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Assay Detail

CHEMBL750421

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]-p-DPDPE human cloned receptors.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

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 8.00 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13470 SNC-80 1 8.89
CHEMBL98800 1 8.30
CHEMBL101316 1 8.12
CHEMBL431276 1 8.10
CHEMBL102150 1 7.99
CHEMBL430675 1 7.89
CHEMBL316845 1 7.75
CHEMBL101231 1 7.58
CHEMBL98691 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13470 SNC-80 IC50 = 1.3 nM 8.89
CHEMBL98800 IC50 = 5.0 nM 8.30
CHEMBL101316 IC50 = 7.5 nM 8.12
CHEMBL431276 IC50 = 8.0 nM 8.10
CHEMBL102150 IC50 = 10.2 nM 7.99
CHEMBL430675 IC50 = 13.0 nM 7.89
CHEMBL316845 IC50 = 18.0 nM 7.75
CHEMBL101231 IC50 = 26.6 nM 7.58
CHEMBL98691 IC50 = 38.0 nM 7.42