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Assay Detail

CHEMBL900987

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Functional
Agonist activity at guinea pig mu-opioid receptor by GPI assay
10
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-opioid receptor (CHEMBL5430)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.
Lee YS, Petrov R, Park CK, Ma SW, Davis P, Lai J, Porreca F, Vardanyan R, Hruby VJ.
J Med Chem (2007) 50 : 5528 -5532
PubMed 17927164 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.17 8.07
Activity 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235109 1 8.07
CHEMBL235743 1 7.33
CHEMBL235107 1 7.33
CHEMBL392206 1 7.02
CHEMBL439026 1 6.92
CHEMBL235106 1 6.80
CHEMBL392207 1 6.70
CHEMBL216239 CARBOXYFENTANYL 1 -
CHEMBL392185 1 -
CHEMBL235108 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235109 IC50 = 8.5 nM 8.07
CHEMBL235743 IC50 = 47.0 nM 7.33
CHEMBL235107 IC50 = 47.0 nM 7.33
CHEMBL392206 IC50 = 95.0 nM 7.02
CHEMBL439026 IC50 = 120.0 nM 6.92
CHEMBL235106 IC50 = 160.0 nM 6.80
CHEMBL392207 IC50 = 200.0 nM 6.70
CHEMBL216239 CARBOXYFENTANYL Activity = - % -
CHEMBL392185 Activity = 15.0 % -
CHEMBL235108 Activity = 3.0 % -