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Assay Detail

CHEMBL753746

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

Binding
Binding affinity towards Opioid receptor mu 1 using [3H]DAMGO as radioligand.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Enantiomers of diastereomeric cis-N-[1-(2-hydroxy-2-phenylethyl)- 3-methyl-4-piperidyl]-N-phenylpropanamides: synthesis, X-ray analysis, and biological activities.
Brine GA, Stark PA, Liu Y, Carroll FI, Singh P, Xu H, Rothman RB.
J Med Chem (1995) 38 : 1547 -1557
PubMed 7739013 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.67 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2373217 1 10.89
CHEMBL38685 1 10.70
CHEMBL596 FENTANYL 4.0 1 8.40
CHEMBL70 MORPHINE 4.0 1 8.09
CHEMBL2373216 1 7.78
CHEMBL290411 1 7.51
CHEMBL2373185 1 7.33
CHEMBL2373184 1 -
CHEMBL544473 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2373217 Ki = 0.013 nM 10.89
CHEMBL38685 Ki = 0.02 nM 10.70
CHEMBL596 FENTANYL Ki = 3.97 nM 8.40
CHEMBL70 MORPHINE Ki = 8.14 nM 8.09
CHEMBL2373216 Ki = 16.47 nM 7.78
CHEMBL290411 Ki = 30.6 nM 7.51
CHEMBL2373185 Ki = 47.07 nM 7.33
CHEMBL2373184 Ki = 0.005 nM -
CHEMBL544473 Ki = 0.0055 nM -