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Assay Detail

CHEMBL753667

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Binding
Binding affinity determined on Opioid receptor delta 1 in Guinea pig brain membranes using radioligand [3H]DADLE
4
Total Activities
4
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 Autocuration

Target

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

Publication

Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
Thomas JB, Fall MJ, Cooper JB, Rothman RB, Mascarella SW, Xu H, Partilla JS, Dersch CM, McCullough KB, Cantrell BE, Zimmerman DM, Carroll FI.
J Med Chem (1998) 41 : 5188 -5197
PubMed 9857089 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.96 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573214 NORBINALTORPHIMINE 1 7.37
CHEMBL19019 NALTREXONE 4.0 1 7.02
CHEMBL150052 1 6.49
CHEMBL10986 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573214 NORBINALTORPHIMINE Ki = 42.9 nM 7.37
CHEMBL19019 NALTREXONE Ki = 94.9 nM 7.02
CHEMBL150052 Ki = 322.0 nM 6.49
CHEMBL10986 Ki > 5700.0 nM -