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Assay Detail

CHEMBL754612

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

Binding
Binding affinity to displace radioligand [3H]U-69593 on Opioid receptor kappa 1 in guinea pig membranes.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Selective protection and functionalization of morphine: synthesis and opioid receptor binding properties of 3-amino-3-desoxymorphine derivatives.
Wentland MP, Duan W, Cohen DJ, Bidlack JM.
J Med Chem (2000) 43 : 3558 -3565
PubMed 11000010 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.38 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56585 CYCLAZOCINE 2.0 1 10.28
CHEMBL2367916 1 9.27
CHEMBL2367918 1 8.92
CHEMBL70 MORPHINE 4.0 1 7.62
CHEMBL333965 1 6.62
CHEMBL119332 1 6.54
CHEMBL333959 1 6.13
CHEMBL119692 1 5.55
CHEMBL332927 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56585 CYCLAZOCINE Ki = 0.052 nM 10.28
CHEMBL2367916 Ki = 0.54 nM 9.27
CHEMBL2367918 Ki = 1.2 nM 8.92
CHEMBL70 MORPHINE Ki = 24.0 nM 7.62
CHEMBL333965 Ki = 240.0 nM 6.62
CHEMBL119332 Ki = 290.0 nM 6.54
CHEMBL333959 Ki = 740.0 nM 6.13
CHEMBL119692 Ki = 2800.0 nM 5.55
CHEMBL332927 Ki = 3400.0 nM 5.47