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Assay Detail

CHEMBL754180

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Binding
Binding affinity was determined towards Opioid receptor delta 1 using [3H]naltrindole as radioligand
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.
Wentland MP, Sun X, Ye Y, Lou R, Bidlack JM.
Bioorg Med Chem Lett (2003) 13 : 1911 -1914
PubMed 12749896 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.16 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56585 CYCLAZOCINE 2.0 1 8.96
CHEMBL279968 ETHYLKETOCYCLAZOCINE 1 8.47
CHEMBL58646 1 8.08
CHEMBL57628 1 8.01
CHEMBL60869 1 8.01
CHEMBL19019 NALTREXONE 4.0 1 7.96
CHEMBL56246 1 7.43
CHEMBL299709 1 7.28
CHEMBL56695 1 6.96
CHEMBL298590 1 6.38
CHEMBL59314 1 6.06
CHEMBL56357 1 5.77
CHEMBL56208 1 5.62
CHEMBL293485 1 5.21
CHEMBL299027 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56585 CYCLAZOCINE Ki = 1.1 nM 8.96
CHEMBL279968 ETHYLKETOCYCLAZOCINE Ki = 3.4 nM 8.47
CHEMBL58646 Ki = 8.3 nM 8.08
CHEMBL57628 Ki = 9.8 nM 8.01
CHEMBL60869 Ki = 9.8 nM 8.01
CHEMBL19019 NALTREXONE Ki = 11.0 nM 7.96
CHEMBL56246 Ki = 37.0 nM 7.43
CHEMBL299709 Ki = 52.0 nM 7.28
CHEMBL56695 Ki = 110.0 nM 6.96
CHEMBL298590 Ki = 420.0 nM 6.38
CHEMBL59314 Ki = 880.0 nM 6.06
CHEMBL56357 Ki = 1700.0 nM 5.77
CHEMBL56208 Ki = 2400.0 nM 5.62
CHEMBL293485 Ki = 6200.0 nM 5.21
CHEMBL299027 Ki > 10000.0 nM -