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Assay Detail

CHEMBL4028623

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

Binding
Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by manual-patch-clamp electrophysiology assay
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

3-((R)-4-(((R)-6-(2-Bromo-4-fluorophenyl)-5-(ethoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholin-2-yl)propanoic Acid (HEC72702), a Novel Hepatitis B Virus Capsid Inhibitor Based on Clinical Candidate GLS4.
Ren Q, Liu X, Yan G, Nie B, Zou Z, Li J, Chen Y, Wei Y, Huang J, Luo Z, Gu B, Goldmann S, Zhang J, Zhang Y.
J Med Chem (2018) 61 : 1355 -1374
PubMed 29381358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 59 5.66 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4079561 1 6.77
CHEMBL4103602 1 6.58
CHEMBL4078766 1 6.52
CHEMBL4082519 1 6.16
CHEMBL3742114 1 6.07
CHEMBL4077161 1 6.05
CHEMBL4087396 1 5.97
CHEMBL4088287 1 5.79
CHEMBL4076401 1 5.64
CHEMBL4075908 1 5.46
CHEMBL4070728 1 5.42
CHEMBL4062770 1 5.39
CHEMBL4068707 1 5.38
CHEMBL4064808 1 5.35
CHEMBL4092509 1 5.31
CHEMBL4067663 1 5.30
CHEMBL4098434 1 5.24
CHEMBL4102761 1 5.13
CHEMBL4103771 1 5.06
CHEMBL4100106 1 4.62
CHEMBL4089481 1 -
CHEMBL4068300 1 -
CHEMBL4081602 1 -
CHEMBL4059649 1 -
CHEMBL4097181 1 -
CHEMBL4104891 1 -
CHEMBL4102843 1 -
CHEMBL4084893 1 -
CHEMBL4079517 1 -
CHEMBL4060052 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4079561 IC50 = 170.0 nM 6.77
CHEMBL4103602 IC50 = 260.0 nM 6.58
CHEMBL4078766 IC50 = 300.0 nM 6.52
CHEMBL4082519 IC50 = 700.0 nM 6.16
CHEMBL3742114 IC50 = 860.0 nM 6.07
CHEMBL4077161 IC50 = 900.0 nM 6.05
CHEMBL4087396 IC50 = 1070.0 nM 5.97
CHEMBL4088287 IC50 = 1640.0 nM 5.79
CHEMBL4076401 IC50 = 2310.0 nM 5.64
CHEMBL4075908 IC50 = 3490.0 nM 5.46
CHEMBL4070728 IC50 = 3800.0 nM 5.42
CHEMBL4062770 IC50 = 4040.0 nM 5.39
CHEMBL4068707 IC50 = 4190.0 nM 5.38
CHEMBL4064808 IC50 = 4500.0 nM 5.35
CHEMBL4092509 IC50 = 4880.0 nM 5.31
CHEMBL4067663 IC50 = 4960.0 nM 5.30
CHEMBL4098434 IC50 = 5740.0 nM 5.24
CHEMBL4102761 IC50 = 7330.0 nM 5.13
CHEMBL4103771 IC50 = 8680.0 nM 5.06
CHEMBL4100106 IC50 = 24200.0 nM 4.62
CHEMBL4085181 IC50 > 30000.0 nM -
CHEMBL4063560 IC50 > 30000.0 nM -
CHEMBL4074324 IC50 > 30000.0 nM -
CHEMBL4094822 IC50 > 30000.0 nM -
CHEMBL4061060 IC50 > 30000.0 nM -
CHEMBL4092352 IC50 > 30000.0 nM -
CHEMBL4064672 IC50 > 30000.0 nM -
CHEMBL4073176 IC50 > 30000.0 nM -
CHEMBL4091444 IC50 > 30000.0 nM -
CHEMBL4061904 IC50 > 30000.0 nM -
CHEMBL4087026 IC50 > 10000.0 nM -
CHEMBL4068628 IC50 > 30000.0 nM -
CHEMBL4095407 IC50 > 30000.0 nM -
CHEMBL4095001 IC50 > 30000.0 nM -
CHEMBL4077526 IC50 > 10000.0 nM -
CHEMBL4101622 IC50 > 30000.0 nM -
CHEMBL4074934 IC50 > 30000.0 nM -
CHEMBL4093889 IC50 > 30000.0 nM -
CHEMBL4083668 IC50 > 30000.0 nM -
CHEMBL4096023 IC50 > 10000.0 nM -
CHEMBL4060052 IC50 > 10000.0 nM -
CHEMBL4079517 IC50 > 10000.0 nM -
CHEMBL4084893 IC50 > 10000.0 nM -
CHEMBL4102843 IC50 > 10000.0 nM -
CHEMBL4104891 IC50 > 10000.0 nM -
CHEMBL4097181 IC50 > 10000.0 nM -
CHEMBL4059649 IC50 > 10000.0 nM -
CHEMBL4081602 IC50 > 10000.0 nM -
CHEMBL4068300 IC50 > 10000.0 nM -
CHEMBL4089481 IC50 > 10000.0 nM -