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Assay Detail

CHEMBL3366772

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Binding
Allosteric modulatory activity at FLAG-tagged wild type human cytomegalovirus US28 receptor expressed in HEK293T cells by PathDetectElk1 assay
12
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human betaherpesvirus 5
Cell Type HEK-293T
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

G-protein coupled receptor homolog US28 (CHEMBL4259)
Type SINGLE PROTEIN
Organism Human cytomegalovirus (strain AD169) (HHV-5) (Human herpesvirus 5)

Publication

Allosteric modulation of the G protein-coupled US28 receptor of human cytomegalovirus: are the small-weight inverse agonist of US28 'camouflaged' agonists?
Tschammer N.
Bioorg Med Chem Lett (2014) 24 : 3744 -3747
PubMed 25052428 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 5.74 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93240 METITEPINE 2.0 2 6.46
CHEMBL1824272 2 6.00
CHEMBL1824269 2 5.82
CHEMBL1824275 2 5.47
CHEMBL1824270 2 5.36
CHEMBL34166 BERLEX COMPOUND 2 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93240 METITEPINE EC50 = 350.0 nM 6.46
CHEMBL93240 METITEPINE EC50 = 354.81 nM 6.45
CHEMBL1824272 EC50 = 1000.0 nM 6.00
CHEMBL1824272 EC50 = 1023.29 nM 5.99
CHEMBL1824269 EC50 = 1513.56 nM 5.82
CHEMBL1824269 EC50 = 1500.0 nM 5.82
CHEMBL1824275 EC50 = 3400.0 nM 5.47
CHEMBL1824275 EC50 = 3467.37 nM 5.46
CHEMBL1824270 EC50 = 4365.16 nM 5.36
CHEMBL1824270 EC50 = 4400.0 nM 5.36
CHEMBL34166 BERLEX COMPOUND EC50 = 4500.0 nM 5.35
CHEMBL34166 BERLEX COMPOUND EC50 = 4570.88 nM 5.34