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Assay Detail

CHEMBL758127

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

Binding
Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 from mouse brain membranes.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

7-spirobenzocyclohexyl derivatives of naltrexone, oxymorphone, and hydromorphone as selective opioid receptor ligands.
Fang X, Larson DL, Portoghese PS.
J Med Chem (1997) 40 : 3064 -3070
PubMed 9301669 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.25 9.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101694 1 9.42
CHEMBL105081 1 9.14
CHEMBL610293 1 8.82
CHEMBL104159 1 8.55
CHEMBL399708 SPIROINDANYLOXYMORPHONE 1 7.85
CHEMBL104179 1 7.75
CHEMBL318598 1 7.55
CHEMBL318361 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101694 Ki = 0.38 nM 9.42
CHEMBL105081 Ki = 0.72 nM 9.14
CHEMBL610293 Ki = 1.5 nM 8.82
CHEMBL104159 Ki = 2.8 nM 8.55
CHEMBL399708 SPIROINDANYLOXYMORPHONE Ki = 14.0 nM 7.85
CHEMBL104179 Ki = 18.0 nM 7.75
CHEMBL318598 Ki = 28.0 nM 7.55
CHEMBL318361 Ki = 119.0 nM 6.92