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Assay Detail

CHEMBL753334

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

Functional
Inhibitory activity against forskolin-stimulated cAMP production in chinese hamster ovary cells expressing Opioid receptor delta 1
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Delta-type opioid receptor (CHEMBL269)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Syntheses of potent Leu-enkephalin analogs possessing beta-hydroxy-alpha,alpha-disubstituted-alpha-amino acid and their characterization to opioid receptors.
Horikawa M, Shigeri Y, Yumoto N, Yoshikawa S, Nakajima T, Ohfune Y.
Bioorg Med Chem Lett (1998) 8 : 2027 -2032
PubMed 9873480 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.34 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2114469 1 11.00
CHEMBL60936 1 10.15
CHEMBL2114470 1 8.70
CHEMBL31421 1 8.40
CHEMBL2115492 1 8.00
CHEMBL2373084 1 6.85
CHEMBL62688 1 5.30
CHEMBL2115493 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2114469 IC50 = 0.01 nM 11.00
CHEMBL60936 IC50 = 0.071 nM 10.15
CHEMBL2114470 IC50 = 2.0 nM 8.70
CHEMBL31421 IC50 = 4.0 nM 8.40
CHEMBL2115492 IC50 = 10.0 nM 8.00
CHEMBL2373084 IC50 = 140.0 nM 6.85
CHEMBL62688 IC50 = 5000.0 nM 5.30
CHEMBL2115493 IC50 = 0.005 nM -