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Assay Detail

CHEMBL1799273

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

Binding
Displacement of [125I]-IBNalA from MOR-1 expressed in CHO cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Generation of novel radiolabeled opiates through site-selective iodination.
Majumdar S, Burgman M, Haselton N, Grinnell S, Ocampo J, Pasternak AR, Pasternak GW.
Bioorg Med Chem Lett (2011) 21 : 4001 -4004
PubMed 21621410 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.74 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38874 DAMGO 1 9.35
CHEMBL1254682 LEVALLORPHAN 4.0 1 8.77
CHEMBL80 NALOXONE 4.0 1 8.64
CHEMBL70 MORPHINE 4.0 1 8.60
CHEMBL19019 NALTREXONE 4.0 1 8.57
CHEMBL1795717 1 8.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38874 DAMGO Ki = 0.45 nM 9.35
CHEMBL1254682 LEVALLORPHAN Ki = 1.69 nM 8.77
CHEMBL80 NALOXONE Ki = 2.27 nM 8.64
CHEMBL70 MORPHINE Ki = 2.52 nM 8.60
CHEMBL19019 NALTREXONE Ki = 2.71 nM 8.57
CHEMBL1795717 Ki = 2.96 nM 8.53