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Assay Detail

CHEMBL3826757

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

Binding
Displacement of [3H]DAMGO from mu-type opioid receptor in rat brain membranes incubated for 2 hrs
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

[Dmt(1)]DALDA analogues modified with tyrosine analogues at position 1.
Cai Y, Lu D, Chen Z, Ding Y, Chung NN, Li T, Schiller PW.
Bioorg Med Chem Lett (2016) 26 : 3629 -3631
PubMed 27301366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 9.14 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2181202 1 9.85
CHEMBL3822676 1 9.44
CHEMBL3823054 1 9.34
CHEMBL3822822 1 9.06
CHEMBL60444 1 8.77
CHEMBL3822702 1 8.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2181202 Ki = 0.143 nM 9.85
CHEMBL3822676 Ki = 0.367 nM 9.44
CHEMBL3823054 Ki = 0.458 nM 9.34
CHEMBL3822822 Ki = 0.875 nM 9.06
CHEMBL60444 Ki = 1.69 nM 8.77
CHEMBL3822702 Ki = 4.29 nM 8.37