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Assay Detail

CHEMBL839554

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

Binding
Inhibition of [3H]-DAMGO binding to recombinant human Opioid receptor mu 1
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.
MacDougall JM, Zhang XD, Polgar WE, Khroyan TV, Toll L, Cashman JR.
Bioorg Med Chem Lett (2005) 15 : 1583 -1586
PubMed 15745801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.40 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL366917 1 9.30
CHEMBL362202 DEPROTECTED COGENER OF M6G 1 8.46
CHEMBL359644 1 8.27
CHEMBL359534 1 8.06
CHEMBL1330 MORPHINE GLUCURONIDE 2.0 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL366917 Ki = 0.5 nM 9.30
CHEMBL362202 DEPROTECTED COGENER OF M6G Ki = 3.5 nM 8.46
CHEMBL359644 Ki = 5.4 nM 8.27
CHEMBL359534 Ki = 8.7 nM 8.06
CHEMBL1330 MORPHINE GLUCURONIDE Ki = 12.9 nM 7.89