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Assay Detail

CHEMBL755015

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

Functional
In vitro opioid inhibitory activity against in guinea pig ileum
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Opioid receptors; mu/kappa/delta (CHEMBL2095181)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and opioid activity of dermorphin tetrapeptides bearing D-methionine S-oxide at position 2.
Salvadori S, Marastoni M, Balboni G, Sarto GP, Tomatis R.
J Med Chem (1986) 29 : 889 -894
PubMed 2872334 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.74 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278789 DERMORPHIN 1 8.85
CHEMBL369354 1 8.57
CHEMBL296148 1 8.53
CHEMBL171459 1 7.87
CHEMBL171887 1 7.78
CHEMBL171014 1 7.68
CHEMBL171089 1 7.66
CHEMBL434111 1 7.59
CHEMBL170817 1 7.45
CHEMBL355446 1 7.34
CHEMBL70 MORPHINE 4.0 1 7.19
CHEMBL435267 1 7.14
CHEMBL171028 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278789 DERMORPHIN IC50 = 1.41 nM 8.85
CHEMBL369354 IC50 = 2.68 nM 8.57
CHEMBL296148 IC50 = 2.97 nM 8.53
CHEMBL171459 IC50 = 13.6 nM 7.87
CHEMBL171887 IC50 = 16.7 nM 7.78
CHEMBL171014 IC50 = 21.0 nM 7.68
CHEMBL171089 IC50 = 22.0 nM 7.66
CHEMBL434111 IC50 = 25.5 nM 7.59
CHEMBL170817 IC50 = 35.6 nM 7.45
CHEMBL355446 IC50 = 45.2 nM 7.34
CHEMBL70 MORPHINE IC50 = 65.0 nM 7.19
CHEMBL435267 IC50 = 72.1 nM 7.14
CHEMBL171028 IC50 = 97.6 nM 7.01