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Assay Detail

CHEMBL4124270

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

Functional
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Chemical space screening around Phe3 in opioid peptides: Modulating µ versus δ agonism by Suzuki-Miyaura cross-couplings.
Willemse T, Eiselt E, Hollanders K, Schepens W, van Vlijmen HWT, Chung NN, Blais V, Holleran B, Longpré JM, Schiller PW, Maes BUW, Sarret P, Gendron L, Ballet S.
Bioorg Med Chem Lett (2018) 28 : 2320 -2323
PubMed 29853330 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 8.15 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26575 DELTORPHIN 1 10.00
CHEMBL4129679 1 8.95
CHEMBL4126050 1 8.62
CHEMBL4128530 1 8.36
CHEMBL4126470 1 8.31
CHEMBL4129901 1 8.24
CHEMBL4126102 1 8.15
CHEMBL4126322 1 7.71
CHEMBL4128945 1 7.57
CHEMBL4129689 1 7.31
CHEMBL38874 DAMGO 1 7.31
CHEMBL4129753 1 7.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26575 DELTORPHIN EC50 = 0.1 nM 10.00
CHEMBL4129679 EC50 = 1.13 nM 8.95
CHEMBL4126050 EC50 = 2.4 nM 8.62
CHEMBL4128530 EC50 = 4.4 nM 8.36
CHEMBL4126470 EC50 = 4.9 nM 8.31
CHEMBL4129901 EC50 = 5.8 nM 8.24
CHEMBL4126102 EC50 = 7.0 nM 8.15
CHEMBL4126322 EC50 = 19.4 nM 7.71
CHEMBL4128945 EC50 = 26.8 nM 7.57
CHEMBL4129689 EC50 = 49.0 nM 7.31
CHEMBL38874 DAMGO EC50 = 49.0 nM 7.31
CHEMBL4129753 EC50 = 56.0 nM 7.25