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Assay Detail

CHEMBL756059

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

Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors.
Pagé D, Naismith A, Schmidt R, Coupal M, Labarre M, Gosselin M, Bellemare D, Payza K, Brown W.
J Med Chem (2001) 44 : 2387 -2390
PubMed 11448220 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 8.72 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL421520 1 9.49
CHEMBL310842 1 9.19
CHEMBL80463 1 9.12
CHEMBL77001 1 9.04
CHEMBL76089 1 9.01
CHEMBL80823 1 8.82
CHEMBL75802 1 8.77
CHEMBL76573 1 8.55
CHEMBL317956 DELTORPHIN C 1 8.33
CHEMBL309783 1 8.24
CHEMBL76846 1 7.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL421520 EC50 = 0.32 nM 9.49
CHEMBL310842 EC50 = 0.65 nM 9.19
CHEMBL80463 EC50 = 0.75 nM 9.12
CHEMBL77001 EC50 = 0.92 nM 9.04
CHEMBL76089 EC50 = 0.97 nM 9.01
CHEMBL80823 EC50 = 1.5 nM 8.82
CHEMBL75802 EC50 = 1.7 nM 8.77
CHEMBL76573 EC50 = 2.8 nM 8.55
CHEMBL317956 DELTORPHIN C EC50 = 4.71 nM 8.33
CHEMBL309783 EC50 = 5.7 nM 8.24
CHEMBL76846 EC50 = 49.4 nM 7.31