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Assay Detail

CHEMBL2388468

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

Binding
Inverse agonist activity at human cytomegalovirus US28 receptor transfected in HEK293T cells assessed as activation of MAPK signaling pathway after 20 to 24 hrs by luciferase-based Elk1 reporter gene assay
40
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human betaherpesvirus 5
Cell Type HEK-293T
Confidence 3 — Cell-line / Tissue
Curated By Autocuration

Publication

Development of flavonoid-based inverse agonists of the key signaling receptor US28 of human cytomegalovirus.
Kralj A, Nguyen MT, Tschammer N, Ocampo N, Gesiotto Q, Heinrich MR, Phanstiel O.
J Med Chem (2013) 56 : 5019 -5032
PubMed 23768434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 39 5.45 6.51
pEC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2386689 2 6.51
CHEMBL2386683 2 6.10
CHEMBL2386688 2 5.88
CHEMBL594854 2 5.85
CHEMBL2386690 2 5.75
CHEMBL2386681 2 5.54
CHEMBL2386541 2 5.46
CHEMBL244746 2 5.34
CHEMBL2386673 2 5.31
CHEMBL2386671 2 5.30
CHEMBL2386675 2 5.26
CHEMBL2386674 2 5.22
CHEMBL2386677 2 5.19
CHEMBL2386672 2 5.18
CHEMBL2386540 2 5.14
CHEMBL2386670 2 5.11
CHEMBL2386676 2 5.11
CHEMBL2386542 2 5.09
CHEMBL2386678 2 5.00
CHEMBL2386679 1 -
CHEMBL2386680 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2386689 EC50 = 309.03 nM 6.51
CHEMBL2386689 EC50 = 310.0 nM 6.51
CHEMBL2386683 EC50 = 800.0 nM 6.10
CHEMBL2386683 EC50 = 831.76 nM 6.08
CHEMBL2386688 EC50 = 1320.0 nM 5.88
CHEMBL2386688 EC50 = 1318.26 nM 5.88
CHEMBL594854 EC50 = 1400.0 nM 5.85
CHEMBL594854 EC50 = 1445.44 nM 5.84
CHEMBL2386690 EC50 = 1780.0 nM 5.75
CHEMBL2386690 EC50 = 1778.28 nM 5.75
CHEMBL2386681 EC50 = 2884.03 nM 5.54
CHEMBL2386681 EC50 = 2900.0 nM 5.54
CHEMBL2386541 EC50 = 3500.0 nM 5.46
CHEMBL2386541 EC50 = 3467.37 nM 5.46
CHEMBL244746 EC50 = 4600.0 nM 5.34
CHEMBL244746 EC50 = 4570.88 nM 5.34
CHEMBL2386673 EC50 = 4897.79 nM 5.31
CHEMBL2386673 EC50 = 4900.0 nM 5.31
CHEMBL2386671 EC50 = 5011.87 nM 5.30
CHEMBL2386671 EC50 = 5000.0 nM 5.30
CHEMBL2386675 EC50 = 5495.41 nM 5.26
CHEMBL2386675 EC50 = 5500.0 nM 5.26
CHEMBL2386674 EC50 = 6000.0 nM 5.22
CHEMBL2386674 EC50 = 6025.6 nM 5.22
CHEMBL2386677 EC50 = 6456.54 nM 5.19
CHEMBL2386677 EC50 = 6400.0 nM 5.19
CHEMBL2386672 EC50 = 6606.93 nM 5.18
CHEMBL2386672 EC50 = 6700.0 nM 5.17
CHEMBL2386540 EC50 = 7244.36 nM 5.14
CHEMBL2386540 EC50 = 7300.0 nM 5.14
CHEMBL2386676 EC50 = 7800.0 nM 5.11
CHEMBL2386676 EC50 = 7762.47 nM 5.11
CHEMBL2386670 EC50 = 7762.47 nM 5.11
CHEMBL2386670 EC50 = 7800.0 nM 5.11
CHEMBL2386542 EC50 = 8100.0 nM 5.09
CHEMBL2386542 EC50 = 8128.31 nM 5.09
CHEMBL2386678 EC50 = 10000.0 nM 5.00
CHEMBL2386680 EC50 - -
CHEMBL2386678 pEC50 - -
CHEMBL2386679 EC50 - -