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Assay Detail

CHEMBL689696

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

Functional
In vitro inhibitory concentration against electrically induced twitches in guinea pig ileum
15
Total Activities
15
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

Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties.
Fujita Y, Tsuda Y, Li T, Motoyama T, Takahashi M, Shimizu Y, Yokoi T, Sasaki Y, Ambo A, Kita A, Jinsmaa Y, Bryant SD, Lazarus LH, Okada Y.
J Med Chem (2004) 47 : 3591 -3599
PubMed 15214786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.25 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL331325 1 10.15
CHEMBL334147 1 9.59
CHEMBL339417 1 9.31
CHEMBL433643 1 9.03
CHEMBL120758 1 8.63
CHEMBL332196 1 8.30
CHEMBL333357 ENDOMORPHIN 2 1 8.24
CHEMBL331255 1 8.21
CHEMBL327036 1 8.04
CHEMBL409907 1 7.93
CHEMBL118942 1 7.82
CHEMBL419591 1 7.66
CHEMBL120091 1 7.42
CHEMBL332371 1 7.14
CHEMBL333350 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL331325 IC50 = 0.07 nM 10.15
CHEMBL334147 IC50 = 0.26 nM 9.59
CHEMBL339417 IC50 = 0.49 nM 9.31
CHEMBL433643 IC50 = 0.94 nM 9.03
CHEMBL120758 IC50 = 2.33 nM 8.63
CHEMBL332196 IC50 = 5.03 nM 8.30
CHEMBL333357 ENDOMORPHIN 2 IC50 = 5.79 nM 8.24
CHEMBL331255 IC50 = 6.21 nM 8.21
CHEMBL327036 IC50 = 9.14 nM 8.04
CHEMBL409907 IC50 = 11.8 nM 7.93
CHEMBL118942 IC50 = 15.0 nM 7.82
CHEMBL419591 IC50 = 22.0 nM 7.66
CHEMBL120091 IC50 = 37.7 nM 7.42
CHEMBL332371 IC50 = 72.8 nM 7.14
CHEMBL333350 IC50 = 445.0 nM 6.35