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Assay Detail

CHEMBL955070

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
19
Total Activities
19
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

Syntheses of novel high affinity ligands for opioid receptors.
Wentland MP, Lou R, Lu Q, Bu Y, Denhardt C, Jin J, Ganorkar R, VanAlstine MA, Guo C, Cohen DJ, Bidlack JM.
Bioorg Med Chem Lett (2009) 19 : 2289 -2294
PubMed 19282177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.61 10.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL469815 1 10.60
CHEMBL567175 NALTRINDOLE 1 9.85
CHEMBL511795 1 9.52
CHEMBL471243 1 8.59
CHEMBL511645 1 8.41
CHEMBL470005 1 8.38
CHEMBL471048 1 8.08
CHEMBL398707 HYDROMORPHONE 4.0 1 7.42
CHEMBL19019 NALTREXONE 4.0 1 7.22
CHEMBL512150 1 7.11
CHEMBL511816 1 7.10
CHEMBL513762 1 6.82
CHEMBL471049 1 6.58
CHEMBL511302 1 6.55
CHEMBL56695 1 6.26
CHEMBL895 NALBUPHINE 4.0 1 6.24
CHEMBL511621 1 6.20
CHEMBL470617 NALTREXONE METHIODIDE 1 6.05
CHEMBL511461 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL469815 Ki = 0.025 nM 10.60
CHEMBL567175 NALTRINDOLE Ki = 0.14 nM 9.85
CHEMBL511795 Ki = 0.3 nM 9.52
CHEMBL471243 Ki = 2.6 nM 8.59
CHEMBL511645 Ki = 3.9 nM 8.41
CHEMBL470005 Ki = 4.2 nM 8.38
CHEMBL471048 Ki = 8.3 nM 8.08
CHEMBL398707 HYDROMORPHONE Ki = 38.0 nM 7.42
CHEMBL19019 NALTREXONE Ki = 60.0 nM 7.22
CHEMBL512150 Ki = 78.0 nM 7.11
CHEMBL511816 Ki = 79.0 nM 7.10
CHEMBL513762 Ki = 150.0 nM 6.82
CHEMBL471049 Ki = 260.0 nM 6.58
CHEMBL511302 Ki = 280.0 nM 6.55
CHEMBL56695 Ki = 550.0 nM 6.26
CHEMBL895 NALBUPHINE Ki = 580.0 nM 6.24
CHEMBL511621 Ki = 630.0 nM 6.20
CHEMBL470617 NALTREXONE METHIODIDE Ki = 900.0 nM 6.05
CHEMBL511461 Ki > 10000.0 nM -