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Assay Detail

CHEMBL751918

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

Functional
Effective concentration as delta agonist potency using [35S]GTP-gamma-S binding assay.
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues.
Wei ZY, Brown W, Takasaki B, Plobeck N, Delorme D, Zhou F, Yang H, Jones P, Gawell L, Gagnon H, Schmidt R, Yue SY, Walpole C, Payza K, St-Onge S, Labarre M, Godbout C, Jakob A, Butterworth J, Kamassah A, Morin PE, Projean D, Ducharme J, Roberts E.
J Med Chem (2000) 43 : 3895 -3905
PubMed 11052794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 7.79 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129034 1 9.05
CHEMBL339898 1 8.50
CHEMBL13470 SNC-80 1 8.44
CHEMBL339457 1 8.34
CHEMBL278078 1 8.23
CHEMBL415521 1 8.14
CHEMBL340131 1 8.07
CHEMBL126857 1 8.05
CHEMBL129300 1 7.97
CHEMBL339922 1 7.92
CHEMBL423694 1 7.86
CHEMBL126141 1 7.85
CHEMBL126370 1 7.80
CHEMBL127495 1 7.69
CHEMBL129693 1 7.63
CHEMBL127007 1 7.59
CHEMBL126255 1 7.55
CHEMBL129315 1 7.51
CHEMBL338980 1 7.44
CHEMBL127788 1 7.37
CHEMBL127802 1 7.34
CHEMBL126946 1 7.01
CHEMBL126382 1 6.92
CHEMBL126842 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129034 EC50 = 0.9 nM 9.05
CHEMBL339898 EC50 = 3.18 nM 8.50
CHEMBL13470 SNC-80 EC50 = 3.67 nM 8.44
CHEMBL339457 EC50 = 4.6 nM 8.34
CHEMBL278078 EC50 = 5.9 nM 8.23
CHEMBL415521 EC50 = 7.2 nM 8.14
CHEMBL340131 EC50 = 8.6 nM 8.07
CHEMBL126857 EC50 = 8.96 nM 8.05
CHEMBL129300 EC50 = 10.6 nM 7.97
CHEMBL339922 EC50 = 12.1 nM 7.92
CHEMBL423694 EC50 = 13.7 nM 7.86
CHEMBL126141 EC50 = 14.1 nM 7.85
CHEMBL126370 EC50 = 15.9 nM 7.80
CHEMBL127495 EC50 = 20.5 nM 7.69
CHEMBL129693 EC50 = 23.4 nM 7.63
CHEMBL127007 EC50 = 25.5 nM 7.59
CHEMBL126255 EC50 = 28.3 nM 7.55
CHEMBL129315 EC50 = 30.6 nM 7.51
CHEMBL338980 EC50 = 36.5 nM 7.44
CHEMBL127788 EC50 = 42.3 nM 7.37
CHEMBL127802 EC50 = 46.0 nM 7.34
CHEMBL126946 EC50 = 98.1 nM 7.01
CHEMBL126382 EC50 = 121.0 nM 6.92
CHEMBL126842 EC50 = 161.0 nM 6.79