Assay Detail
Binding
CHEMBL1914115
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Irreversible inhibition of PAD4 R374K mutant assessed as hydrolysis of benzoyl-L-arginine ethyl ester preincubated for 15 mins measured after 15 mins
4
Total Activities
4
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 |
Publication
The development of N-α-(2-carboxyl)benzoyl-N(5)-(2-fluoro-1-iminoethyl)-l-ornithine amide (o-F-amidine) and N-α-(2-carboxyl)benzoyl-N(5)-(2-chloro-1-iminoethyl)-l-ornithine amide (o-Cl-amidine) as second generation protein arginine deiminase (PAD) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.12 | 5.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1910970 | — | — | 1 | 5.34 |
| CHEMBL1910971 | — | — | 1 | 5.28 |
| CHEMBL1910972 | — | — | 1 | 5.05 |
| CHEMBL1910973 | — | — | 1 | 4.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1910970 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL1910971 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL1910972 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL1910973 | — | IC50 | = | 15000.0 | nM | 4.82 |