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Assay Detail

CHEMBL867593

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

Binding
Displacement of [3H]deltorphin-II from delta opioid receptor in rat brain synaptosomal membranes
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 Expert

Target

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

Publication

Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
Li T, Fujita Y, Shiotani K, Miyazaki A, Tsuda Y, Ambo A, Sasaki Y, Jinsmaa Y, Marczak E, Bryant SD, Salvadori S, Lazarus LH, Okada Y.
J Med Chem (2005) 48 : 8035 -8044
PubMed 16335927 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 9.84 10.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL571492 1 10.66
CHEMBL370399 1 10.22
CHEMBL370398 1 10.04
CHEMBL198800 1 10.02
CHEMBL196774 1 9.97
CHEMBL370197 1 9.91
CHEMBL197185 1 9.89
CHEMBL381874 1 9.81
CHEMBL198646 1 9.80
CHEMBL200890 1 9.79
CHEMBL261905 1 9.54
CHEMBL373668 1 9.49
CHEMBL373192 1 8.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL571492 Ki = 0.022 nM 10.66
CHEMBL370399 Ki = 0.06 nM 10.22
CHEMBL370398 Ki = 0.092 nM 10.04
CHEMBL198800 Ki = 0.095 nM 10.02
CHEMBL196774 Ki = 0.107 nM 9.97
CHEMBL370197 Ki = 0.124 nM 9.91
CHEMBL197185 Ki = 0.129 nM 9.89
CHEMBL381874 Ki = 0.155 nM 9.81
CHEMBL198646 Ki = 0.16 nM 9.80
CHEMBL200890 Ki = 0.163 nM 9.79
CHEMBL261905 Ki = 0.287 nM 9.54
CHEMBL373668 Ki = 0.323 nM 9.49
CHEMBL373192 Ki = 1.53 nM 8.81