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Assay Detail

CHEMBL989028

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Functional
Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 20 7.28 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25230 1 9.40
CHEMBL494479 1 8.85
CHEMBL13470 SNC-80 1 8.00
CHEMBL494462 1 7.72
CHEMBL494480 ADL-5859 2.0 1 7.70
CHEMBL494265 1 7.09
CHEMBL494275 1 7.05
CHEMBL495094 1 6.85
CHEMBL495073 1 6.72
CHEMBL495278 1 6.70
CHEMBL495074 1 6.66
CHEMBL494266 1 6.66
CHEMBL492447 1 6.42
CHEMBL492448 1 6.09
CHEMBL523204 1 -
CHEMBL493454 1 -
CHEMBL494274 1 -
CHEMBL494472 1 -
CHEMBL492449 1 -
CHEMBL523507 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25230 EC50 = 0.4 nM 9.40
CHEMBL494479 EC50 = 1.4 nM 8.85
CHEMBL13470 SNC-80 EC50 = 10.0 nM 8.00
CHEMBL494462 EC50 = 19.0 nM 7.72
CHEMBL494480 ADL-5859 EC50 = 20.0 nM 7.70
CHEMBL494265 EC50 = 81.0 nM 7.09
CHEMBL494275 EC50 = 89.0 nM 7.05
CHEMBL495094 EC50 = 140.0 nM 6.85
CHEMBL495073 EC50 = 190.0 nM 6.72
CHEMBL495278 EC50 = 200.0 nM 6.70
CHEMBL495074 EC50 = 220.0 nM 6.66
CHEMBL494266 EC50 = 220.0 nM 6.66
CHEMBL492447 EC50 = 380.0 nM 6.42
CHEMBL492448 EC50 = 810.0 nM 6.09
CHEMBL523204 EC50 - -
CHEMBL493454 EC50 - -
CHEMBL494274 EC50 - -
CHEMBL494472 EC50 - -
CHEMBL492449 EC50 - -
CHEMBL523507 EC50 - -