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Assay Detail

CHEMBL753185

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

Binding
Binding affinity against Opioid receptor kappa 1 was determined in brain membrane preparations from male Hartley guinea-pigs
7
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

C-alkylated spiro[benzofuran-3(2H),4'-1'-methyl-piperidine-7-ols] as potent opioids: a conformation-activity study.
Tsai YC, Liou JP, Liao R, Cheng CY, Tao PL.
Bioorg Med Chem Lett (1998) 8 : 1813 -1818
PubMed 9873439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.26 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300689 2 6.75
CHEMBL70 MORPHINE 4.0 1 5.73
CHEMBL607 MEPERIDINE 4.0 1 -
CHEMBL50098 1 -
CHEMBL431156 1 -
CHEMBL297281 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300689 Ki = 177.0 nM 6.75
CHEMBL300689 Ki = 505.0 nM 6.30
CHEMBL70 MORPHINE Ki = 1870.0 nM 5.73
CHEMBL607 MEPERIDINE Ki > 100000.0 nM -
CHEMBL50098 Ki > 100000.0 nM -
CHEMBL431156 Ki > 100000.0 nM -
CHEMBL297281 Ki > 100000.0 nM -