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Assay Detail

CHEMBL757106

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

Binding
Binding affinity against Opioid receptor mu 1 using [3H][D-Ala2, MePhe4, Gly-ol5]-enkephalin as radioligand
11
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL2858)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.
Dondio G, Ronzoni S, Eggleston DS, Artico M, Petrillo P, Petrone G, Visentin L, Farina C, Vecchietti V, Clarke GD.
J Med Chem (1997) 40 : 3192 -3198
PubMed 9379438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.51 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL324236 1 7.85
CHEMBL567175 NALTRINDOLE 1 7.82
CHEMBL108076 1 7.03
CHEMBL100729 3 6.89
CHEMBL401093 OXYMORPHINDOLE 1 6.18
CHEMBL13470 SNC-80 1 5.89
CHEMBL107670 3 5.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL324236 Ki = 14.1 nM 7.85
CHEMBL567175 NALTRINDOLE Ki = 15.0 nM 7.82
CHEMBL108076 Ki = 93.0 nM 7.03
CHEMBL100729 Ki = 129.0 nM 6.89
CHEMBL100729 Ki = 407.0 nM 6.39
CHEMBL401093 OXYMORPHINDOLE Ki = 661.0 nM 6.18
CHEMBL13470 SNC-80 Ki = 1300.0 nM 5.89
CHEMBL107670 Ki = 1631.0 nM 5.79
CHEMBL107670 Ki = 2093.0 nM 5.68
CHEMBL107670 Ki = 2618.0 nM 5.58
CHEMBL100729 Ki > 5000.0 nM -