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Assay Detail

CHEMBL744173

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

Binding
The compound was tested for binding affinity nisoxatine ligand
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Norepinephrine transporter (CHEMBL304)
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 9 5.38 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112789 1 5.89
CHEMBL275707 RIMCAZOLE 2.0 1 5.67
CHEMBL2112783 1 5.60
CHEMBL2112787 1 5.44
CHEMBL324896 1 5.38
CHEMBL2112788 1 5.34
CHEMBL2112784 1 5.17
CHEMBL2112760 1 5.03
CHEMBL2112791 1 4.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112789 Ki = 1300.0 nM 5.89
CHEMBL275707 RIMCAZOLE Ki = 2160.0 nM 5.67
CHEMBL2112783 Ki = 2490.0 nM 5.60
CHEMBL2112787 Ki = 3640.0 nM 5.44
CHEMBL324896 Ki = 4120.0 nM 5.38
CHEMBL2112788 Ki = 4580.0 nM 5.34
CHEMBL2112784 Ki = 6810.0 nM 5.17
CHEMBL2112760 Ki = 9370.0 nM 5.03
CHEMBL2112791 Ki = 13900.0 nM 4.86