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Assay Detail

CHEMBL3614958

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

Binding
Displacement of [3H]DPDPE from DOR in mouse whole brain membranes without cerebellum
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Delta-type opioid receptor (CHEMBL3222)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
Nakajima R, Yamamoto N, Hirayama S, Iwai T, Saitoh A, Nagumo Y, Fujii H, Nagase H.
Bioorg Med Chem (2015) 23 : 6271 -6279
PubMed 26346669 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.35 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3613171 1 9.74
CHEMBL3613172 1 8.94
CHEMBL3613173 1 8.92
CHEMBL3613282 1 8.90
CHEMBL3613165 1 8.78
CHEMBL3613166 1 8.65
CHEMBL3613164 1 8.45
CHEMBL3613174 1 8.44
CHEMBL3613163 1 8.40
CHEMBL3613169 1 8.35
CHEMBL3613170 1 8.19
CHEMBL3613168 1 7.97
CHEMBL3613167 1 7.85
CHEMBL3613281 1 7.82
CHEMBL3613175 1 7.72
CHEMBL3613280 1 7.49
CHEMBL490665 NALFURAFINE HYDROCHLORIDE 4.0 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3613171 Ki = 0.182 nM 9.74
CHEMBL3613172 Ki = 1.15 nM 8.94
CHEMBL3613173 Ki = 1.19 nM 8.92
CHEMBL3613282 Ki = 1.27 nM 8.90
CHEMBL3613165 Ki = 1.66 nM 8.78
CHEMBL3613166 Ki = 2.23 nM 8.65
CHEMBL3613164 Ki = 3.52 nM 8.45
CHEMBL3613174 Ki = 3.65 nM 8.44
CHEMBL3613163 Ki = 3.98 nM 8.40
CHEMBL3613169 Ki = 4.5 nM 8.35
CHEMBL3613170 Ki = 6.46 nM 8.19
CHEMBL3613168 Ki = 10.7 nM 7.97
CHEMBL3613167 Ki = 14.2 nM 7.85
CHEMBL3613281 Ki = 15.0 nM 7.82
CHEMBL3613175 Ki = 19.1 nM 7.72
CHEMBL3613280 Ki = 32.4 nM 7.49
CHEMBL490665 NALFURAFINE HYDROCHLORIDE Ki = 51.3 nM 7.29