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Assay Detail

CHEMBL754435

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

Binding
Inhibition of [3H]naltrindole binding to opioid receptor delta 1 of Chinese hamster ovary membrane
14
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
Zhang A, Xiong W, Hilbert JE, DeVita EK, Bidlack JM, Neumeyer JL.
J Med Chem (2004) 47 : 1886 -1888
PubMed 15055988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.32 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59092 1 8.96
CHEMBL49269 CYCLORPHAN 1 8.72
CHEMBL592 LEVORPHANOL 4.0 1 8.38
CHEMBL301160 BUTORPHAN 1 8.23
CHEMBL242756 1 7.54
CHEMBL294168 1 7.50
CHEMBL301701 1 7.03
CHEMBL70 MORPHINE 4.0 1 6.85
CHEMBL1766021 2 6.72
CHEMBL390866 1 6.64
CHEMBL48241 1 6.58
CHEMBL56356 1 6.03
CHEMBL299713 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59092 Ki = 1.1 nM 8.96
CHEMBL49269 CYCLORPHAN Ki = 1.9 nM 8.72
CHEMBL592 LEVORPHANOL Ki = 4.2 nM 8.38
CHEMBL301160 BUTORPHAN Ki = 5.9 nM 8.23
CHEMBL242756 Ki = 29.0 nM 7.54
CHEMBL294168 Ki = 32.0 nM 7.50
CHEMBL301701 Ki = 93.0 nM 7.03
CHEMBL70 MORPHINE Ki = 140.0 nM 6.85
CHEMBL1766021 Ki = 190.0 nM 6.72
CHEMBL390866 Ki = 230.0 nM 6.64
CHEMBL48241 Ki = 260.0 nM 6.58
CHEMBL56356 Ki = 940.0 nM 6.03
CHEMBL1766021 Ki = 1100.0 nM 5.96
CHEMBL299713 Ki > 10000.0 nM -