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Assay Detail

CHEMBL679185

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

Binding
Binding affinity Sprague-Dawley rats using [3H]WIN-35428 ligand
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues.
Husbands SM, Izenwasser S, Kopajtic T, Bowen WD, Vilner BJ, Katz JL, Newman AH.
J Med Chem (1999) 42 : 4446 -4455
PubMed 10543888 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.24 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112787 1 7.21
CHEMBL2112788 1 6.96
CHEMBL275707 RIMCAZOLE 2.0 1 6.65
CHEMBL2112783 1 6.58
CHEMBL2112760 1 6.36
CHEMBL2112784 1 6.09
CHEMBL2112791 1 5.62
CHEMBL2112789 1 5.41
CHEMBL324896 1 5.31
CHEMBL110726 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112787 Ki = 61.0 nM 7.21
CHEMBL2112788 Ki = 109.0 nM 6.96
CHEMBL275707 RIMCAZOLE Ki = 224.0 nM 6.65
CHEMBL2112783 Ki = 263.0 nM 6.58
CHEMBL2112760 Ki = 436.0 nM 6.36
CHEMBL2112784 Ki = 813.0 nM 6.09
CHEMBL2112791 Ki = 2400.0 nM 5.62
CHEMBL2112789 Ki = 3890.0 nM 5.41
CHEMBL324896 Ki = 4930.0 nM 5.31
CHEMBL110726 Ki = 112700.0 nM -