0 nM 5.57
CHEMBL2310865 IC50 = 4824.0 nM 5.32
CHEMBL2310880 IC50 = 7240.0 nM 5.14