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Assay Detail

CHEMBL753852

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

Binding
Displacement of [3H]EK from Opioid receptor delta 1 in guinea pig brain membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors.
Portoghese PS, Larson DL, Sayre LM, Yim CB, Ronsisvalle G, Tam SW, Takemori AE.
J Med Chem (1986) 29 : 1855 -1861
PubMed 3020244 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.32 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3350130 1 8.31
CHEMBL3350137 1 8.19
CHEMBL3350138 1 8.11
CHEMBL3350129 1 7.92
CHEMBL3350128 1 7.58
CHEMBL610018 1 7.42
CHEMBL3350140 1 7.38
CHEMBL3350132 1 7.30
CHEMBL3350135 1 7.07
CHEMBL3350127 1 7.00
CHEMBL3350133 1 6.96
CHEMBL3350134 1 6.70
CHEMBL607319 1 6.32
CHEMBL3350139 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3350130 Ki = 4.9 nM 8.31
CHEMBL3350137 Ki = 6.4 nM 8.19
CHEMBL3350138 Ki = 7.8 nM 8.11
CHEMBL3350129 Ki = 12.0 nM 7.92
CHEMBL3350128 Ki = 26.0 nM 7.58
CHEMBL610018 Ki = 38.0 nM 7.42
CHEMBL3350140 Ki = 42.0 nM 7.38
CHEMBL3350132 Ki = 50.0 nM 7.30
CHEMBL3350135 Ki = 86.0 nM 7.07
CHEMBL3350127 Ki = 100.0 nM 7.00
CHEMBL3350133 Ki = 110.0 nM 6.96
CHEMBL3350134 Ki = 200.0 nM 6.70
CHEMBL607319 Ki = 480.0 nM 6.32
CHEMBL3350139 Ki = 700.0 nM 6.16