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Assay Detail

CHEMBL792299

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

Functional
Binding of [3H]diprenorphine to rat brain membranes was evaluated and the dissociation constant (KD) was determined.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

N-(3-[18F]fluoropropyl)-N-nordiprenorphine: synthesis and characterization of a new agent for imaging opioid receptors with positron emission tomography.
Chesis PL, Hwang DR, Welch MJ.
J Med Chem (1990) 33 : 1482 -1490
PubMed 2158564 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 9.11 10.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2311186 1 10.33
CHEMBL281786 DIPRENORPHINE 2.0 1 9.00
CHEMBL80 NALOXONE 4.0 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2311186 Kd = 0.047 nM 10.33
CHEMBL281786 DIPRENORPHINE Kd = 1.0 nM 9.00
CHEMBL80 NALOXONE Kd = 10.0 nM 8.00