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Assay Detail

CHEMBL754476

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

Binding
Inhibition of radioligand [3H]DADLE binding to rat brain delta receptor
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

A marked change of receptor affinity of the 2-methyl-5-(3-hydroxyphenyl)morphans upon attachment of an (E)-8-benzylidene moiety: synthesis and evaluation of a new class of sigma receptor ligands.
Bertha CM, Mattson MV, Flippen-Anderson JL, Rothman RB, Xu H, Cha XY, Becketts K, Rice KC.
J Med Chem (1994) 37 : 3163 -3170
PubMed 7932540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.39 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38791 2 6.92
CHEMBL322468 1 6.62
CHEMBL2008608 1 6.57
CHEMBL2111686 1 6.30
CHEMBL3350264 1 6.13
CHEMBL2111684 1 5.70
CHEMBL110319 1 -
CHEMBL109160 1 -
CHEMBL2111685 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38791 Ki = 121.5 nM 6.92
CHEMBL322468 Ki = 240.4 nM 6.62
CHEMBL2008608 Ki = 271.0 nM 6.57
CHEMBL38791 Ki = 320.0 nM 6.50
CHEMBL2111686 Ki = 504.9 nM 6.30
CHEMBL3350264 Ki = 734.7 nM 6.13
CHEMBL2111684 Ki = 1989.0 nM 5.70
CHEMBL110319 Ki > 500.0 nM -
CHEMBL109160 Ki > 1000.0 nM -
CHEMBL2111685 Ki > 500.0 nM -