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Assay Detail

CHEMBL2423366

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

Binding
Displacement of [3H]DPDPE from rat MOR expressed in HN9.10 cell membranes
8
Total Activities
8
Compounds Tested
1
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

Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities.
Nair P, Yamamoto T, Largent-Milnes TM, Cowell S, Kulkarni V, Moye S, Navratilova E, Davis P, Ma SW, Vanderah TW, Lai J, Porreca F, Hruby VJ.
Bioorg Med Chem Lett (2013) 23 : 4975 -4978
PubMed 23899615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.57 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2419544 1 9.54
CHEMBL2419543 1 7.82
CHEMBL2419541 1 7.64
CHEMBL2419542 1 7.48
CHEMBL2419539 1 7.20
CHEMBL2419540 1 7.12
CHEMBL2419538 1 6.96
CHEMBL2419537 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2419544 Ki = 0.29 nM 9.54
CHEMBL2419543 Ki = 15.0 nM 7.82
CHEMBL2419541 Ki = 23.0 nM 7.64
CHEMBL2419542 Ki = 33.0 nM 7.48
CHEMBL2419539 Ki = 63.0 nM 7.20
CHEMBL2419540 Ki = 76.0 nM 7.12
CHEMBL2419538 Ki = 110.0 nM 6.96
CHEMBL2419537 Ki = 150.0 nM 6.82