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Assay Detail

CHEMBL5236041

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

Binding
Agonist activity at mouse MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 60 mins by scintillation spectroscopy analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type CHO
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL2858)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Oxidative Metabolism as a Modulator of Kratom's Biological Actions.
Chakraborty S, Uprety R, Slocum ST, Irie T, Le Rouzic V, Li X, Wilson LL, Scouller B, Alder AF, Kruegel AC, Ansonoff M, Varadi A, Eans SO, Hunkele A, Allaoa A, Kalra S, Xu J, Pan YX, Pintar J, Kivell BM, Pasternak GW, Cameron MD, McLaughlin JP, Sames D, Majumdar S.
J Med Chem (2021) 64 : 16553 -16572
PubMed 34783240 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 5.80 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5276728 1 7.17
CHEMBL292521 1 6.37
CHEMBL5287921 1 5.24
CHEMBL4859858 1 5.21
CHEMBL4848517 1 5.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5276728 EC50 = 67.5 nM 7.17
CHEMBL292521 EC50 = 422.4 nM 6.37
CHEMBL5287921 EC50 = 5778.0 nM 5.24
CHEMBL4859858 EC50 = 6225.7 nM 5.21
CHEMBL4848517 EC50 = 9384.0 nM 5.03