Assay Detail
Binding
CHEMBL4023993
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of fluorescent-labeled 3-(3-((3-(4-amino-5-(4-(3-(2-fluoro-5-(trifluoromethyl)phenyl)ureido)-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)propyl)amino)-3-oxopropyl)-5,5-difluoro-7,9-dimethyl-5H-dipyrrolo[1,2-c:2',1'-f]-[1,3,2]diazaborinin-4-ium-5-uide binding to human N-terminal GST/His-tagged RIPK1 (1 to 375 residues) expressed in baculovirus expression system by TR-FRET assay
27
Total Activities
27
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 7-Oxo-2,4,5,7-tetrahydro-6 H-pyrazolo[3,4- c]pyridine Derivatives as Potent, Orally Available, and Brain-Penetrating Receptor Interacting Protein 1 (RIP1) Kinase Inhibitors: Analysis of Structure-Kinetic Relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 8.03 | 9.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4075976 | — | — | 1 | 9.39 |
| CHEMBL4061975 | — | — | 1 | 9.07 |
| CHEMBL4069537 | — | — | 1 | 9.04 |
| CHEMBL4100398 | — | — | 1 | 9.04 |
| CHEMBL4071864 | GSK2982772 | 2.0 | 1 | 9.01 |
| CHEMBL4084681 | — | — | 1 | 8.94 |
| CHEMBL4082215 | — | — | 1 | 8.94 |
| CHEMBL4090975 | — | — | 1 | 8.76 |
| CHEMBL4075705 | — | — | 1 | 8.75 |
| CHEMBL247228 | GW770249X | — | 1 | 8.69 |
| CHEMBL4102622 | — | — | 1 | 8.60 |
| CHEMBL4064701 | — | — | 1 | 8.59 |
| CHEMBL4085728 | — | — | 1 | 8.53 |
| CHEMBL4073321 | — | — | 1 | 8.46 |
| CHEMBL4088216 | TP-030-1 | — | 1 | 8.41 |
| CHEMBL4071690 | — | — | 1 | 8.29 |
| CHEMBL4098708 | — | — | 1 | 8.10 |
| CHEMBL4060308 | — | — | 1 | 7.86 |
| CHEMBL4090065 | — | — | 1 | 7.47 |
| CHEMBL4076592 | — | — | 1 | 7.42 |
| CHEMBL4100309 | — | — | 1 | 7.26 |
| CHEMBL4077039 | — | — | 1 | 7.20 |
| CHEMBL4066941 | — | — | 1 | 6.97 |
| CHEMBL4082291 | — | — | 1 | 6.93 |
| CHEMBL4063075 | — | — | 1 | 6.60 |
| CHEMBL4079755 | — | — | 1 | 5.37 |
| CHEMBL4097778 | TP-030n | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4075976 | — | Ki | = | 0.4074 | nM | 9.39 |
| CHEMBL4061975 | — | Ki | = | 0.8511 | nM | 9.07 |
| CHEMBL4069537 | — | Ki | = | 0.912 | nM | 9.04 |
| CHEMBL4100398 | — | Ki | = | 0.912 | nM | 9.04 |
| CHEMBL4071864 | GSK2982772 | Ki | = | 0.9772 | nM | 9.01 |
| CHEMBL4084681 | — | Ki | = | 1.148 | nM | 8.94 |
| CHEMBL4082215 | — | Ki | = | 1.148 | nM | 8.94 |
| CHEMBL4090975 | — | Ki | = | 1.738 | nM | 8.76 |
| CHEMBL4075705 | — | Ki | = | 1.778 | nM | 8.75 |
| CHEMBL247228 | GW770249X | Ki | = | 2.042 | nM | 8.69 |
| CHEMBL4102622 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL4064701 | — | Ki | = | 2.57 | nM | 8.59 |
| CHEMBL4085728 | — | Ki | = | 2.951 | nM | 8.53 |
| CHEMBL4073321 | — | Ki | = | 3.467 | nM | 8.46 |
| CHEMBL4088216 | TP-030-1 | Ki | = | 3.89 | nM | 8.41 |
| CHEMBL4071690 | — | Ki | = | 5.129 | nM | 8.29 |
| CHEMBL4098708 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL4060308 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL4090065 | — | Ki | = | 33.88 | nM | 7.47 |
| CHEMBL4076592 | — | Ki | = | 38.02 | nM | 7.42 |
| CHEMBL4100309 | — | Ki | = | 54.95 | nM | 7.26 |
| CHEMBL4077039 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL4066941 | — | Ki | = | 107.15 | nM | 6.97 |
| CHEMBL4082291 | — | Ki | = | 117.49 | nM | 6.93 |
| CHEMBL4063075 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL4079755 | — | Ki | = | 4265.8 | nM | 5.37 |
| CHEMBL4097778 | TP-030n | Ki | = | 6918.31 | nM | 5.16 |