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Assay Detail

CHEMBL1777019

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

Binding
Displacement of [3H]naltrindole from human delta-opioid receptor expressed in CHO cells after 3 hrs by scintillation counting
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors.
Zhang B, Zhang T, Sromek AW, Scrimale T, Bidlack JM, Neumeyer JL.
Bioorg Med Chem (2011) 19 : 2808 -2816
PubMed 21482470 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.75 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL147511 1 8.38
CHEMBL301160 BUTORPHAN 1 8.23
CHEMBL1774949 1 8.10
CHEMBL1774946 1 8.09
CHEMBL146756 1 8.03
CHEMBL33986 BUTORPHANOL 4.0 1 7.92
CHEMBL1774947 1 7.89
CHEMBL1773091 1 7.85
CHEMBL242756 1 7.54
CHEMBL1774950 1 7.46
CHEMBL80 NALOXONE 4.0 1 7.42
CHEMBL1774952 1 7.41
CHEMBL1774948 1 7.41
CHEMBL1774951 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL147511 Ki = 4.2 nM 8.38
CHEMBL301160 BUTORPHAN Ki = 5.9 nM 8.23
CHEMBL1774949 Ki = 8.0 nM 8.10
CHEMBL1774946 Ki = 8.1 nM 8.09
CHEMBL146756 Ki = 9.4 nM 8.03
CHEMBL33986 BUTORPHANOL Ki = 12.0 nM 7.92
CHEMBL1774947 Ki = 13.0 nM 7.89
CHEMBL1773091 Ki = 14.0 nM 7.85
CHEMBL242756 Ki = 29.0 nM 7.54
CHEMBL1774950 Ki = 35.0 nM 7.46
CHEMBL80 NALOXONE Ki = 38.0 nM 7.42
CHEMBL1774952 Ki = 39.0 nM 7.41
CHEMBL1774948 Ki = 39.0 nM 7.41
CHEMBL1774951 Ki = 170.0 nM 6.77