Assay Detail
Binding
CHEMBL4305904
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of pDEST8HisGSTTev-tagged human RIP1 (1 to 375 residues) expressed in baculovirus infected insect cells preincubated with enzyme for 1 hr followed by ATP addition and measured after 5 hrs by ADP-Glo kinase assay
8
Total Activities
8
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
Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.10 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4071864 | GSK2982772 | 2.0 | 1 | 9.00 |
| CHEMBL3785703 | — | — | 1 | 8.80 |
| CHEMBL4554676 | — | — | 1 | 8.30 |
| CHEMBL4452233 | — | — | 1 | 8.20 |
| CHEMBL4453758 | — | — | 1 | 8.20 |
| CHEMBL3786293 | — | — | 1 | 7.50 |
| CHEMBL4068352 | — | — | 1 | 7.50 |
| CHEMBL4470945 | — | — | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4071864 | GSK2982772 | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3785703 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4554676 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4452233 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4453758 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3786293 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4068352 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4470945 | — | IC50 | = | 50.0 | nM | 7.30 |