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Assay Detail

CHEMBL673203

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

Binding
Displacement of [3H]WIN-35428(0.5 nM) from Dopamine transporter
13
Total Activities
11
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 ligand binding of tropane ring analogues of paroxetine.
Keverline-Frantz KI, Boja JW, Kuhar MJ, Abraham P, Burgess JP, Lewin AH, Carroll FI.
J Med Chem (1998) 41 : 247 -257
PubMed 9457247 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.73 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL606881 1 8.52
CHEMBL88301 2 8.41
CHEMBL312977 1 7.56
CHEMBL314878 1 6.85
CHEMBL606825 1 6.76
CHEMBL606927 1 6.53
CHEMBL606877 1 6.51
CHEMBL87616 2 6.39
CHEMBL490 PAROXETINE 4.0 1 6.21
CHEMBL606828 1 5.98
CHEMBL606826 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL606881 IC50 = 3.01 nM 8.52
CHEMBL88301 IC50 = 3.86 nM 8.41
CHEMBL312977 IC50 = 27.6 nM 7.56
CHEMBL314878 IC50 = 142.0 nM 6.85
CHEMBL606825 IC50 = 172.0 nM 6.76
CHEMBL606927 IC50 = 298.0 nM 6.53
CHEMBL606877 IC50 = 308.0 nM 6.51
CHEMBL87616 IC50 = 403.0 nM 6.39
CHEMBL490 PAROXETINE IC50 = 623.0 nM 6.21
CHEMBL87616 IC50 = 835.0 nM 6.08
CHEMBL606828 IC50 = 1050.0 nM 5.98
CHEMBL88301 IC50 = 1210.0 nM 5.92
CHEMBL606826 IC50 = 1500.0 nM 5.82