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Assay Detail

CHEMBL745618

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

Functional
Inhibitory concentration against electrically evoked contractions of guinea pig ileum longitudinal muscle-myenteric plexus
8
Total Activities
8
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 Expert

Target

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

Publication

Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors.
Bartosz-Bechowski H, Davis P, Zalewska T, Slaninova J, Porreca F, Yamamura HI, Hruby VJ.
J Med Chem (1994) 37 : 146 -150
PubMed 8289188 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.71 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2372327 1 7.50
CHEMBL2372328 1 7.44
CHEMBL339320 1 7.08
CHEMBL2372314 1 6.92
CHEMBL2372329 1 6.68
CHEMBL2372310 1 6.19
CHEMBL31421 1 5.14
CHEMBL317956 DELTORPHIN C 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2372327 IC50 = 32.0 nM 7.50
CHEMBL2372328 IC50 = 36.0 nM 7.44
CHEMBL339320 IC50 = 82.7 nM 7.08
CHEMBL2372314 IC50 = 120.0 nM 6.92
CHEMBL2372329 IC50 = 210.0 nM 6.68
CHEMBL2372310 IC50 = 640.0 nM 6.19
CHEMBL31421 IC50 = 7300.0 nM 5.14
CHEMBL317956 DELTORPHIN C IC50 > 1500.0 nM -