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Assay Detail

CHEMBL4399057

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

Binding
Displacement of [3H]DAMGO from human recombinant MOR expressed in CHO cell membranes incubated for 2 hrs by liquid scintillation counting method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Endomorphin-2 analogs containing modified tyrosines: Biological and theoretical investigation of the influence on conformation and pharmacological profile.
Wtorek K, Artali R, Piekielna-Ciesielska J, Koszuk J, Kluczyk A, Gentilucci L, Janecka A.
Eur J Med Chem (2019) 179 : 527 -536
PubMed 31276897 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.60 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4514319 1 9.59
CHEMBL331325 1 9.09
CHEMBL333357 ENDOMORPHIN 2 1 8.53
CHEMBL4475274 1 8.36
CHEMBL4466953 1 8.30
CHEMBL4527584 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4514319 Ki = 0.26 nM 9.59
CHEMBL331325 Ki = 0.81 nM 9.09
CHEMBL333357 ENDOMORPHIN 2 Ki = 2.95 nM 8.53
CHEMBL4475274 Ki = 4.38 nM 8.36
CHEMBL4466953 Ki = 4.98 nM 8.30
CHEMBL4527584 Ki = 18.91 nM 7.72