Assay Detail
Binding
CHEMBL5500873
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to RIP1 (unknown origin) assessed as dissociation constant by KINOMEscan assay
27
Total Activities
27
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
Receptor-interacting serine/threonine-protein kinase 1 (CHEMBL5464) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Scaffold hopping derived novel benzoxazepinone receptor-interacting protein kinase 1 (RIP1) inhibitors as anti-necroptosis agents: Anti-inflammatory effect in systemic inflammatory response syndrome (SIRS) and epilepsy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 27 | 6.22 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4071864 | GSK2982772 | 2.0 | 1 | 7.22 |
| CHEMBL5557467 | — | — | 1 | 6.95 |
| CHEMBL5426073 | — | — | 1 | 6.72 |
| CHEMBL5555230 | — | — | 1 | 6.67 |
| CHEMBL5558176 | — | — | 1 | 6.65 |
| CHEMBL5532569 | — | — | 1 | 6.60 |
| CHEMBL5542667 | — | — | 1 | 6.43 |
| CHEMBL5556996 | — | — | 1 | 6.35 |
| CHEMBL5549854 | — | — | 1 | 6.34 |
| CHEMBL5559287 | — | — | 1 | 6.31 |
| CHEMBL5559296 | — | — | 1 | 6.28 |
| CHEMBL5557979 | — | — | 1 | 6.23 |
| CHEMBL5517885 | — | — | 1 | 5.90 |
| CHEMBL5557281 | — | — | 1 | 5.90 |
| CHEMBL5555071 | — | — | 1 | 5.82 |
| CHEMBL5542308 | — | — | 1 | 5.53 |
| CHEMBL5555720 | — | — | 1 | 5.50 |
| CHEMBL5558745 | — | — | 1 | 5.46 |
| CHEMBL5558635 | — | — | 1 | 5.40 |
| CHEMBL5549748 | — | — | 1 | - |
| CHEMBL5523573 | — | — | 1 | - |
| CHEMBL5559021 | — | — | 1 | - |
| CHEMBL5505794 | — | — | 1 | - |
| CHEMBL5542676 | — | — | 1 | - |
| CHEMBL5555121 | — | — | 1 | - |
| CHEMBL5559107 | — | — | 1 | - |
| CHEMBL5558784 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4071864 | GSK2982772 | Kd | = | 60.0 | nM | 7.22 |
| CHEMBL5557467 | — | Kd | = | 112.0 | nM | 6.95 |
| CHEMBL5426073 | — | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL5555230 | — | Kd | = | 216.0 | nM | 6.67 |
| CHEMBL5558176 | — | Kd | = | 223.0 | nM | 6.65 |
| CHEMBL5532569 | — | Kd | = | 251.0 | nM | 6.60 |
| CHEMBL5542667 | — | Kd | = | 373.0 | nM | 6.43 |
| CHEMBL5556996 | — | Kd | = | 450.0 | nM | 6.35 |
| CHEMBL5549854 | — | Kd | = | 453.0 | nM | 6.34 |
| CHEMBL5559287 | — | Kd | = | 493.0 | nM | 6.31 |
| CHEMBL5559296 | — | Kd | = | 520.0 | nM | 6.28 |
| CHEMBL5557979 | — | Kd | = | 583.0 | nM | 6.23 |
| CHEMBL5517885 | — | Kd | = | 1269.0 | nM | 5.90 |
| CHEMBL5557281 | — | Kd | = | 1265.0 | nM | 5.90 |
| CHEMBL5555071 | — | Kd | = | 1523.0 | nM | 5.82 |
| CHEMBL5542308 | — | Kd | = | 2982.0 | nM | 5.53 |
| CHEMBL5555720 | — | Kd | = | 3162.0 | nM | 5.50 |
| CHEMBL5558745 | — | Kd | = | 3448.0 | nM | 5.46 |
| CHEMBL5558635 | — | Kd | = | 3973.0 | nM | 5.40 |
| CHEMBL5549748 | — | Kd | - | — | - | |
| CHEMBL5523573 | — | Kd | - | — | - | |
| CHEMBL5559021 | — | Kd | - | — | - | |
| CHEMBL5505794 | — | Kd | > | 5000.0 | nM | - |
| CHEMBL5542676 | — | Kd | - | — | - | |
| CHEMBL5555121 | — | Kd | - | — | - | |
| CHEMBL5559107 | — | Kd | > | 5000.0 | nM | - |
| CHEMBL5558784 | — | Kd | - | — | - |