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Assay Detail

CHEMBL1003109

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
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
Balboni G, Fiorini S, Baldisserotto A, Trapella C, Sasaki Y, Ambo A, Marczak ED, Lazarus LH, Salvadori S.
J Med Chem (2008) 51 : 5109 -5117
PubMed 18680274 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.10 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL501451 1 9.80
CHEMBL458631 1 9.80
CHEMBL109390 1 9.30
CHEMBL500937 1 8.76
CHEMBL450263 1 8.23
CHEMBL498799 1 8.13
CHEMBL501202 1 7.97
CHEMBL499099 1 7.93
CHEMBL444197 1 7.79
CHEMBL502302 1 7.35
CHEMBL442577 1 7.27
CHEMBL450566 1 6.51
CHEMBL448360 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL501451 Ki = 0.16 nM 9.80
CHEMBL458631 Ki = 0.16 nM 9.80
CHEMBL109390 Ki = 0.5 nM 9.30
CHEMBL500937 Ki = 1.75 nM 8.76
CHEMBL450263 Ki = 5.93 nM 8.23
CHEMBL498799 Ki = 7.49 nM 8.13
CHEMBL501202 Ki = 10.8 nM 7.97
CHEMBL499099 Ki = 11.8 nM 7.93
CHEMBL444197 Ki = 16.1 nM 7.79
CHEMBL502302 Ki = 45.0 nM 7.35
CHEMBL442577 Ki = 53.9 nM 7.27
CHEMBL450566 Ki = 309.4 nM 6.51
CHEMBL448360 Ki = 364.3 nM 6.44