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Assay Detail

CHEMBL758066

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

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

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 6.70 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL355178 1 8.92
CHEMBL278789 DERMORPHIN 1 8.43
CHEMBL168110 1 7.35
CHEMBL317956 DELTORPHIN C 1 5.26
CHEMBL169860 1 5.17
CHEMBL169439 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL355178 IC50 = 1.21 nM 8.92
CHEMBL278789 DERMORPHIN IC50 = 3.74 nM 8.43
CHEMBL168110 IC50 = 44.4 nM 7.35
CHEMBL317956 DELTORPHIN C IC50 = 5437.0 nM 5.26
CHEMBL169860 IC50 = 6705.0 nM 5.17
CHEMBL169439 IC50 = 8214.0 nM 5.08