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Assay Detail

CHEMBL689695

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

Functional
In vitro inhibition of contractions in the electrically stimulated guinea pig ileum.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 1 — Organism
Curated By Expert

Target

Cavia porcellus (CHEMBL369)
Type ORGANISM
Organism Cavia porcellus

Publication

Synthesis and pharmacological activity of partially modified retro-inverso dermorphin tetrapeptides.
Salvadori S, Marastoni M, Balboni G, Sarto GP, Tomatis R.
J Med Chem (1985) 28 : 769 -774
PubMed 4009598 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.82 9.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL164983 1 9.51
CHEMBL351419 1 9.30
CHEMBL166038 1 9.23
CHEMBL278789 DERMORPHIN 1 8.85
CHEMBL165745 1 8.69
CHEMBL166081 1 8.69
CHEMBL351202 1 8.67
CHEMBL348764 1 8.53
CHEMBL165319 1 8.35
CHEMBL165551 1 7.74
CHEMBL165654 1 7.72
CHEMBL351087 1 7.60
CHEMBL350348 1 7.51
CHEMBL351861 1 7.41
CHEMBL349816 1 7.34
CHEMBL70 MORPHINE 4.0 1 7.23
CHEMBL164786 1 6.97
CHEMBL424181 1 6.72
CHEMBL350979 1 6.62
CHEMBL348845 1 6.50
CHEMBL166084 1 6.48
CHEMBL434680 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL164983 IC50 = 0.31 nM 9.51
CHEMBL351419 IC50 = 0.5 nM 9.30
CHEMBL166038 IC50 = 0.59 nM 9.23
CHEMBL278789 DERMORPHIN IC50 = 1.41 nM 8.85
CHEMBL165745 IC50 = 2.05 nM 8.69
CHEMBL166081 IC50 = 2.05 nM 8.69
CHEMBL351202 IC50 = 2.12 nM 8.67
CHEMBL348764 IC50 = 2.97 nM 8.53
CHEMBL165319 IC50 = 4.45 nM 8.35
CHEMBL165551 IC50 = 18.2 nM 7.74
CHEMBL165654 IC50 = 19.2 nM 7.72
CHEMBL351087 IC50 = 25.2 nM 7.60
CHEMBL350348 IC50 = 31.2 nM 7.51
CHEMBL351861 IC50 = 39.2 nM 7.41
CHEMBL349816 IC50 = 45.2 nM 7.34
CHEMBL70 MORPHINE IC50 = 58.6 nM 7.23
CHEMBL164786 IC50 = 108.0 nM 6.97
CHEMBL424181 IC50 = 191.2 nM 6.72
CHEMBL350979 IC50 = 242.5 nM 6.62
CHEMBL348845 IC50 = 320.0 nM 6.50
CHEMBL166084 IC50 = 330.0 nM 6.48
CHEMBL434680 IC50 = 380.1 nM 6.42