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Assay Detail

CHEMBL759233

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

Binding
Opioid receptor mu 1 binding affinity by displacement of radioligand [3H][DAla,MePhe,Gly-ol]enkephalin (DAGO) from rat brain membrane synaptosomes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.
Tomatis R, Marastoni M, Balboni G, Guerrini R, Capasso A, Sorrentino L, Santagada V, Caliendo G, Lazarus LH, Salvadori S.
J Med Chem (1997) 40 : 2948 -2952
PubMed 9288177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.04 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278789 DERMORPHIN 1 9.55
CHEMBL1790778 1 9.54
CHEMBL2369626 1 9.34
CHEMBL317956 DELTORPHIN C 1 6.83
CHEMBL2370328 1 6.24
CHEMBL1790779 1 6.20
CHEMBL2370331 1 5.82
CHEMBL2370329 1 5.77
CHEMBL2370332 1 5.70
CHEMBL2370333 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278789 DERMORPHIN Ki = 0.28 nM 9.55
CHEMBL1790778 Ki = 0.29 nM 9.54
CHEMBL2369626 Ki = 0.46 nM 9.34
CHEMBL317956 DELTORPHIN C Ki = 147.0 nM 6.83
CHEMBL2370328 Ki = 578.9 nM 6.24
CHEMBL1790779 Ki = 634.9 nM 6.20
CHEMBL2370331 Ki = 1520.0 nM 5.82
CHEMBL2370329 Ki = 1700.0 nM 5.77
CHEMBL2370332 Ki = 1993.0 nM 5.70
CHEMBL2370333 Ki = 4400.0 nM 5.36