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Assay Detail

CHEMBL758275

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

Functional
Inhibition of electrically evoked contraction of guinea pig ileum (myenteric plexus:longitudinal muscle preparation) by antagonist action at mu 1 opioid receptors
23
Total Activities
23
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

Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides.
Gacel G, Zajac JM, Delay-Goyet P, Daugé V, Roques BP.
J Med Chem (1988) 31 : 374 -383
PubMed 2828622 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.59 7.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38874 DAMGO 1 7.94
CHEMBL2370601 1 7.67
CHEMBL125060 1 7.19
CHEMBL70 MORPHINE 4.0 1 7.16
CHEMBL2370602 1 7.06
CHEMBL125564 1 7.00
CHEMBL2370600 1 6.96
CHEMBL338773 1 6.81
CHEMBL339020 1 6.70
CHEMBL123631 1 6.67
CHEMBL341480 1 6.65
CHEMBL419414 1 6.62
CHEMBL338307 1 6.59
CHEMBL127711 1 6.58
CHEMBL275050 1 6.49
CHEMBL341500 1 6.42
CHEMBL124283 1 6.39
CHEMBL127378 1 6.34
CHEMBL2370599 1 6.14
CHEMBL339002 1 5.73
CHEMBL31421 1 5.00
CHEMBL333064 1 4.85
CHEMBL14094 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38874 DAMGO IC50 = 11.5 nM 7.94
CHEMBL2370601 IC50 = 21.3 nM 7.67
CHEMBL125060 IC50 = 64.0 nM 7.19
CHEMBL70 MORPHINE IC50 = 70.0 nM 7.16
CHEMBL2370602 IC50 = 88.0 nM 7.06
CHEMBL125564 IC50 = 99.0 nM 7.00
CHEMBL2370600 IC50 = 111.0 nM 6.96
CHEMBL338773 IC50 = 154.0 nM 6.81
CHEMBL339020 IC50 = 200.0 nM 6.70
CHEMBL123631 IC50 = 216.0 nM 6.67
CHEMBL341480 IC50 = 224.0 nM 6.65
CHEMBL419414 IC50 = 237.0 nM 6.62
CHEMBL338307 IC50 = 257.0 nM 6.59
CHEMBL127711 IC50 = 260.0 nM 6.58
CHEMBL275050 IC50 = 323.0 nM 6.49
CHEMBL341500 IC50 = 379.0 nM 6.42
CHEMBL124283 IC50 = 406.0 nM 6.39
CHEMBL127378 IC50 = 460.0 nM 6.34
CHEMBL2370599 IC50 = 718.0 nM 6.14
CHEMBL339002 IC50 = 1850.0 nM 5.73
CHEMBL31421 IC50 = 10000.0 nM 5.00
CHEMBL333064 IC50 = 14000.0 nM 4.85
CHEMBL14094 IC50 >= 50000.0 nM -