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Assay Detail

CHEMBL753903

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

Binding
relative affinity against Opioid receptor kappa 1 in insular Ctx using [3H]U-69593 as radioligand
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Kappa-type opioid receptor (CHEMBL3614)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Modified ibogaine fragments: synthesis and preliminary pharmacological characterization of 3-ethyl-5-phenyl-1,2,3,4,5, 6-hexahydroazepino[4,5-b]benzothiophenes.
Efange SM, Mash DC, Khare AB, Ouyang Q.
J Med Chem (1998) 41 : 4486 -4491
PubMed 9804688 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.00 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL141863 1 5.89
CHEMBL343956 1 5.37
CHEMBL139081 1 4.90
CHEMBL336437 1 4.80
CHEMBL341805 1 4.79
CHEMBL23529 1 4.67
CHEMBL222287 IBOGAINE 2.0 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL141863 IC50 = 1300.0 nM 5.89
CHEMBL343956 IC50 = 4240.0 nM 5.37
CHEMBL139081 IC50 = 12500.0 nM 4.90
CHEMBL336437 IC50 = 15900.0 nM 4.80
CHEMBL341805 IC50 = 16200.0 nM 4.79
CHEMBL23529 IC50 = 21200.0 nM 4.67
CHEMBL222287 IBOGAINE IC50 = 25000.0 nM 4.60