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Assay Detail

CHEMBL3766866

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

Binding
Displacement of [3H]U69,593 from guinea pig KOR after 2 hrs by liquid scintillation counting method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.
Li Y, Cazares M, Wu J, Houghten RA, Toll L, Dooley C.
J Med Chem (2016) 59 : 1239 -1245
PubMed 26789491 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.23 5.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3763495 1 5.49
CHEMBL3765059 1 5.35
CHEMBL316446 ENDOMORPHIN-1 1 5.29
CHEMBL3763920 1 5.27
CHEMBL3764556 1 5.09
CHEMBL3764157 1 5.07
CHEMBL3765741 1 5.07
CHEMBL3763985 1 -
CHEMBL3763452 1 -
CHEMBL3764234 1 -
CHEMBL3763905 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3763495 Ki = 3231.0 nM 5.49
CHEMBL3765059 Ki = 4450.0 nM 5.35
CHEMBL316446 ENDOMORPHIN-1 Ki = 5069.0 nM 5.29
CHEMBL3763920 Ki = 5330.0 nM 5.27
CHEMBL3764556 Ki = 8160.0 nM 5.09
CHEMBL3764157 Ki = 8430.0 nM 5.07
CHEMBL3765741 Ki = 8530.0 nM 5.07
CHEMBL3763985 Ki > 10000.0 nM -
CHEMBL3763452 Ki > 10000.0 nM -
CHEMBL3764234 Ki > 10000.0 nM -
CHEMBL3763905 Ki > 10000.0 nM -