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Assay Detail

CHEMBL757536

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

Binding
Binding affinity was measured on delta opioid receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL3222)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.
Lu Y, Nguyen TM, Weltrowska G, Berezowska I, Lemieux C, Chung NN, Schiller PW.
J Med Chem (2001) 44 : 3048 -3053
PubMed 11543672 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.11 8.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL436911 1 8.93
CHEMBL216640 1 7.87
CHEMBL573214 NORBINALTORPHIMINE 1 7.75
CHEMBL414502 1 6.91
CHEMBL506821 1 6.79
CHEMBL407124 1 6.44
CHEMBL414068 1 6.38
CHEMBL216899 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL436911 Ki = 1.18 nM 8.93
CHEMBL216640 Ki = 13.5 nM 7.87
CHEMBL573214 NORBINALTORPHIMINE Ki = 17.7 nM 7.75
CHEMBL414502 Ki = 122.0 nM 6.91
CHEMBL506821 Ki = 163.0 nM 6.79
CHEMBL407124 Ki = 364.0 nM 6.44
CHEMBL414068 Ki = 419.0 nM 6.38
CHEMBL216899 Ki = 1500.0 nM 5.82