Assay Detail
Binding
CHEMBL3999296
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human RIP1 (1 to 375 residues) expressed in baculovirus infected insect cells preincubated for 1 hr followed by ATP addition measured after 5 hrs by ADP-Glo luminescence assay
20
Total Activities
20
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
Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 9.25 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4067372 | — | — | 1 | 10.30 |
| CHEMBL3785745 | — | — | 1 | 10.20 |
| CHEMBL4093220 | — | — | 1 | 10.10 |
| CHEMBL3786997 | — | — | 1 | 9.70 |
| CHEMBL4068954 | — | — | 1 | 9.49 |
| CHEMBL4096224 | — | — | 1 | 9.49 |
| CHEMBL4060644 | — | — | 1 | 9.40 |
| CHEMBL4069318 | — | — | 1 | 9.40 |
| CHEMBL4099004 | — | — | 1 | 9.30 |
| CHEMBL4089558 | — | — | 1 | 9.30 |
| CHEMBL4065561 | — | — | 1 | 9.20 |
| CHEMBL4081685 | — | — | 1 | 9.20 |
| CHEMBL4088857 | — | — | 1 | 9.10 |
| CHEMBL3786078 | — | — | 1 | 9.10 |
| CHEMBL4099698 | — | — | 1 | 9.00 |
| CHEMBL4071864 | GSK2982772 | 2.0 | 1 | 9.00 |
| CHEMBL4080978 | — | — | 1 | 9.00 |
| CHEMBL4071080 | — | — | 1 | 8.70 |
| CHEMBL4069959 | — | — | 1 | 8.30 |
| CHEMBL3786293 | — | — | 1 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4067372 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL3785745 | — | IC50 | = | 0.063 | nM | 10.20 |
| CHEMBL4093220 | — | IC50 | = | 0.079 | nM | 10.10 |
| CHEMBL3786997 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4068954 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4096224 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4060644 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4069318 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4099004 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4089558 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4065561 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL4081685 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL4088857 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL3786078 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL4099698 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4071864 | GSK2982772 | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4080978 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4071080 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4069959 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3786293 | — | IC50 | = | 16.0 | nM | 7.80 |