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Assay Detail

CHEMBL5510885

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

Binding
Inhibition of PAD2 (unknown origin) using Nalpha-benzoyl-L-arginine ethyl ester as substrate preincubated for 60 mins followed by substrate addition and measured after 90 mins by colorimetric analysis
42
Total Activities
42
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

Protein-arginine deiminase type-2 (CHEMBL1909487)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A β-Carboline Derivate PAD4 Inhibitor Reshapes Neutrophil Phenotype and Improves the Tumor Immune Microenvironment against Triple-Negative Breast Cancer.
Zhu D, Lu Y, Yan Z, Deng Q, Hu B, Wang Y, Wang W, Wang Y, Wang Y.
J Med Chem (2024) 67 : 7973 -7994
PubMed 38728549 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 5.60 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5542325 1 6.46
CHEMBL5532370 1 6.08
CHEMBL5562134 1 6.00
CHEMBL5555170 1 5.99
CHEMBL5563751 1 5.94
CHEMBL5564382 1 5.90
CHEMBL5564422 1 5.88
CHEMBL5560601 1 5.87
CHEMBL5559926 1 5.84
CHEMBL5527968 1 5.82
CHEMBL5556269 1 5.79
CHEMBL5562016 1 5.71
CHEMBL5559509 1 5.68
CHEMBL5565461 1 5.68
CHEMBL5560885 1 5.65
CHEMBL5563821 1 5.64
CHEMBL5562945 1 5.63
CHEMBL5555615 1 5.56
CHEMBL5558736 1 5.53
CHEMBL5562648 1 5.53
CHEMBL5542302 1 5.52
CHEMBL5556573 1 5.52
CHEMBL5560217 1 5.44
CHEMBL5567700 1 5.42
CHEMBL5555765 1 5.39
CHEMBL5563295 1 5.37
CHEMBL5564029 1 5.34
CHEMBL5561457 1 5.33
CHEMBL3682418 1 5.28
CHEMBL5566624 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5542325 IC50 = 350.0 nM 6.46
CHEMBL5532370 IC50 = 830.0 nM 6.08
CHEMBL5562134 IC50 = 1000.0 nM 6.00
CHEMBL5555170 IC50 = 1030.0 nM 5.99
CHEMBL5563751 IC50 = 1140.0 nM 5.94
CHEMBL5564382 IC50 = 1270.0 nM 5.90
CHEMBL5564422 IC50 = 1320.0 nM 5.88
CHEMBL5560601 IC50 = 1360.0 nM 5.87
CHEMBL5559926 IC50 = 1430.0 nM 5.84
CHEMBL5527968 IC50 = 1510.0 nM 5.82
CHEMBL5556269 IC50 = 1630.0 nM 5.79
CHEMBL5562016 IC50 = 1930.0 nM 5.71
CHEMBL5559509 IC50 = 2100.0 nM 5.68
CHEMBL5565461 IC50 = 2080.0 nM 5.68
CHEMBL5560885 IC50 = 2260.0 nM 5.65
CHEMBL5563821 IC50 = 2280.0 nM 5.64
CHEMBL5562945 IC50 = 2320.0 nM 5.63
CHEMBL5555615 IC50 = 2730.0 nM 5.56
CHEMBL5558736 IC50 = 2950.0 nM 5.53
CHEMBL5562648 IC50 = 2970.0 nM 5.53
CHEMBL5556573 IC50 = 3040.0 nM 5.52
CHEMBL5542302 IC50 = 3000.0 nM 5.52
CHEMBL5560217 IC50 = 3640.0 nM 5.44
CHEMBL5567700 IC50 = 3770.0 nM 5.42
CHEMBL5555765 IC50 = 4050.0 nM 5.39
CHEMBL5563295 IC50 = 4320.0 nM 5.37
CHEMBL5564029 IC50 = 4590.0 nM 5.34
CHEMBL5561457 IC50 = 4650.0 nM 5.33
CHEMBL3682418 IC50 = 5280.0 nM 5.28
CHEMBL5566624 IC50 = 5400.0 nM 5.27
CHEMBL5564618 IC50 = 10800.0 nM 4.97
CHEMBL5568119 IC50 = 11600.0 nM 4.94
CHEMBL5518030 IC50 = 16800.0 nM 4.78
CHEMBL5560100 IC50 > 10000.0 nM -
CHEMBL5555673 IC50 > 10000.0 nM -
CHEMBL5558439 IC50 > 10000.0 nM -
CHEMBL5555892 IC50 > 10000.0 nM -
CHEMBL5568266 IC50 > 10000.0 nM -
CHEMBL5560309 IC50 > 10000.0 nM -
CHEMBL5560638 IC50 > 10000.0 nM -
CHEMBL5517956 IC50 > 10000.0 nM -
CHEMBL5559918 IC50 > 10000.0 nM -