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Assay Detail

CHEMBL871072

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane
11
Total Activities
11
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

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

Publication

Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
Balboni G, Onnis V, Congiu C, Zotti M, Sasaki Y, Ambo A, Bryant SD, Jinsmaa Y, Lazarus LH, Trapella C, Salvadori S.
J Med Chem (2006) 49 : 5610 -5617
PubMed 16942034 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.84 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3143820 1 9.89
CHEMBL3143819 1 9.82
CHEMBL3143821 1 9.80
CHEMBL3143818 1 9.43
CHEMBL2028971 1 9.20
CHEMBL2028972 1 9.03
CHEMBL2028970 1 8.83
CHEMBL2028969 1 8.39
CHEMBL2028967 1 8.36
CHEMBL2028968 1 8.26
CHEMBL2371927 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3143820 Ki = 0.13 nM 9.89
CHEMBL3143819 Ki = 0.15 nM 9.82
CHEMBL3143821 Ki = 0.16 nM 9.80
CHEMBL3143818 Ki = 0.37 nM 9.43
CHEMBL2028971 Ki = 0.63 nM 9.20
CHEMBL2028972 Ki = 0.93 nM 9.03
CHEMBL2028970 Ki = 1.47 nM 8.83
CHEMBL2028969 Ki = 4.05 nM 8.39
CHEMBL2028967 Ki = 4.41 nM 8.36
CHEMBL2028968 Ki = 5.5 nM 8.26
CHEMBL2371927 Ki = 529.0 nM 6.28