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Assay Detail

CHEMBL1024697

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

Binding
Displacement of [3H]DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cell membrane by liquid scintillation counting
7
Total Activities
4
Compounds Tested
2
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

The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Yamamoto T, Nair P, Jacobsen NE, Davis P, Ma SW, Navratilova E, Moye S, Lai J, Yamamura HI, Vanderah TW, Porreca F, Hruby VJ.
J Med Chem (2008) 51 : 6334 -6347
PubMed 18821747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.21 8.85
IC50 3 7.63 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200199 BIPHALIN 1 8.85
CHEMBL448998 2 8.74
CHEMBL507340 2 7.80
CHEMBL389652 2 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200199 BIPHALIN Ki = 1.4 nM 8.85
CHEMBL448998 Ki = 1.8 nM 8.74
CHEMBL448998 IC50 = 3.981 nM 8.40
CHEMBL507340 Ki = 16.0 nM 7.80
CHEMBL389652 Ki = 36.0 nM 7.44
CHEMBL507340 IC50 = 39.81 nM 7.40
CHEMBL389652 IC50 = 79.43 nM 7.10