Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL754606

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

Binding
Binding affinity for delta opioid receptors was determined by displacement of [3H]DSLET from rat brain membrane binding site
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
Schmidt R, Vogel D, Mrestani-Klaus C, Brandt W, Neubert K, Chung NN, Lemieux C, Schiller PW.
J Med Chem (1994) 37 : 1136 -1144
PubMed 8164255 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.44 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8234 ENKEPHALIN 1 8.60
CHEMBL557035 1 8.52
CHEMBL14887 1 7.99
CHEMBL15100 1 7.88
CHEMBL275670 1 7.76
CHEMBL278891 1 7.63
CHEMBL280264 1 7.55
CHEMBL274012 1 7.20
CHEMBL278889 1 7.15
CHEMBL2370199 1 5.89
CHEMBL2370207 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8234 ENKEPHALIN Ki = 2.53 nM 8.60
CHEMBL557035 Ki = 3.0 nM 8.52
CHEMBL14887 Ki = 10.3 nM 7.99
CHEMBL15100 Ki = 13.2 nM 7.88
CHEMBL275670 Ki = 17.2 nM 7.76
CHEMBL278891 Ki = 23.6 nM 7.63
CHEMBL280264 Ki = 28.3 nM 7.55
CHEMBL274012 Ki = 62.6 nM 7.20
CHEMBL278889 Ki = 70.8 nM 7.15
CHEMBL2370199 Ki = 1280.0 nM 5.89
CHEMBL2370207 Ki = 2140.0 nM 5.67