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Assay Detail

CHEMBL4190749

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

Binding
Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis
12
Total Activities
12
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 Autocuration

Target

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

Publication

Medchemcomm (2016) 7 : 2368 -2380
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.14 9.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL440765 U-69593 1 9.01
CHEMBL80 NALOXONE 4.0 1 8.16
CHEMBL70 MORPHINE 4.0 1 7.46
CHEMBL4212604 1 6.88
CHEMBL4215892 1 6.54
CHEMBL4206082 1 6.04
CHEMBL4203694 1 5.89
CHEMBL4216136 1 -
CHEMBL4203850 1 -
CHEMBL4209225 1 -
CHEMBL4218965 1 -
CHEMBL4216717 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL440765 U-69593 Ki = 0.97 nM 9.01
CHEMBL80 NALOXONE Ki = 6.9 nM 8.16
CHEMBL70 MORPHINE Ki = 35.0 nM 7.46
CHEMBL4212604 Ki = 132.0 nM 6.88
CHEMBL4215892 Ki = 286.0 nM 6.54
CHEMBL4206082 Ki = 912.0 nM 6.04
CHEMBL4203694 Ki = 1300.0 nM 5.89
CHEMBL4216136 Ki > 1000.0 nM -
CHEMBL4203850 Ki > 1000.0 nM -
CHEMBL4209225 Ki > 1000.0 nM -
CHEMBL4218965 Ki > 1000.0 nM -
CHEMBL4216717 Ki > 1000.0 nM -