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Assay Detail

CHEMBL756222

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

Binding
Binding affinity against Opioid receptor delta 1 using [3H]DADLE as radioligand in guinea pig brain
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors.
Cappelli A, Anzini M, Vomero S, Menziani MC, De Benedetti PG, Sbacchi M, Clarke GD, Mennuni L.
J Med Chem (1996) 39 : 860 -872
PubMed 8632410 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.59 6.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127969 1 6.98
CHEMBL169703 TIFLUADOM 2.0 1 6.82
CHEMBL127463 1 6.56
CHEMBL127968 1 6.00
CHEMBL341529 1 -
CHEMBL124015 1 -
CHEMBL126282 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127969 Ki = 105.0 nM 6.98
CHEMBL169703 TIFLUADOM Ki = 153.0 nM 6.82
CHEMBL127463 Ki = 275.0 nM 6.56
CHEMBL127968 Ki = 1000.0 nM 6.00
CHEMBL341529 Ki > 300.0 nM -
CHEMBL124015 Ki > 1000.0 nM -
CHEMBL126282 Ki > 1000.0 nM -