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Assay Detail

CHEMBL864530

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

Binding
Displacement of [3H]DAMGO from recombinant human mu opioid receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Syntheses, biological evaluation, and molecular modeling of 18F-labeled 4-anilidopiperidines as mu-opioid receptor imaging agents.
Henriksen G, Platzer S, Marton J, Hauser A, Berthele A, Schwaiger M, Marinelli L, Lavecchia A, Novellino E, Wester HJ.
J Med Chem (2005) 48 : 7720 -7732
PubMed 16302812 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 9.22 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2311157 [11C]-CARFENTANIL 1.0 1 10.15
CHEMBL200456 1 9.89
CHEMBL196960 1 9.89
CHEMBL371710 1 9.13
CHEMBL200392 1 8.92
CHEMBL197479 1 8.68
CHEMBL371268 1 7.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2311157 [11C]-CARFENTANIL Ki = 0.07 nM 10.15
CHEMBL200456 Ki = 0.13 nM 9.89
CHEMBL196960 Ki = 0.13 nM 9.89
CHEMBL371710 Ki = 0.74 nM 9.13
CHEMBL200392 Ki = 1.2 nM 8.92
CHEMBL197479 Ki = 2.1 nM 8.68
CHEMBL371268 Ki = 13.5 nM 7.87