Assay Detail
Binding
CHEMBL1914013
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Irreversible inhibition of PAD2 assessed as hydrolysis of benzoyl-L-arginine ethyl ester preincubated for 15 mins measured after 15 mins by fluorometric analysis
5
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Protein-arginine deiminase type-2 (CHEMBL1909487) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 4.76 | 5.21 |
| Ki | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1910971 | — | — | 1 | 5.21 |
| CHEMBL1910972 | — | — | 1 | 4.77 |
| CHEMBL1910973 | — | — | 1 | 4.29 |
| CHEMBL1910970 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1910971 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL1910972 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL1910973 | — | IC50 | = | 51000.0 | nM | 4.29 |
| CHEMBL1910970 | — | IC50 | >= | 50000.0 | nM | - |
| CHEMBL1910970 | — | Ki | - | — | - |