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Assay Detail

CHEMBL752187

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

Binding
Displacement of [3H]naloxone from Opioid receptor mu 1 in guinea pig brain membrane
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors.
Portoghese PS, Larson DL, Sayre LM, Yim CB, Ronsisvalle G, Tam SW, Takemori AE.
J Med Chem (1986) 29 : 1855 -1861
PubMed 3020244 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.92 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL610018 1 8.85
CHEMBL3350130 1 8.82
CHEMBL3350137 1 8.80
CHEMBL3350129 1 8.77
CHEMBL3350138 1 8.64
CHEMBL3350136 1 8.00
CHEMBL3350132 1 7.85
CHEMBL3350135 1 7.75
CHEMBL3350140 1 7.66
CHEMBL3350134 1 7.64
CHEMBL3350128 1 7.47
CHEMBL3350133 1 7.36
CHEMBL3350127 1 7.30
CHEMBL3350139 1 7.20
CHEMBL607319 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL610018 Ki = 1.4 nM 8.85
CHEMBL3350130 Ki = 1.5 nM 8.82
CHEMBL3350137 Ki = 1.6 nM 8.80
CHEMBL3350129 Ki = 1.7 nM 8.77
CHEMBL3350138 Ki = 2.3 nM 8.64
CHEMBL3350136 Ki = 10.0 nM 8.00
CHEMBL3350132 Ki = 14.0 nM 7.85
CHEMBL3350135 Ki = 18.0 nM 7.75
CHEMBL3350140 Ki = 22.0 nM 7.66
CHEMBL3350134 Ki = 23.0 nM 7.64
CHEMBL3350128 Ki = 34.0 nM 7.47
CHEMBL3350133 Ki = 44.0 nM 7.36
CHEMBL3350127 Ki = 50.0 nM 7.30
CHEMBL3350139 Ki = 63.0 nM 7.20
CHEMBL607319 Ki = 180.0 nM 6.75