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Assay Detail

CHEMBL5165029

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

Binding
Inhibition of Cathepsin C in human U-937 cells using H-Gly-Phe-AFC as substrate pretreated for 1 hr followed by substrate addition and incubated for 60 mins by microplate reader assay
ChEMBL ↗
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U-937
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dipeptidyl peptidase 1 (CHEMBL2252) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Non-peptidyl non-covalent cathepsin C inhibitoEEr bearing a unique thiophene-substituted pyridine: Design, structure-activity relationship and anti-inflammatory activity in vivo.
Chen X, Yan Y, Du J, Shen X, He C, Pan H, Zhu J, Liu X.
Eur J Med Chem (2022) 236 : 114368 -114368
PubMed 35429909 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 6.83 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3900409 BRENSOCATIB 3.0 1 7.82
CHEMBL5186557 — — 1 7.15
CHEMBL4875307 — — 1 7.13
CHEMBL4847055 — — 1 7.13
CHEMBL5207778 — — 1 7.06
CHEMBL5196138 — — 1 7.05
CHEMBL5204393 — — 1 7.04
CHEMBL5201740 — — 1 7.00
CHEMBL5183337 — — 1 6.90
CHEMBL4868834 — — 1 6.89
CHEMBL4848242 — — 1 6.87
CHEMBL5185056 — — 1 6.87
CHEMBL5202532 — — 1 6.83
CHEMBL5178862 — — 1 6.81
CHEMBL5181508 — — 1 6.81
CHEMBL5205065 — — 1 6.81
CHEMBL5187782 — — 1 6.77
CHEMBL5200608 — — 1 6.76
CHEMBL5189882 — — 1 6.75
CHEMBL5206614 — — 1 6.75
CHEMBL5198638 — — 1 6.74
CHEMBL5176223 — — 1 6.70
CHEMBL5171002 — — 1 6.67
CHEMBL5169830 — — 1 6.64
CHEMBL5189411 — — 1 6.61
CHEMBL5208614 — — 1 6.56
CHEMBL5186296 — — 1 6.54
CHEMBL5206777 — — 1 6.45
CHEMBL5180968 — — 1 6.40
CHEMBL5177679 — — 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3900409 BRENSOCATIB IC50 = 15.2 nM 7.82
CHEMBL5186557 — IC50 = 70.2 nM 7.15
CHEMBL4847055 — IC50 = 74.5 nM 7.13
CHEMBL4875307 — IC50 = 74.4 nM 7.13
CHEMBL5207778 — IC50 = 86.5 nM 7.06
CHEMBL5196138 — IC50 = 89.5 nM 7.05
CHEMBL5204393 — IC50 = 92.2 nM 7.04
CHEMBL5201740 — IC50 = 99.9 nM 7.00
CHEMBL5183337 — IC50 = 126.9 nM 6.90
CHEMBL4868834 — IC50 = 130.0 nM 6.89
CHEMBL4848242 — IC50 = 134.0 nM 6.87
CHEMBL5185056 — IC50 = 133.9 nM 6.87
CHEMBL5202532 — IC50 = 149.6 nM 6.83
CHEMBL5205065 — IC50 = 154.9 nM 6.81
CHEMBL5181508 — IC50 = 153.6 nM 6.81
CHEMBL5178862 — IC50 = 155.3 nM 6.81
CHEMBL5187782 — IC50 = 169.4 nM 6.77
CHEMBL5200608 — IC50 = 173.7 nM 6.76
CHEMBL5189882 — IC50 = 177.6 nM 6.75
CHEMBL5206614 — IC50 = 179.5 nM 6.75
CHEMBL5198638 — IC50 = 180.7 nM 6.74
CHEMBL5176223 — IC50 = 200.5 nM 6.70
CHEMBL5171002 — IC50 = 215.6 nM 6.67
CHEMBL5169830 — IC50 = 227.6 nM 6.64
CHEMBL5189411 — IC50 = 246.3 nM 6.61
CHEMBL5208614 — IC50 = 275.6 nM 6.56
CHEMBL5186296 — IC50 = 285.1 nM 6.54
CHEMBL5206777 — IC50 = 356.3 nM 6.45
CHEMBL5180968 — IC50 = 396.5 nM 6.40
CHEMBL5177679 — IC50 = 416.4 nM 6.38
CHEMBL5179212 — IC50 > 5000.0 nM -
CHEMBL5175900 — IC50 > 5000.0 nM -
CHEMBL5173569 — IC50 > 5000.0 nM -
CHEMBL5191730 — IC50 > 5000.0 nM -
CHEMBL5186113 — IC50 > 5000.0 nM -
CHEMBL5198107 — IC50 > 5000.0 nM -
CHEMBL5176578 — IC50 > 5000.0 nM -
CHEMBL5176848 — IC50 > 5000.0 nM -
CHEMBL5202703 — IC50 > 5000.0 nM -
CHEMBL5208509 — IC50 > 5000.0 nM -
CHEMBL5184805 — IC50 > 5000.0 nM -
CHEMBL5189518 — IC50 > 5000.0 nM -
CHEMBL5174217 — IC50 > 5000.0 nM -
CHEMBL5195835 — IC50 > 5000.0 nM -
CHEMBL5172531 — IC50 > 5000.0 nM -