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Assay Detail

CHEMBL4615662

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

Binding
Displacement of [3H]-U69,593 from KOR in guinea pig brain membranes incubated for 30 mins by liquid scintillation counting
15
Total Activities
15
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

Novel <i>N</i>-Substituted Benzomorphan-Based Compounds: From MOR-Agonist/DOR-Antagonist to Biased/Unbiased MOR Agonists.
Pasquinucci L, Parenti C, Ruiz-Cantero MC, Georgoussi Z, Pallaki P, Cobos EJ, Amata E, Marrazzo A, Prezzavento O, Arena E, Dichiara M, Salerno L, Turnaturi R.
ACS Med Chem Lett (2020) 11 : 678 -685
PubMed 32435370 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.96 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290543 1 9.57
CHEMBL4643466 1 7.51
CHEMBL4648293 1 6.82
CHEMBL4633897 1 6.60
CHEMBL4637982 1 6.50
CHEMBL4641938 1 6.50
CHEMBL4638339 1 6.47
CHEMBL4647583 1 6.35
CHEMBL4642448 1 6.32
CHEMBL4647736 1 -
CHEMBL4638553 1 -
CHEMBL4644789 1 -
CHEMBL4634899 1 -
CHEMBL4638139 1 -
CHEMBL4644522 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290543 Ki = 0.27 nM 9.57
CHEMBL4643466 Ki = 31.0 nM 7.51
CHEMBL4648293 Ki = 151.0 nM 6.82
CHEMBL4633897 Ki = 252.0 nM 6.60
CHEMBL4637982 Ki = 313.0 nM 6.50
CHEMBL4641938 Ki = 320.0 nM 6.50
CHEMBL4638339 Ki = 340.0 nM 6.47
CHEMBL4647583 Ki = 444.0 nM 6.35
CHEMBL4642448 Ki = 480.0 nM 6.32
CHEMBL4647736 Ki > 5000.0 nM -
CHEMBL4638553 Ki > 3000.0 nM -
CHEMBL4644789 Ki > 2000.0 nM -
CHEMBL4634899 Ki > 3000.0 nM -
CHEMBL4638139 Ki > 1000.0 nM -
CHEMBL4644522 Ki > 2000.0 nM -