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Assay Detail

CHEMBL2188280

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes
14
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The effect of Pro(2) modifications on the structural and pharmacological properties of endomorphin-2.
Borics A, Mallareddy JR, Timári I, Kövér KE, Keresztes A, Tóth G.
J Med Chem (2012) 55 : 8418 -8428
PubMed 22957923 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 7 - -
Ki 7 7.51 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178089 2 8.89
CHEMBL333357 ENDOMORPHIN 2 2 8.85
CHEMBL2178087 2 8.59
CHEMBL1253632 2 7.57
CHEMBL2178090 2 7.36
CHEMBL2178088 2 5.67
CHEMBL2178086 2 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178089 Ki = 1.3 nM 8.89
CHEMBL333357 ENDOMORPHIN 2 Ki = 1.4 nM 8.85
CHEMBL2178087 Ki = 2.6 nM 8.59
CHEMBL1253632 Ki = 27.0 nM 7.57
CHEMBL2178090 Ki = 44.0 nM 7.36
CHEMBL2178088 Ki = 2158.0 nM 5.67
CHEMBL2178086 Ki = 2299.0 nM 5.64
CHEMBL2178086 Activity - -
CHEMBL2178087 Activity - -
CHEMBL2178088 Activity - -
CHEMBL2178089 Activity - -
CHEMBL1253632 Activity - -
CHEMBL2178090 Activity - -
CHEMBL333357 ENDOMORPHIN 2 Activity - -