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Assay Detail

CHEMBL842482

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

Binding
In vitro inhibitory activity against mu opioid receptor using guinea pig ileum (GPI) assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

A topochemical approach to explain morphiceptin bioactivity.
Yamazaki T, Ro S, Goodman M, Chung NN, Schiller PW.
J Med Chem (1993) 36 : 708 -719
PubMed 8384662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.57 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL283287 1 7.68
CHEMBL267708 1 7.54
CHEMBL2371360 1 7.51
CHEMBL2371359 1 6.96
CHEMBL2371339 1 6.77
CHEMBL362991 MORPHICEPTIN 1 6.26
CHEMBL2371340 1 6.25
CHEMBL2371336 1 5.58
CHEMBL2371361 1 4.57
CHEMBL2371337 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL283287 IC50 = 20.7 nM 7.68
CHEMBL267708 IC50 = 28.7 nM 7.54
CHEMBL2371360 IC50 = 30.6 nM 7.51
CHEMBL2371359 IC50 = 109.0 nM 6.96
CHEMBL2371339 IC50 = 170.0 nM 6.77
CHEMBL362991 MORPHICEPTIN IC50 = 552.0 nM 6.26
CHEMBL2371340 IC50 = 557.0 nM 6.25
CHEMBL2371336 IC50 = 2660.0 nM 5.58
CHEMBL2371361 IC50 = 26900.0 nM 4.57
CHEMBL2371337 IC50 > 100000.0 nM -