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Assay Detail

CHEMBL753270

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

Binding
Binding affinity was determined on delta [3H]DPDPE site in rat brain synaptosomes by radioreceptor assay
17
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Synaptosomes
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors.
Salvadori S, Bryant SD, Bianchi C, Balboni G, Scaranari V, Attila M, Lazarus LH.
J Med Chem (1993) 36 : 3748 -3756
PubMed 8254604 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.27 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL124941 2 10.15
CHEMBL124435 1 9.70
CHEMBL317956 DELTORPHIN C 1 9.51
CHEMBL339456 1 9.21
CHEMBL125872 1 8.63
CHEMBL340909 1 8.54
CHEMBL263698 1 8.37
CHEMBL332416 1 8.31
CHEMBL125285 1 7.97
CHEMBL334299 1 7.47
CHEMBL125289 1 7.34
CHEMBL339683 1 7.34
CHEMBL121946 2 7.31
CHEMBL330991 1 7.04
CHEMBL122159 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL124941 Ki = 0.07 nM 10.15
CHEMBL124941 Ki = 0.12 nM 9.92
CHEMBL124435 Ki = 0.2 nM 9.70
CHEMBL317956 DELTORPHIN C Ki = 0.31 nM 9.51
CHEMBL339456 Ki = 0.61 nM 9.21
CHEMBL125872 Ki = 2.34 nM 8.63
CHEMBL340909 Ki = 2.85 nM 8.54
CHEMBL263698 Ki = 4.23 nM 8.37
CHEMBL332416 Ki = 4.84 nM 8.31
CHEMBL125285 Ki = 10.7 nM 7.97
CHEMBL334299 Ki = 34.0 nM 7.47
CHEMBL339683 Ki = 45.4 nM 7.34
CHEMBL125289 Ki = 45.5 nM 7.34
CHEMBL121946 Ki = 48.6 nM 7.31
CHEMBL121946 Ki = 69.1 nM 7.16
CHEMBL330991 Ki = 90.2 nM 7.04
CHEMBL122159 Ki = 284.0 nM 6.55