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Assay Detail

CHEMBL754931

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

Binding
Displacement of [3H]DSLET from rat brain membrane delta opioid receptor
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

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 12 7.09 8.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2110229 1 8.36
CHEMBL171763 1 8.07
CHEMBL353943 2 8.03
CHEMBL2110337 1 7.26
CHEMBL169183 1 7.19
CHEMBL353806 1 6.90
CHEMBL354641 1 6.42
CHEMBL170317 1 6.22
CHEMBL170935 1 6.05
CHEMBL422900 1 -
CHEMBL170594 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2110229 IC50 = 4.4 nM 8.36
CHEMBL171763 IC50 = 8.6 nM 8.07
CHEMBL353943 IC50 = 9.4 nM 8.03
CHEMBL2110337 IC50 = 55.0 nM 7.26
CHEMBL169183 IC50 = 64.0 nM 7.19
CHEMBL353806 IC50 = 127.0 nM 6.90
CHEMBL354641 IC50 = 385.0 nM 6.42
CHEMBL353943 IC50 = 409.0 nM 6.39
CHEMBL170317 IC50 = 600.0 nM 6.22
CHEMBL170935 IC50 = 882.0 nM 6.05
CHEMBL422900 IC50 > 1000.0 nM -
CHEMBL170594 IC50 > 1000.0 nM -