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Assay Detail

CHEMBL754284

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

Binding
Binding affinity for Opioid receptor delta 1 by the inhibition of binding of [3H]DADAL in rat brain membranes.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Brain membranes
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Probes for narcotic receptor-mediated phenomena. 25. Synthesis and evaluation of N-alkyl-substituted (alpha-piperazinylbenzyl)benzamides as novel, highly selective delta opioid receptor agonists.
Katsura Y, Zhang X, Homma K, Rice KC, Calderon SN, Rothman RB, Yamamura HI, Davis P, Flippen-Anderson JL, Xu H, Becketts K, Foltz EJ, Porreca F.
J Med Chem (1997) 40 : 2936 -2947
PubMed 9288176 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.71 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431276 1 8.38
CHEMBL316845 1 8.32
CHEMBL102150 1 8.18
CHEMBL98800 1 8.15
CHEMBL101316 1 7.88
CHEMBL101231 1 7.74
CHEMBL330644 1 7.46
CHEMBL98644 1 6.75
CHEMBL319790 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431276 IC50 = 4.2 nM 8.38
CHEMBL316845 IC50 = 4.8 nM 8.32
CHEMBL102150 IC50 = 6.6 nM 8.18
CHEMBL98800 IC50 = 7.1 nM 8.15
CHEMBL101316 IC50 = 13.1 nM 7.88
CHEMBL101231 IC50 = 18.1 nM 7.74
CHEMBL330644 IC50 = 34.5 nM 7.46
CHEMBL98644 IC50 = 176.0 nM 6.75
CHEMBL319790 IC50 = 281.0 nM 6.55