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Assay Detail

CHEMBL751055

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

Binding
Evaluated for its affinity towards Opioid receptor mu 1 in rat forebrain by displacing the radioligand [3H]sufentanil.
2
Total Activities
2
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

Dermorphin sequence with high -afinity by fixing the phe sidechain to trans at 1
Tourwe D, Verschueren K, Van Binst G, Davis P, Porreca F, Hruby V
Bioorg Med Chem Lett (1992) 2 : 1305 -1308
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.29 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278789 DERMORPHIN 1 8.62
CHEMBL25465 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278789 DERMORPHIN IC50 = 2.4 nM 8.62
CHEMBL25465 IC50 = 11.0 nM 7.96