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Assay Detail

CHEMBL5042903

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

Functional
Antagonist activity at mouse MOR expressed in CHO cells assessed as inhibition of DAMGO-induced calcium mobilization preincubated for 60 mins measured after 15 mins by calcium mobilization assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-Based Design and Development of Chemical Probes Targeting Putative MOR-CCR5 Heterodimers to Inhibit Opioid Exacerbated HIV-1 Infectivity.
Huang B, Wang H, Zheng Y, Li M, Kang G, Barreto-de-Souza V, Nassehi N, Knapp PE, Selley DE, Hauser KF, Zhang Y.
J Med Chem (2021) 64 : 7702 -7723
PubMed 34027668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.19 8.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19019 NALTREXONE 4.0 1 8.18
CHEMBL5071060 1 7.40
CHEMBL5074744 1 7.30
CHEMBL5089300 1 7.13
CHEMBL5074037 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19019 NALTREXONE IC50 = 6.62 nM 8.18
CHEMBL5071060 IC50 = 40.0 nM 7.40
CHEMBL5074744 IC50 = 50.0 nM 7.30
CHEMBL5089300 IC50 = 74.4 nM 7.13
CHEMBL5074037 IC50 = 1103.0 nM 5.96