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Assay Detail

CHEMBL4124265

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

Binding
Displacement of [125I]-Deltorphin 2 from mouse Flag-tagged delta-opioid receptor expressed in HEK293 cell membranes after 60 mins by gamma counting
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Delta-type opioid receptor (CHEMBL3222)
Type SINGLE PROTEIN
Organism Mus musculus

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
IC50 22 7.00 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26575 DELTORPHIN 1 9.00
CHEMBL4129901 1 8.10
CHEMBL4129679 1 7.85
CHEMBL4126102 1 7.75
CHEMBL4126470 1 7.70
CHEMBL4127080 1 7.69
CHEMBL4126050 1 7.65
CHEMBL4128945 1 7.41
CHEMBL4125848 1 7.37
CHEMBL4128530 1 7.23
CHEMBL4127485 1 7.15
CHEMBL4126249 1 6.78
CHEMBL4127226 1 6.57
CHEMBL4128463 1 6.51
CHEMBL4127702 1 6.46
CHEMBL4127547 1 6.36
CHEMBL4126322 1 6.23
CHEMBL4128313 1 6.22
CHEMBL4129689 1 6.20
CHEMBL4129753 1 6.16
CHEMBL4129548 1 5.85
CHEMBL38874 DAMGO 1 5.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26575 DELTORPHIN IC50 = 1.0 nM 9.00
CHEMBL4129901 IC50 = 8.0 nM 8.10
CHEMBL4129679 IC50 = 14.0 nM 7.85
CHEMBL4126102 IC50 = 18.0 nM 7.75
CHEMBL4126470 IC50 = 19.8 nM 7.70
CHEMBL4127080 IC50 = 20.25 nM 7.69
CHEMBL4126050 IC50 = 22.6 nM 7.65
CHEMBL4128945 IC50 = 39.2 nM 7.41
CHEMBL4125848 IC50 = 42.3 nM 7.37
CHEMBL4128530 IC50 = 59.4 nM 7.23
CHEMBL4127485 IC50 = 70.2 nM 7.15
CHEMBL4126249 IC50 = 165.0 nM 6.78
CHEMBL4127226 IC50 = 268.8 nM 6.57
CHEMBL4128463 IC50 = 309.0 nM 6.51
CHEMBL4127702 IC50 = 346.0 nM 6.46
CHEMBL4127547 IC50 = 435.0 nM 6.36
CHEMBL4126322 IC50 = 585.0 nM 6.23
CHEMBL4128313 IC50 = 601.0 nM 6.22
CHEMBL4129689 IC50 = 625.0 nM 6.20
CHEMBL4129753 IC50 = 687.0 nM 6.16
CHEMBL4129548 IC50 = 1415.0 nM 5.85
CHEMBL38874 DAMGO IC50 = 1533.0 nM 5.81