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Assay Detail

CHEMBL4196838

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

Binding
Inhibition of PGPH activity of human 26S proteasome using Z-LLE-MCA as substrate measured for 1 hr by fluorescence assay
17
Total Activities
17
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

Proteasome component C5 (CHEMBL4208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Ridaifen-F conjugated with cell-penetrating peptides inhibits intracellular proteasome activities and induces drug-resistant cell death.
Tanaka M, Zhu Y, Shionyu M, Ota N, Shibata N, Watanabe C, Mizusawa A, Sasaki R, Mizukami T, Shiina I, Hasegawa M.
Eur J Med Chem (2018) 146 : 636 -650
PubMed 29407987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.41 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL325041 BORTEZOMIB 3.0 1 7.72
CHEMBL4209883 1 4.77
CHEMBL4210397 1 4.66
CHEMBL4206039 1 4.48
CHEMBL4212401 1 -
CHEMBL4217338 1 -
CHEMBL4212383 1 -
CHEMBL4212914 1 -
CHEMBL159 VINBLASTINE 4.0 1 -
CHEMBL374308 LACTACYSTIN 1 -
CHEMBL3099618 1 -
CHEMBL4215864 1 -
CHEMBL4218282 1 -
CHEMBL4213348 1 -
CHEMBL4217753 1 -
CHEMBL4205518 1 -
CHEMBL4204198 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL325041 BORTEZOMIB IC50 = 19.0 nM 7.72
CHEMBL4209883 IC50 = 17000.0 nM 4.77
CHEMBL4210397 IC50 = 22000.0 nM 4.66
CHEMBL4206039 IC50 = 33000.0 nM 4.48
CHEMBL4212401 IC50 > 50000.0 nM -
CHEMBL4217338 IC50 > 40000.0 nM -
CHEMBL4212383 IC50 > 40000.0 nM -
CHEMBL4212914 IC50 > 40000.0 nM -
CHEMBL159 VINBLASTINE IC50 > 40000.0 nM -
CHEMBL374308 LACTACYSTIN IC50 > 40000.0 nM -
CHEMBL3099618 IC50 > 100000.0 nM -
CHEMBL4215864 IC50 > 40000.0 nM -
CHEMBL4218282 IC50 > 40000.0 nM -
CHEMBL4213348 IC50 > 40000.0 nM -
CHEMBL4217753 IC50 > 40000.0 nM -
CHEMBL4205518 IC50 > 40000.0 nM -
CHEMBL4204198 IC50 > 40000.0 nM -