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Assay Detail

CHEMBL754334

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

Binding
Inhibitory activity against Opioid receptor delta 1 in chinese Hamster Ovary (CHO) cell membranes was determined using [3H]naltrindole radioligand
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
Neumeyer JL, Zhang A, Xiong W, Gu XH, Hilbert JE, Knapp BI, Negus SS, Mello NK, Bidlack JM.
J Med Chem (2003) 46 : 5162 -5170
PubMed 14613319 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.36 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49269 CYCLORPHAN 1 8.72
CHEMBL413512 1 8.42
CHEMBL592 LEVORPHANOL 4.0 1 8.38
CHEMBL147511 1 8.38
CHEMBL301160 BUTORPHAN 1 8.23
CHEMBL146756 1 8.03
CHEMBL433697 1 8.03
CHEMBL150061 1 7.80
CHEMBL346436 1 7.68
CHEMBL405131 1 7.62
CHEMBL358104 1 7.50
CHEMBL357334 1 7.36
CHEMBL346885 1 7.10
CHEMBL424328 1 7.09
CHEMBL356889 1 6.43
CHEMBL149074 1 6.40
CHEMBL424327 1 6.22
CHEMBL348023 1 6.14
CHEMBL435084 1 6.04
CHEMBL151872 1 5.60
CHEMBL318859 ENADOLINE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49269 CYCLORPHAN Ki = 1.9 nM 8.72
CHEMBL413512 Ki = 3.8 nM 8.42
CHEMBL592 LEVORPHANOL Ki = 4.2 nM 8.38
CHEMBL147511 Ki = 4.2 nM 8.38
CHEMBL301160 BUTORPHAN Ki = 5.9 nM 8.23
CHEMBL146756 Ki = 9.4 nM 8.03
CHEMBL433697 Ki = 9.4 nM 8.03
CHEMBL150061 Ki = 16.0 nM 7.80
CHEMBL346436 Ki = 21.0 nM 7.68
CHEMBL405131 Ki = 24.0 nM 7.62
CHEMBL358104 Ki = 32.0 nM 7.50
CHEMBL357334 Ki = 44.0 nM 7.36
CHEMBL346885 Ki = 80.0 nM 7.10
CHEMBL424328 Ki = 82.0 nM 7.09
CHEMBL356889 Ki = 370.0 nM 6.43
CHEMBL149074 Ki = 400.0 nM 6.40
CHEMBL424327 Ki = 600.0 nM 6.22
CHEMBL348023 Ki = 730.0 nM 6.14
CHEMBL435084 Ki = 920.0 nM 6.04
CHEMBL151872 Ki = 2500.0 nM 5.60
CHEMBL318859 ENADOLINE Ki > 1000.0 nM -