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Assay Detail

CHEMBL4380091

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Functional
Agonist activity at human recombinant mu opioid receptor expressed in CHO cells assessed as stimulation of cAMP accumulation incubated for 10 mins by HTRF assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
Obeng S, Kamble SH, Reeves ME, Restrepo LF, Patel A, Behnke M, Chear NJ, Ramanathan S, Sharma A, León F, Hiranita T, Avery BA, McMahon LR, McCurdy CR.
J Med Chem (2020) 63 : 433 -439
PubMed 31834797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.35 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61630 1 8.12
CHEMBL4546925 1 7.41
CHEMBL299031 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61630 EC50 = 7.6 nM 8.12
CHEMBL4546925 EC50 = 39.2 nM 7.41
CHEMBL299031 EC50 = 307.5 nM 6.51