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Assay Detail

CHEMBL749732

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

Binding
Inhibitory activity in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor mu 1 in chinese Hamster Ovary (CHO) cell membranes was determined
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
Neumeyer JL, Zhang A, Xiong W, Gu XH, Hilbert JE, Knapp BI, Negus SS, Mello NK, Bidlack JM.
J Med Chem (2003) 46 : 5162 -5170
PubMed 14613319 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 8.39 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49269 CYCLORPHAN 1 9.10
CHEMBL147511 1 8.89
CHEMBL146756 1 8.54
CHEMBL433697 1 8.13
CHEMBL357334 1 8.10
CHEMBL405131 1 8.00
CHEMBL346436 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49269 CYCLORPHAN EC50 = 0.8 nM 9.10
CHEMBL147511 EC50 = 1.3 nM 8.89
CHEMBL146756 EC50 = 2.9 nM 8.54
CHEMBL433697 EC50 = 7.4 nM 8.13
CHEMBL357334 EC50 = 8.0 nM 8.10
CHEMBL405131 EC50 = 10.0 nM 8.00
CHEMBL346436 EC50 = 11.0 nM 7.96