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Assay Detail

CHEMBL907181

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain homogenate
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
Rennison D, Moynihan H, Traynor JR, Lewis JW, Husbands SM.
J Med Chem (2006) 49 : 6104 -6110
PubMed 17004724 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 9.62 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267027 1 10.40
CHEMBL443311 1 9.89
CHEMBL217395 1 9.62
CHEMBL19019 NALTREXONE 4.0 1 9.40
CHEMBL384497 1 9.23
CHEMBL216251 1 9.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267027 Ki = 0.04 nM 10.40
CHEMBL443311 Ki = 0.13 nM 9.89
CHEMBL217395 Ki = 0.24 nM 9.62
CHEMBL19019 NALTREXONE Ki = 0.4 nM 9.40
CHEMBL384497 Ki = 0.59 nM 9.23
CHEMBL216251 Ki = 0.7 nM 9.15