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Assay Detail

CHEMBL755202

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

Functional
Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor delta 1 in Guinea pig Caudate stimulated by SNC80
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
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 7.72 8.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL150052 1 8.83
CHEMBL573214 NORBINALTORPHIMINE 1 7.99
CHEMBL19019 NALTREXONE 4.0 1 7.71
CHEMBL10986 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL150052 Ki = 1.48 nM 8.83
CHEMBL573214 NORBINALTORPHIMINE Ki = 10.14 nM 7.99
CHEMBL19019 NALTREXONE Ki = 19.3 nM 7.71
CHEMBL10986 Ki = 450.0 nM 6.35