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Assay Detail

CHEMBL3863200

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

Binding
Displacement of [3H]DSLET from DOR in rat brain membrane measured after 2 hrs
10
Total Activities
10
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 Autocuration

Target

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

Publication

A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinity μ Opioid Receptor Antagonists.
Weltrowska G, Nguyen TM, Chung NN, Wood J, Ma X, Guo J, Wilkes BC, Ge Y, Laferrière A, Coderre TJ, Schiller PW.
J Med Chem (2016) 59 : 9243 -9254
PubMed 27676089 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.35 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3924888 1 9.09
CHEMBL3897031 1 8.81
CHEMBL3908315 1 8.42
CHEMBL3951723 1 7.82
CHEMBL3979449 1 7.78
CHEMBL507214 1 6.59
CHEMBL3976694 1 6.58
CHEMBL3904924 1 6.38
CHEMBL3944636 1 6.37
CHEMBL363142 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3924888 Ki = 0.807 nM 9.09
CHEMBL3897031 Ki = 1.53 nM 8.81
CHEMBL3908315 Ki = 3.84 nM 8.42
CHEMBL3951723 Ki = 15.0 nM 7.82
CHEMBL3979449 Ki = 16.7 nM 7.78
CHEMBL507214 Ki = 258.0 nM 6.59
CHEMBL3976694 Ki = 263.0 nM 6.58
CHEMBL3904924 Ki = 422.0 nM 6.38
CHEMBL3944636 Ki = 425.0 nM 6.37
CHEMBL363142 Ki = 2100.0 nM 5.68