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Assay Detail

CHEMBL989026

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

Binding
Displacement of [3H]diprenorphine from human delta opioid receptor in CHO cells
22
Total Activities
22
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

Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
Le Bourdonnec B, Windh RT, Ajello CW, Leister LK, Gu M, Chu GH, Tuthill PA, Barker WM, Koblish M, Wiant DD, Graczyk TM, Belanger S, Cassel JA, Feschenko MS, Brogdon BL, Smith SA, Christ DD, Derelanko MJ, Kutz S, Little PJ, DeHaven RN, DeHaven-Hudkins DL, Dolle RE.
J Med Chem (2008) 51 : 5893 -5896
PubMed 18788723 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.62 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25230 1 9.49
CHEMBL494479 1 9.37
CHEMBL494480 ADL-5859 2.0 1 9.08
CHEMBL13470 SNC-80 1 8.92
CHEMBL495094 1 8.82
CHEMBL494462 1 8.74
CHEMBL494275 1 8.46
CHEMBL494265 1 8.03
CHEMBL494266 1 7.96
CHEMBL495278 1 7.75
CHEMBL495073 1 7.24
CHEMBL495074 1 7.23
CHEMBL494472 1 7.17
CHEMBL492447 1 7.15
CHEMBL492448 1 7.14
CHEMBL492449 1 6.82
CHEMBL493687 1 6.80
CHEMBL523204 1 6.48
CHEMBL523507 1 6.44
CHEMBL493454 1 6.32
CHEMBL522004 1 6.30
CHEMBL494274 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25230 Ki = 0.32 nM 9.49
CHEMBL494479 Ki = 0.43 nM 9.37
CHEMBL494480 ADL-5859 Ki = 0.84 nM 9.08
CHEMBL13470 SNC-80 Ki = 1.2 nM 8.92
CHEMBL495094 Ki = 1.5 nM 8.82
CHEMBL494462 Ki = 1.8 nM 8.74
CHEMBL494275 Ki = 3.5 nM 8.46
CHEMBL494265 Ki = 9.3 nM 8.03
CHEMBL494266 Ki = 11.0 nM 7.96
CHEMBL495278 Ki = 18.0 nM 7.75
CHEMBL495073 Ki = 58.0 nM 7.24
CHEMBL495074 Ki = 59.0 nM 7.23
CHEMBL494472 Ki = 68.0 nM 7.17
CHEMBL492447 Ki = 71.0 nM 7.15
CHEMBL492448 Ki = 72.0 nM 7.14
CHEMBL492449 Ki = 150.0 nM 6.82
CHEMBL493687 Ki = 160.0 nM 6.80
CHEMBL523204 Ki = 330.0 nM 6.48
CHEMBL523507 Ki = 360.0 nM 6.44
CHEMBL493454 Ki = 480.0 nM 6.32
CHEMBL522004 Ki = 500.0 nM 6.30
CHEMBL494274 Ki = 1300.0 nM 5.89