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Assay Detail

CHEMBL4685299

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

Binding
Displacement of [3H]Ile5'6-deltorphin II from DOR in Wistar rat brain membranes measured after 45 mins by scintillation counting method
13
Total Activities
13
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

Synthesis, biochemical, pharmacological characterization and in silico profile modelling of highly potent opioid orvinol and thevinol derivatives.
Szűcs E,Marton J,Szabó Z,Hosztafi S,Kékesi G,Tuboly G,Bánki L,Horváth G,Szabó PT,Tömböly C,Varga ZK,Benyhe S,Ötvös F
Eur J Med Chem (2020) 191 : 112145 -112145
PubMed 32092588 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.96 8.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4746512 1 8.83
CHEMBL4776706 1 8.73
CHEMBL4751305 1 8.69
CHEMBL4754079 1 8.68
CHEMBL4745764 1 8.62
CHEMBL4753839 1 8.61
CHEMBL4762529 1 8.11
CHEMBL4761619 1 7.80
CHEMBL4758814 1 7.58
CHEMBL4764372 1 7.56
CHEMBL4752367 1 7.44
CHEMBL4758369 1 7.43
CHEMBL4787652 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4746512 Ki = 1.49 nM 8.83
CHEMBL4776706 Ki = 1.85 nM 8.73
CHEMBL4751305 Ki = 2.06 nM 8.69
CHEMBL4754079 Ki = 2.11 nM 8.68
CHEMBL4745764 Ki = 2.41 nM 8.62
CHEMBL4753839 Ki = 2.44 nM 8.61
CHEMBL4762529 Ki = 7.73 nM 8.11
CHEMBL4761619 Ki = 15.72 nM 7.80
CHEMBL4758814 Ki = 26.12 nM 7.58
CHEMBL4764372 Ki = 27.53 nM 7.56
CHEMBL4752367 Ki = 36.56 nM 7.44
CHEMBL4758369 Ki = 37.37 nM 7.43
CHEMBL4787652 Ki = 3906.3 nM 5.41