Assay Detail
Binding
CHEMBL3110730
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of (14-(2-{[3-({2-{[4-(cyanomethyl)phenyl]amino}-6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-4-pyrimidinyl}amino)propyl]amino}-2-oxoethyl)-16,16,18,18-tetramethyl-6,7,7a,8a,9,10,16,18-octahydrobenzo[2'',3'']indolizino[8'',7'':5',6']pyrano[3',2':3,4]pyrido[1,2-a]indol-5-ium-2-sulfonate from human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) expressed in baculovirus infected insect Sf9 cells preincubated for 10 mins followed by fluorescent ligand addition measured after 15 mins by fluorescence polarization assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 | 7.26 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3109212 | — | — | 1 | 8.89 |
| CHEMBL3109194 | — | — | 1 | 8.49 |
| CHEMBL3109209 | — | — | 1 | 8.10 |
| CHEMBL3109196 | — | — | 1 | 7.89 |
| CHEMBL3109206 | — | — | 1 | 7.89 |
| CHEMBL3109202 | — | — | 1 | 7.80 |
| CHEMBL3109203 | — | — | 1 | 7.80 |
| CHEMBL3109210 | — | — | 1 | 7.80 |
| CHEMBL3109214 | — | — | 1 | 7.80 |
| CHEMBL3109195 | — | — | 1 | 7.70 |
| CHEMBL3108785 | — | — | 1 | 7.70 |
| CHEMBL273564 | GW795493X | — | 1 | 7.70 |
| CHEMBL3109219 | — | — | 1 | 7.60 |
| CHEMBL3109205 | — | — | 1 | 7.50 |
| CHEMBL3109213 | — | — | 1 | 7.50 |
| CHEMBL3109221 | — | — | 1 | 7.50 |
| CHEMBL3109204 | — | — | 1 | 7.50 |
| CHEMBL3109200 | — | — | 1 | 7.40 |
| CHEMBL247228 | GW770249X | — | 1 | 7.20 |
| CHEMBL3109211 | — | — | 1 | 7.20 |
| CHEMBL436806 | — | — | 1 | 7.00 |
| CHEMBL3109216 | — | — | 1 | 6.89 |
| CHEMBL3109220 | — | — | 1 | 6.80 |
| CHEMBL3109215 | — | — | 1 | 6.80 |
| CHEMBL3109197 | — | — | 1 | 6.80 |
| CHEMBL3109218 | — | — | 1 | 6.80 |
| CHEMBL3109207 | — | — | 1 | 6.70 |
| CHEMBL3109217 | — | — | 1 | 6.60 |
| CHEMBL3109198 | — | — | 1 | 6.50 |
| CHEMBL396107 | GW795486X | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3109212 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3109194 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3109209 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL3109196 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3109206 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3109202 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3109203 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3109210 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3109214 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3109195 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3108785 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL273564 | GW795493X | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3109219 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3109204 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3109221 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3109205 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3109213 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3109200 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3109211 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL247228 | GW770249X | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL436806 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3109216 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3109220 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3109215 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3109197 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3109218 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3109207 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3109217 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3109198 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL396107 | GW795486X | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL550273 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3109208 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3109201 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL437369 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3109199 | — | IC50 | > | 10000.0 | nM | - |