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Assay Detail

CHEMBL989030

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

Binding
Inhibition of human ERG channel in HEK293 cells by voltage-clamp method
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

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
IC50 20 5.52 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL523204 1 6.52
CHEMBL492449 1 6.42
CHEMBL492448 1 6.33
CHEMBL495073 1 6.23
CHEMBL495074 1 6.19
CHEMBL494265 1 6.18
CHEMBL492447 1 6.17
CHEMBL494275 1 6.12
CHEMBL494472 1 5.74
CHEMBL493454 1 5.19
CHEMBL494462 1 5.10
CHEMBL523507 1 4.74
CHEMBL494479 1 4.70
CHEMBL494274 1 4.32
CHEMBL495094 1 4.22
CHEMBL494480 ADL-5859 2.0 1 4.11
CHEMBL494266 1 -
CHEMBL495278 1 -
CHEMBL25230 1 -
CHEMBL13470 SNC-80 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL523204 IC50 = 303.0 nM 6.52
CHEMBL492449 IC50 = 379.0 nM 6.42
CHEMBL492448 IC50 = 462.0 nM 6.33
CHEMBL495073 IC50 = 585.0 nM 6.23
CHEMBL495074 IC50 = 643.0 nM 6.19
CHEMBL494265 IC50 = 663.0 nM 6.18
CHEMBL492447 IC50 = 680.0 nM 6.17
CHEMBL494275 IC50 = 766.0 nM 6.12
CHEMBL494472 IC50 = 1814.0 nM 5.74
CHEMBL493454 IC50 = 6450.0 nM 5.19
CHEMBL494462 IC50 = 7900.0 nM 5.10
CHEMBL523507 IC50 = 18310.0 nM 4.74
CHEMBL494479 IC50 = 19750.0 nM 4.70
CHEMBL494274 IC50 = 47440.0 nM 4.32
CHEMBL495094 IC50 = 60000.0 nM 4.22
CHEMBL494480 ADL-5859 IC50 = 78000.0 nM 4.11
CHEMBL494266 IC50 > 100000.0 nM -
CHEMBL495278 IC50 < 100.0 nM -
CHEMBL25230 IC50 - -
CHEMBL13470 SNC-80 IC50 - -