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Assay Detail

CHEMBL755215

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

Binding
Inhibitory concentration was evaluated against delta opioid receptor by the displacement of tritiated DSLET from rat brain membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Delta-type opioid receptor (CHEMBL269)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Enkephalin analogs as systemically active antinociceptive agents: O- and N-alkylated derivatives of the dipeptide amide L-2,6-dimethyltyrosyl-N-(3-phenylpropyl)-D-alaninamide.
Pitzele BS, Hamilton RW, Kudla KD, Tsymbalov S, Stapelfeld A, Savage MA, Clare M, Hammond DL, Hansen DW.
J Med Chem (1994) 37 : 888 -896
PubMed 7908696 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.05 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2110229 1 8.10
CHEMBL171763 1 8.02
CHEMBL353943 1 8.00
CHEMBL169183 1 6.91
CHEMBL2110337 1 6.88
CHEMBL2110227 1 5.75
CHEMBL170594 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2110229 IC50 = 8.0 nM 8.10
CHEMBL171763 IC50 = 9.57 nM 8.02
CHEMBL353943 IC50 = 10.0 nM 8.00
CHEMBL169183 IC50 = 124.0 nM 6.91
CHEMBL2110337 IC50 = 133.0 nM 6.88
CHEMBL2110227 IC50 = 1799.0 nM 5.75
CHEMBL170594 IC50 = 2094.0 nM 5.68