Assay Detail
Binding
CHEMBL5147328
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Binding affinity to wild-type human partial length RIPK1 (M1 to K305 residues) expressed in bacterial expression system incubated for 1 hr under shaking condition by Kinomescan method
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
Investigation on the chemical space of the substituted triazole thio-benzoxazepinone RIPK1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 8 | 7.04 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4871408 | — | — | 1 | 7.51 |
| CHEMBL5188220 | — | — | 1 | 7.51 |
| CHEMBL4071864 | GSK2982772 | 2.0 | 1 | 7.31 |
| CHEMBL5180233 | — | — | 1 | 7.22 |
| CHEMBL5177347 | — | — | 1 | 7.10 |
| CHEMBL5181292 | — | — | 1 | 6.57 |
| CHEMBL5181126 | — | — | 1 | 6.57 |
| CHEMBL5183211 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4871408 | — | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL5188220 | — | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL4071864 | GSK2982772 | Kd | = | 49.0 | nM | 7.31 |
| CHEMBL5180233 | — | Kd | = | 60.0 | nM | 7.22 |
| CHEMBL5177347 | — | Kd | = | 79.0 | nM | 7.10 |
| CHEMBL5181292 | — | Kd | = | 267.0 | nM | 6.57 |
| CHEMBL5181126 | — | Kd | = | 272.0 | nM | 6.57 |
| CHEMBL5183211 | — | Kd | = | 301.0 | nM | 6.52 |