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Assay Detail

CHEMBL750418

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

Binding
Binding affinity on cloned opioid receptor delta 1 in human HEK293S cells using [125I]-[D-Ala2]-deltorphin II as radioligand.
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293S
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
IC50 27 8.39 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339898 1 9.20
CHEMBL339457 1 9.13
CHEMBL129300 1 9.07
CHEMBL415521 1 9.06
CHEMBL278078 1 9.01
CHEMBL126370 1 8.98
CHEMBL340131 1 8.96
CHEMBL129034 1 8.91
CHEMBL13470 SNC-80 1 8.88
CHEMBL423694 1 8.81
CHEMBL339922 1 8.69
CHEMBL129693 1 8.68
CHEMBL126141 1 8.68
CHEMBL126857 1 8.64
CHEMBL127495 1 8.59
CHEMBL129315 1 8.54
CHEMBL126255 1 8.52
CHEMBL127007 1 8.38
CHEMBL127802 1 8.19
CHEMBL126382 1 8.06
CHEMBL127788 1 8.03
CHEMBL338980 1 7.95
CHEMBL126946 1 7.82
CHEMBL126842 1 7.57
CHEMBL340476 1 7.45
CHEMBL126884 1 6.73
CHEMBL338089 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339898 IC50 = 0.63 nM 9.20
CHEMBL339457 IC50 = 0.74 nM 9.13
CHEMBL129300 IC50 = 0.86 nM 9.07
CHEMBL415521 IC50 = 0.87 nM 9.06
CHEMBL278078 IC50 = 0.97 nM 9.01
CHEMBL126370 IC50 = 1.04 nM 8.98
CHEMBL340131 IC50 = 1.1 nM 8.96
CHEMBL129034 IC50 = 1.23 nM 8.91
CHEMBL13470 SNC-80 IC50 = 1.31 nM 8.88
CHEMBL423694 IC50 = 1.56 nM 8.81
CHEMBL339922 IC50 = 2.04 nM 8.69
CHEMBL129693 IC50 = 2.09 nM 8.68
CHEMBL126141 IC50 = 2.09 nM 8.68
CHEMBL126857 IC50 = 2.31 nM 8.64
CHEMBL127495 IC50 = 2.57 nM 8.59
CHEMBL129315 IC50 = 2.85 nM 8.54
CHEMBL126255 IC50 = 3.0 nM 8.52
CHEMBL127007 IC50 = 4.17 nM 8.38
CHEMBL127802 IC50 = 6.53 nM 8.19
CHEMBL126382 IC50 = 8.77 nM 8.06
CHEMBL127788 IC50 = 9.35 nM 8.03
CHEMBL338980 IC50 = 11.3 nM 7.95
CHEMBL126946 IC50 = 15.0 nM 7.82
CHEMBL126842 IC50 = 27.0 nM 7.57
CHEMBL340476 IC50 = 35.5 nM 7.45
CHEMBL126884 IC50 = 187.0 nM 6.73
CHEMBL338089 IC50 = 736.0 nM 6.13