Assay Detail
Binding
CHEMBL5629637
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Inhibition of human RIPK1 assessed as inhibition constant by ADP-Glo Kinase assay
14
Total Activities
14
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
Design, synthesis and biological evaluation of novel cyclic malonamide derivatives as selective RIPK1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.16 | 8.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4071864 | GSK2982772 | 2.0 | 1 | 8.78 |
| CHEMBL5632371 | — | — | 1 | 8.72 |
| CHEMBL5633468 | — | — | 1 | 7.66 |
| CHEMBL5632067 | — | — | 1 | 7.50 |
| CHEMBL5632839 | — | — | 1 | 7.36 |
| CHEMBL5633027 | — | — | 1 | 7.28 |
| CHEMBL5633836 | — | — | 1 | 7.25 |
| CHEMBL5632090 | — | — | 1 | 7.23 |
| CHEMBL5633747 | — | — | 1 | 6.87 |
| CHEMBL5633631 | — | — | 1 | 6.70 |
| CHEMBL5631547 | — | — | 1 | 6.67 |
| CHEMBL5632042 | — | — | 1 | 6.24 |
| CHEMBL5633109 | — | — | 1 | 6.10 |
| CHEMBL5631753 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4071864 | GSK2982772 | Ki | = | 1.66 | nM | 8.78 |
| CHEMBL5632371 | — | Ki | = | 1.905 | nM | 8.72 |
| CHEMBL5633468 | — | Ki | = | 21.88 | nM | 7.66 |
| CHEMBL5632067 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL5632839 | — | Ki | = | 43.65 | nM | 7.36 |
| CHEMBL5633027 | — | Ki | = | 52.48 | nM | 7.28 |
| CHEMBL5633836 | — | Ki | = | 56.23 | nM | 7.25 |
| CHEMBL5632090 | — | Ki | = | 58.88 | nM | 7.23 |
| CHEMBL5633747 | — | Ki | = | 134.9 | nM | 6.87 |
| CHEMBL5633631 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL5631547 | — | Ki | = | 213.8 | nM | 6.67 |
| CHEMBL5632042 | — | Ki | = | 575.44 | nM | 6.24 |
| CHEMBL5633109 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL5631753 | — | Ki | = | 1445.44 | nM | 5.84 |