Assay Detail
Binding
CHEMBL3110728
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of RIP1 in human U937 cells assessed as prevention of TNFalpha/zVAD.fmk-induced necrotic cell death preincubated for 30 to 60 mins followed by TNF-alpha induction measured after overnight incubation by Cell Titer-Glo luminescence assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-937 |
| 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
Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.38 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3109209 | — | — | 1 | 8.20 |
| CHEMBL3109212 | — | — | 1 | 7.80 |
| CHEMBL3109213 | — | — | 1 | 7.80 |
| CHEMBL3109194 | — | — | 1 | 7.60 |
| CHEMBL3109211 | — | — | 1 | 7.30 |
| CHEMBL3109210 | — | — | 1 | 7.20 |
| CHEMBL3109214 | — | — | 1 | 7.20 |
| CHEMBL3109204 | — | — | 1 | 7.10 |
| CHEMBL3109207 | — | — | 1 | 6.80 |
| CHEMBL3108785 | — | — | 1 | 6.80 |
| CHEMBL3109221 | — | — | 1 | 6.70 |
| CHEMBL247228 | GW770249X | — | 1 | 6.60 |
| CHEMBL3109219 | — | — | 1 | 6.60 |
| CHEMBL3109206 | — | — | 1 | 6.50 |
| CHEMBL3109203 | — | — | 1 | 6.50 |
| CHEMBL3109205 | — | — | 1 | 6.40 |
| CHEMBL550273 | — | — | 1 | 6.22 |
| CHEMBL3109202 | — | — | 1 | 6.20 |
| CHEMBL3109196 | — | — | 1 | 6.20 |
| CHEMBL3109195 | — | — | 1 | 6.20 |
| CHEMBL436806 | — | — | 1 | 6.10 |
| CHEMBL273564 | GW795493X | — | 1 | 6.00 |
| CHEMBL3109215 | — | — | 1 | 5.89 |
| CHEMBL3109218 | — | — | 1 | 5.89 |
| CHEMBL3109200 | — | — | 1 | 5.70 |
| CHEMBL3109198 | — | — | 1 | 5.60 |
| CHEMBL3109197 | — | — | 1 | 5.60 |
| CHEMBL3109216 | — | — | 1 | 5.30 |
| CHEMBL3109208 | — | — | 1 | 5.10 |
| CHEMBL3109220 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3109209 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3109212 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3109213 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3109194 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3109211 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3109210 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL3109214 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL3109204 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3108785 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3109207 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3109221 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL247228 | GW770249X | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3109219 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3109206 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3109203 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3109205 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL550273 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3109202 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL3109195 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL3109196 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL436806 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL273564 | GW795493X | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3109215 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3109218 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3109200 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3109198 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3109197 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3109216 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3109208 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL3109220 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL396107 | GW795486X | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL3109217 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL437369 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3109201 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3109199 | — | IC50 | > | 10000.0 | nM | - |