Assay Detail
Binding
CHEMBL661598
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Evaluated in vitro for inhibitory activity against purified human C1r protease incubated in buffer for 60 minutes
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 4.87 | 5.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL167523 | — | — | 1 | 5.52 |
| CHEMBL10312 | — | — | 1 | 5.40 |
| CHEMBL166801 | — | — | 1 | 5.22 |
| CHEMBL166632 | — | — | 1 | 5.22 |
| CHEMBL168038 | — | — | 1 | 5.08 |
| CHEMBL167163 | — | — | 1 | 5.00 |
| CHEMBL273264 | NAFAMOSTAT | 3.0 | 1 | 4.92 |
| CHEMBL169044 | — | — | 1 | 4.60 |
| CHEMBL165871 | — | — | 1 | 4.24 |
| CHEMBL165932 | — | — | 1 | 4.21 |
| CHEMBL355466 | — | — | 1 | 4.21 |
| CHEMBL168702 | — | — | 1 | - |
| CHEMBL353889 | — | — | 1 | - |
| CHEMBL166393 | — | — | 1 | - |
| CHEMBL166293 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL167523 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL10312 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL166801 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL166632 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL168038 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL167163 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL273264 | NAFAMOSTAT | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL169044 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL165871 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL165932 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL355466 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL168702 | — | IC50 | > | 62000.0 | nM | - |
| CHEMBL353889 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL166393 | — | IC50 | > | 62500.0 | nM | - |
| CHEMBL166293 | — | IC50 | > | 62000.0 | nM | - |