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Assay Detail

CHEMBL753958

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

Binding
Affinity against Opioid receptor mu 1 was determined by measuring the inhibition of [3H]DAMGO binding to rat forebrain membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.
Choi H, Murray TF, DeLander GE, Schmidt WK, Aldrich JV.
J Med Chem (1997) 40 : 2733 -2739
PubMed 9276018 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.99 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL384584 1 9.62
CHEMBL406893 1 8.41
CHEMBL442323 1 8.02
CHEMBL406338 1 7.96
CHEMBL268818 1 7.51
CHEMBL266782 1 7.50
CHEMBL267215 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL384584 Ki = 0.24 nM 9.62
CHEMBL406893 Ki = 3.9 nM 8.41
CHEMBL442323 Ki = 9.6 nM 8.02
CHEMBL406338 Ki = 10.9 nM 7.96
CHEMBL268818 Ki = 31.1 nM 7.51
CHEMBL266782 Ki = 31.7 nM 7.50
CHEMBL267215 Ki = 128.0 nM 6.89