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Assay Detail

CHEMBL1677801

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

Binding
Displacement of [3H][Ile5,6]deltorphin 2 from delta opioid receptor in Sprague-Dawley rat brain membrane by liquid scintillation counting
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 and pharmacological activities of 6-glycine substituted 14-phenylpropoxymorphinans, a novel class of opioids with high opioid receptor affinities and antinociceptive potencies.
Spetea M, Windisch P, Guo Y, Bileviciute-Ljungar I, Schütz J, Asim MF, Berzetei-Gurske IP, Riba P, Kiraly K, Fürst S, Al-Khrasani M, Schmidhammer H.
J Med Chem (2011) 54 : 980 -988
PubMed 21235243 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.62 9.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL514774 1 9.39
CHEMBL1672083 1 9.27
CHEMBL3216476 1 9.19
CHEMBL3216936 1 9.19
CHEMBL3216475 1 9.14
CHEMBL3216716 1 9.09
CHEMBL1672086 1 8.90
CHEMBL1672090 1 8.83
CHEMBL1672091 1 8.75
CHEMBL1672087 1 8.70
CHEMBL1672084 1 7.37
CHEMBL1672085 1 7.35
CHEMBL70 MORPHINE 4.0 1 6.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL514774 Ki = 0.41 nM 9.39
CHEMBL1672083 Ki = 0.54 nM 9.27
CHEMBL3216476 Ki = 0.64 nM 9.19
CHEMBL3216936 Ki = 0.65 nM 9.19
CHEMBL3216475 Ki = 0.73 nM 9.14
CHEMBL3216716 Ki = 0.81 nM 9.09
CHEMBL1672086 Ki = 1.26 nM 8.90
CHEMBL1672090 Ki = 1.49 nM 8.83
CHEMBL1672091 Ki = 1.77 nM 8.75
CHEMBL1672087 Ki = 2.02 nM 8.70
CHEMBL1672084 Ki = 43.2 nM 7.37
CHEMBL1672085 Ki = 44.8 nM 7.35
CHEMBL70 MORPHINE Ki = 113.0 nM 6.95