Assay Detail
Binding
CHEMBL5369206
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Macrophage-stimulating protein receptor (CHEMBL2689) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Novel, Thienopyridine-Based Tyrosine Kinase Inhibitors Targeting Tumorigenic RON Splice Variants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 8.85 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5430218 | — | — | 1 | 9.80 |
| CHEMBL5427445 | — | — | 1 | 9.59 |
| CHEMBL5419134 | — | — | 1 | 9.55 |
| CHEMBL5396164 | — | — | 1 | 9.41 |
| CHEMBL5404435 | — | — | 1 | 9.39 |
| CHEMBL5421161 | — | — | 1 | 9.32 |
| CHEMBL5411457 | — | — | 1 | 9.32 |
| CHEMBL5440908 | — | — | 1 | 9.31 |
| CHEMBL5398932 | — | — | 1 | 9.21 |
| CHEMBL5397231 | — | — | 1 | 9.20 |
| CHEMBL5431928 | — | — | 1 | 9.16 |
| CHEMBL5436390 | — | — | 1 | 9.14 |
| CHEMBL5424053 | — | — | 1 | 9.14 |
| CHEMBL5437130 | — | — | 1 | 9.13 |
| CHEMBL5400656 | — | — | 1 | 9.09 |
| CHEMBL5405709 | — | — | 1 | 9.09 |
| CHEMBL5411204 | — | — | 1 | 9.07 |
| CHEMBL5431851 | — | — | 1 | 9.01 |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | 8.74 |
| CHEMBL5429072 | — | — | 1 | 8.74 |
| CHEMBL5400847 | — | — | 1 | 8.67 |
| CHEMBL5399763 | — | — | 1 | 8.65 |
| CHEMBL5429366 | — | — | 1 | 8.64 |
| CHEMBL5395573 | — | — | 1 | 8.62 |
| CHEMBL5429043 | — | — | 1 | 8.59 |
| CHEMBL5438831 | — | — | 1 | 8.55 |
| CHEMBL5425777 | — | — | 1 | 8.26 |
| CHEMBL5394757 | — | — | 1 | 8.22 |
| CHEMBL5403688 | — | — | 1 | 7.99 |
| CHEMBL5427943 | — | — | 1 | 7.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5430218 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL5427445 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL5419134 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL5396164 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL5404435 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL5421161 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL5411457 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL5440908 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL5398932 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL5397231 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL5431928 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL5436390 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL5424053 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL5437130 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL5405709 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL5400656 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL5411204 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL5431851 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL460702 | BMS-777607 | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5429072 | — | IC50 | = | 1.82 | nM | 8.74 |
| CHEMBL5400847 | — | IC50 | = | 2.15 | nM | 8.67 |
| CHEMBL5399763 | — | IC50 | = | 2.25 | nM | 8.65 |
| CHEMBL5429366 | — | IC50 | = | 2.28 | nM | 8.64 |
| CHEMBL5395573 | — | IC50 | = | 2.39 | nM | 8.62 |
| CHEMBL5429043 | — | IC50 | = | 2.55 | nM | 8.59 |
| CHEMBL5438831 | — | IC50 | = | 2.83 | nM | 8.55 |
| CHEMBL5425777 | — | IC50 | = | 5.47 | nM | 8.26 |
| CHEMBL5394757 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5403688 | — | IC50 | = | 10.29 | nM | 7.99 |
| CHEMBL5427943 | — | IC50 | = | 17.32 | nM | 7.76 |
| CHEMBL5411113 | — | IC50 | = | 21.95 | nM | 7.66 |
| CHEMBL5404027 | — | IC50 | = | 75.62 | nM | 7.12 |