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Assay Detail

CHEMBL805014

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

Binding
Binding affinity of Sigma opioid receptor type 1 in Guinea pig brain membranes using [3H]pentazocine ligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 8 6.25 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112787 1 7.01
CHEMBL2112783 1 6.98
CHEMBL2112784 1 6.86
CHEMBL2112760 1 6.26
CHEMBL2112788 1 6.22
CHEMBL275707 RIMCAZOLE 2.0 1 6.04
CHEMBL2112789 1 5.36
CHEMBL2112791 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112787 Ki = 97.2 nM 7.01
CHEMBL2112783 Ki = 104.1 nM 6.98
CHEMBL2112784 Ki = 138.0 nM 6.86
CHEMBL2112760 Ki = 552.0 nM 6.26
CHEMBL2112788 Ki = 596.0 nM 6.22
CHEMBL275707 RIMCAZOLE Ki = 908.0 nM 6.04
CHEMBL2112789 Ki = 4420.0 nM 5.36
CHEMBL2112791 Ki = 5720.0 nM 5.24