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Assay Detail

CHEMBL754251

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

Functional
In vitro biological activity by electrically induced smooth muscle contractions in mouse vas deferens (Opioid receptor delta 1); inhibitory concentration was evaluated
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Delta-type opioid receptor (CHEMBL3222)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.
Ambo A, Murase H, Niizuma H, Ouchi H, Yamamoto Y, Sasaki Y.
Bioorg Med Chem Lett (2002) 12 : 879 -881
PubMed 11958984 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.16 10.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL169860 1 10.66
CHEMBL317956 DELTORPHIN C 1 9.23
CHEMBL355178 1 8.34
CHEMBL278789 DERMORPHIN 1 7.46
CHEMBL169439 1 6.84
CHEMBL168110 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL169860 IC50 = 0.022 nM 10.66
CHEMBL317956 DELTORPHIN C IC50 = 0.582 nM 9.23
CHEMBL355178 IC50 = 4.62 nM 8.34
CHEMBL278789 DERMORPHIN IC50 = 34.4 nM 7.46
CHEMBL169439 IC50 = 145.0 nM 6.84
CHEMBL168110 IC50 = 358.0 nM 6.45