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Assay Detail

CHEMBL5144871

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

Binding
Displacement of [3H]-DPDPE from recombinant human DOR expressed in CHO cell membranes measured after 2 hrs by microbeta scintillation counting method
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Morphinan derivatives with an oxabicyclo[3.2.1]octane structure as dual agonists toward δ and κ opioid receptors.
Uenohara Y, Tsumura S, Hirayama S, Higashi E, Watanabe Y, Gouda H, Nagase H, Fujii H.
Bioorg Med Chem (2022) 53 : 116552 -116552
PubMed 34894610 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.06 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5178511 1 9.28
CHEMBL5186730 1 8.78
CHEMBL5175717 1 8.30
CHEMBL5200218 1 8.29
CHEMBL5170301 1 8.29
CHEMBL5208385 1 8.25
CHEMBL5185996 1 7.71
CHEMBL5200992 1 7.69
CHEMBL5200050 1 7.63
CHEMBL485583 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5178511 Ki = 0.522 nM 9.28
CHEMBL5186730 Ki = 1.67 nM 8.78
CHEMBL5175717 Ki = 4.98 nM 8.30
CHEMBL5200218 Ki = 5.18 nM 8.29
CHEMBL5170301 Ki = 5.14 nM 8.29
CHEMBL5208385 Ki = 5.68 nM 8.25
CHEMBL5185996 Ki = 19.5 nM 7.71
CHEMBL5200992 Ki = 20.5 nM 7.69
CHEMBL5200050 Ki = 23.2 nM 7.63
CHEMBL485583 Ki = 408.0 nM 6.39