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Assay Detail

CHEMBL4480315

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

Binding
Inhibition of ATG4B (unknown origin) expressed in HEK293T cells coexpressing HTRA4 and Actin-LC3B-dNGLuc after 24 hrs by luciferase release assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cysteine protease ATG4B (CHEMBL1741221)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.
Qiu Z, Kuhn B, Aebi J, Lin X, Ding H, Zhou Z, Xu Z, Xu D, Han L, Liu C, Qiu H, Zhang Y, Haap W, Riemer C, Stahl M, Qin N, Shen HC, Tang G.
ACS Med Chem Lett (2016) 7 : 802 -806
PubMed 27563406 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 5.78 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4581663 1 7.82
CHEMBL4546760 1 7.22
CHEMBL4520267 1 7.14
CHEMBL4520585 1 6.89
CHEMBL4553669 1 6.64
CHEMBL4567870 1 6.28
CHEMBL4574173 1 6.04
CHEMBL4579064 1 6.02
CHEMBL4567655 1 5.92
CHEMBL4588146 1 5.90
CHEMBL4572200 1 5.83
CHEMBL4539211 1 5.75
CHEMBL4535723 1 5.75
CHEMBL4590201 1 5.59
CHEMBL4578571 1 5.52
CHEMBL4569375 1 5.39
CHEMBL4562540 1 5.35
CHEMBL2402203 1 5.29
CHEMBL4570064 1 5.25
CHEMBL4525169 1 4.91
CHEMBL4540188 1 4.87
CHEMBL4527514 1 4.46
CHEMBL4515617 1 4.42
CHEMBL4566110 1 4.42
CHEMBL4520698 1 -
CHEMBL4529816 1 -
CHEMBL4563886 1 -
CHEMBL4564704 1 -
CHEMBL4204523 1 -
CHEMBL344174 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4581663 IC50 = 15.0 nM 7.82
CHEMBL4546760 IC50 = 60.0 nM 7.22
CHEMBL4520267 IC50 = 73.0 nM 7.14
CHEMBL4520585 IC50 = 130.0 nM 6.89
CHEMBL4553669 IC50 = 230.0 nM 6.64
CHEMBL4567870 IC50 = 530.0 nM 6.28
CHEMBL4574173 IC50 = 920.0 nM 6.04
CHEMBL4579064 IC50 = 950.0 nM 6.02
CHEMBL4567655 IC50 = 1190.0 nM 5.92
CHEMBL4588146 IC50 = 1270.0 nM 5.90
CHEMBL4572200 IC50 = 1470.0 nM 5.83
CHEMBL4539211 IC50 = 1780.0 nM 5.75
CHEMBL4535723 IC50 = 1760.0 nM 5.75
CHEMBL4590201 IC50 = 2570.0 nM 5.59
CHEMBL4578571 IC50 = 2990.0 nM 5.52
CHEMBL4569375 IC50 = 4060.0 nM 5.39
CHEMBL4562540 IC50 = 4470.0 nM 5.35
CHEMBL2402203 IC50 = 5090.0 nM 5.29
CHEMBL4570064 IC50 = 5680.0 nM 5.25
CHEMBL4525169 IC50 = 12300.0 nM 4.91
CHEMBL4540188 IC50 = 13400.0 nM 4.87
CHEMBL4527514 IC50 = 34300.0 nM 4.46
CHEMBL4515617 IC50 = 38100.0 nM 4.42
CHEMBL4566110 IC50 = 37600.0 nM 4.42
CHEMBL4554009 IC50 - -
CHEMBL4566679 IC50 - -
CHEMBL4556657 IC50 > 100000.0 nM -
CHEMBL4568708 IC50 > 100000.0 nM -
CHEMBL4594129 IC50 > 100000.0 nM -
CHEMBL4527093 IC50 > 100000.0 nM -
CHEMBL4555270 IC50 - -
CHEMBL4218185 IC50 > 100000.0 nM -
CHEMBL4549686 IC50 > 100000.0 nM -
CHEMBL344174 IC50 > 100000.0 nM -
CHEMBL4204523 IC50 > 100000.0 nM -
CHEMBL4564704 IC50 > 100000.0 nM -
CHEMBL4563886 IC50 > 100000.0 nM -
CHEMBL4529816 IC50 > 100000.0 nM -
CHEMBL4520698 IC50 > 100000.0 nM -