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Assay Detail

CHEMBL3611625

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Functional
Agonist activity at rat mu opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assay
20
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of tripeptide-derived multifunctional ligands possessing delta/mu opioid receptor agonist and neurokinin 1 receptor antagonist activities.
Nair P, Yamamoto T, Cowell S, Kulkarni V, Moye S, Navratilova E, Davis P, Ma SW, Vanderah TW, Lai J, Porreca F, Hruby VJ.
Bioorg Med Chem Lett (2015) 25 : 3716 -3720
PubMed 26212775 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.71 8.80
Emax 10 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3609620 2 8.80
CHEMBL3609621 2 8.28
CHEMBL3608939 2 8.26
CHEMBL3609618 2 8.15
CHEMBL3609617 2 7.64
CHEMBL3608938 2 7.60
CHEMBL3609615 2 7.39
CHEMBL3608937 2 7.23
CHEMBL3609616 2 7.00
CHEMBL3609619 2 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3609620 EC50 = 1.6 nM 8.80
CHEMBL3609621 EC50 = 5.2 nM 8.28
CHEMBL3608939 EC50 = 5.5 nM 8.26
CHEMBL3609618 EC50 = 7.1 nM 8.15
CHEMBL3609617 EC50 = 23.0 nM 7.64
CHEMBL3608938 EC50 = 25.0 nM 7.60
CHEMBL3609615 EC50 = 41.0 nM 7.39
CHEMBL3608937 EC50 = 59.0 nM 7.23
CHEMBL3609616 EC50 = 100.0 nM 7.00
CHEMBL3609619 EC50 = 170.0 nM 6.77
CHEMBL3608937 Emax = 70.0 % -
CHEMBL3608938 Emax = 38.0 % -
CHEMBL3608939 Emax = 58.0 % -
CHEMBL3609615 Emax = 16.0 % -
CHEMBL3609616 Emax = 14.0 % -
CHEMBL3609617 Emax = 34.0 % -
CHEMBL3609618 Emax = 58.0 % -
CHEMBL3609619 Emax = 26.0 % -
CHEMBL3609620 Emax = 49.0 % -
CHEMBL3609621 Emax = 50.0 % -