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Assay Detail

CHEMBL885194

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

Functional
Effective concentration against US28-mediated inositol phosphate production in COS-7 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type COS-7
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and structure-activity relationship of the first nonpeptidergic inverse agonists for the human cytomegalovirus encoded chemokine receptor US28.
Hulshof JW, Casarosa P, Menge WM, Kuusisto LM, van der Goot H, Smit MJ, de Esch IJ, Leurs R.
J Med Chem (2005) 48 : 6461 -6471
PubMed 16190772 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 4.97 5.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34166 BERLEX COMPOUND 1 5.50
CHEMBL198935 1 5.38
CHEMBL198553 1 5.01
CHEMBL370577 1 4.94
CHEMBL198505 1 4.86
CHEMBL195943 1 4.55
CHEMBL141713 1 4.54
CHEMBL380793 1 -
CHEMBL422115 1 -
CHEMBL197978 1 -
CHEMBL198503 1 -
CHEMBL199034 1 -
CHEMBL198308 1 -
CHEMBL198449 1 -
CHEMBL199065 1 -
CHEMBL199252 1 -
CHEMBL197342 1 -
CHEMBL370660 1 -
CHEMBL372756 1 -
CHEMBL199035 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34166 BERLEX COMPOUND EC50 = 3200.0 nM 5.50
CHEMBL198935 EC50 = 4200.0 nM 5.38
CHEMBL198553 EC50 = 9800.0 nM 5.01
CHEMBL370577 EC50 = 11500.0 nM 4.94
CHEMBL198505 EC50 = 13800.0 nM 4.86
CHEMBL195943 EC50 = 28200.0 nM 4.55
CHEMBL141713 EC50 = 28800.0 nM 4.54
CHEMBL380793 EC50 > 100000.0 nM -
CHEMBL422115 EC50 > 100000.0 nM -
CHEMBL197978 EC50 > 100000.0 nM -
CHEMBL198503 EC50 > 100000.0 nM -
CHEMBL199034 EC50 > 100000.0 nM -
CHEMBL198308 EC50 > 100000.0 nM -
CHEMBL198449 EC50 > 100000.0 nM -
CHEMBL199065 EC50 > 100000.0 nM -
CHEMBL199252 EC50 > 100000.0 nM -
CHEMBL197342 EC50 > 100000.0 nM -
CHEMBL370660 EC50 > 100000.0 nM -
CHEMBL372756 EC50 > 100000.0 nM -
CHEMBL199035 EC50 > 100000.0 nM -