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Assay Detail

CHEMBL884449

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Binding
Binding affinity was evaluated using [3H]WIN-35428 binding to dopamine transporter (DAT) in rat caudate-putamen
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Caudate-putamen
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Isothiocyanate derivatives of 9-[3-(cis-3,5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole): irreversible ligands for the dopamine transporter.
Husbands SM, Izenwasser S, Loeloff RJ, Katz JL, Bowen WD, Vilner BJ, Newman AH.
J Med Chem (1997) 40 : 4340 -4346
PubMed 9435903 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.50 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275707 RIMCAZOLE 2.0 1 7.24
CHEMBL138438 1 7.06
CHEMBL2112760 1 6.61
CHEMBL336707 1 6.28
CHEMBL336706 1 5.90
CHEMBL140191 1 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275707 RIMCAZOLE IC50 = 57.6 nM 7.24
CHEMBL138438 IC50 = 86.7 nM 7.06
CHEMBL2112760 IC50 = 244.0 nM 6.61
CHEMBL336707 IC50 = 523.0 nM 6.28
CHEMBL336706 IC50 = 1250.0 nM 5.90
CHEMBL140191 IC50 = 1330.0 nM 5.88