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Assay Detail

CHEMBL3367575

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

Binding
Displacement of [3H]DSLET from delta opioid receptor in rat brain membranes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

'Carba'-carfentanil (trans isomer): a μ opioid receptor (MOR) partial agonist with a distinct binding mode.
Weltrowska G, Lemieux C, Chung NN, Guo JJ, Wilkes BC, Schiller PW.
Bioorg Med Chem (2014) 22 : 4581 -4586
PubMed 25129170 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.82 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290429 CARFENTANIL 2.0 1 8.48
CHEMBL70 MORPHINE 4.0 1 7.08
CHEMBL3325854 1 6.96
CHEMBL1091995 1 4.75
CHEMBL3325853 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290429 CARFENTANIL Ki = 3.3 nM 8.48
CHEMBL70 MORPHINE Ki = 82.5 nM 7.08
CHEMBL3325854 Ki = 110.0 nM 6.96
CHEMBL1091995 Ki = 17700.0 nM 4.75
CHEMBL3325853 Ki > 5000.0 nM -