Assay Detail
Binding
CHEMBL5535135
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human RIPK1 (1 to 294 residues) preincubated for 15 mins followed by [gamma-33P]ATP addition and measured after 40 mins by scintillation counting analysis
51
Total Activities
51
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
From Hit to Lead: Structure-Based Optimization of Novel Selective Inhibitors of Receptor-Interacting Protein Kinase 1 (RIPK1) for the Treatment of Inflammatory Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 7.31 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5595640 | — | — | 1 | 7.82 |
| CHEMBL5594666 | — | — | 1 | 7.80 |
| CHEMBL5564492 | — | — | 1 | 7.80 |
| CHEMBL5572422 | — | — | 1 | 7.80 |
| CHEMBL5570304 | — | — | 1 | 7.77 |
| CHEMBL5591986 | — | — | 1 | 7.77 |
| CHEMBL5593492 | — | — | 1 | 7.75 |
| CHEMBL5574073 | — | — | 1 | 7.72 |
| CHEMBL5571760 | — | — | 1 | 7.70 |
| CHEMBL5575605 | — | — | 1 | 7.68 |
| CHEMBL5570441 | — | — | 1 | 7.68 |
| CHEMBL5570431 | — | — | 1 | 7.64 |
| CHEMBL5572223 | — | — | 1 | 7.64 |
| CHEMBL5592340 | — | — | 1 | 7.64 |
| CHEMBL5570334 | — | — | 1 | 7.62 |
| CHEMBL5574479 | — | — | 1 | 7.60 |
| CHEMBL5591846 | — | — | 1 | 7.60 |
| CHEMBL5568962 | — | — | 1 | 7.58 |
| CHEMBL5594763 | — | — | 1 | 7.55 |
| CHEMBL5568883 | — | — | 1 | 7.54 |
| CHEMBL5572809 | — | — | 1 | 7.54 |
| CHEMBL5542613 | — | — | 1 | 7.50 |
| CHEMBL5570887 | — | — | 1 | 7.48 |
| CHEMBL5567382 | — | — | 1 | 7.46 |
| CHEMBL5562613 | — | — | 1 | 7.46 |
| CHEMBL5403081 | — | — | 1 | 7.46 |
| CHEMBL5574831 | — | — | 1 | 7.44 |
| CHEMBL5568897 | — | — | 1 | 7.36 |
| CHEMBL5575973 | — | — | 1 | 7.32 |
| CHEMBL5569260 | — | — | 1 | 7.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5595640 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5594666 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5572422 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5564492 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5570304 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5591986 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5593492 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5574073 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5571760 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5575605 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5570441 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5592340 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5572223 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5570431 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5570334 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5574479 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5591846 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5568962 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5594763 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5568883 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5572809 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5542613 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5570887 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5403081 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5567382 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5562613 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5574831 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5568897 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5575973 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5569260 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5573733 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5572178 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5574943 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5575742 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL5567231 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5568758 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5573717 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL5571269 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5570768 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL5593087 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL5574116 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5572405 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL5573783 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL5573493 | — | IC50 | = | 406.0 | nM | 6.39 |
| CHEMBL5563373 | — | IC50 | = | 691.0 | nM | 6.16 |
| CHEMBL5571654 | — | IC50 | = | 1898.0 | nM | 5.72 |
| CHEMBL5569347 | — | IC50 | = | 3482.0 | nM | 5.46 |
| CHEMBL5571127 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5567067 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5591359 | — | IC50 | > | 10000.0 | nM | - |