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Assay Detail

CHEMBL1217375

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
18
Total Activities
18
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

Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
Balboni G, Marzola E, Sasaki Y, Ambo A, Marczak ED, Lazarus LH, Salvadori S.
Bioorg Med Chem (2010) 18 : 6024 -6030
PubMed 20637637 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.77 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL109390 1 9.30
CHEMBL1213989 1 8.78
CHEMBL1213991 1 8.39
CHEMBL442577 1 7.27
CHEMBL1213987 1 7.26
CHEMBL1213988 1 7.17
CHEMBL1213990 1 6.81
CHEMBL1213938 1 6.65
CHEMBL1214117 1 6.29
CHEMBL1214050 1 6.24
CHEMBL1214118 1 6.22
CHEMBL296603 DELTORPHINE II 1 6.20
CHEMBL1213939 1 6.17
CHEMBL1213992 1 5.99
CHEMBL1212952 1 5.91
CHEMBL1214119 1 5.84
CHEMBL1214048 1 5.78
CHEMBL1214049 1 5.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL109390 Ki = 0.5 nM 9.30
CHEMBL1213989 Ki = 1.68 nM 8.78
CHEMBL1213991 Ki = 4.05 nM 8.39
CHEMBL442577 Ki = 53.9 nM 7.27
CHEMBL1213987 Ki = 54.5 nM 7.26
CHEMBL1213988 Ki = 66.9 nM 7.17
CHEMBL1213990 Ki = 154.3 nM 6.81
CHEMBL1213938 Ki = 225.1 nM 6.65
CHEMBL1214117 Ki = 511.4 nM 6.29
CHEMBL1214050 Ki = 573.3 nM 6.24
CHEMBL1214118 Ki = 596.4 nM 6.22
CHEMBL296603 DELTORPHINE II Ki = 638.0 nM 6.20
CHEMBL1213939 Ki = 683.9 nM 6.17
CHEMBL1213992 Ki = 1029.0 nM 5.99
CHEMBL1212952 Ki = 1234.0 nM 5.91
CHEMBL1214119 Ki = 1451.0 nM 5.84
CHEMBL1214048 Ki = 1649.0 nM 5.78
CHEMBL1214049 Ki = 2435.0 nM 5.61