Assay Detail
Binding
CHEMBL5504731
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Inhibition of MER (unknown origin) preincubated for 15 mins followed by substrate and ATP addition and measured after 3 hrs by ADP-Glo kinase 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 |
Publication
Discovery of Dual MER/AXL Kinase Inhibitors as Bifunctional Small Molecules for Inhibiting Tumor Growth and Enhancing Tumor Immune Microenvironment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.71 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5532211 | — | — | 1 | 8.68 |
| CHEMBL5517863 | — | — | 1 | 8.64 |
| CHEMBL5512537 | — | — | 1 | 8.62 |
| CHEMBL5557391 | — | — | 1 | 8.39 |
| CHEMBL5558074 | — | — | 1 | 8.24 |
| CHEMBL3326006 | — | — | 1 | 8.24 |
| CHEMBL5314429 | TAMNORZATINIB | 2.0 | 1 | 8.01 |
| CHEMBL5558836 | — | — | 1 | 8.00 |
| CHEMBL5559385 | — | — | 1 | 7.94 |
| CHEMBL5505865 | — | — | 1 | 7.92 |
| CHEMBL5555377 | — | — | 1 | 7.85 |
| CHEMBL5556050 | — | — | 1 | 7.80 |
| CHEMBL5557044 | — | — | 1 | 7.63 |
| CHEMBL5532530 | — | — | 1 | 7.47 |
| CHEMBL5505936 | — | — | 1 | 7.46 |
| CHEMBL5542282 | — | — | 1 | 7.38 |
| CHEMBL5555723 | — | — | 1 | 7.35 |
| CHEMBL5556349 | — | — | 1 | 7.23 |
| CHEMBL5559274 | — | — | 1 | 7.11 |
| CHEMBL5559259 | — | — | 1 | 6.75 |
| CHEMBL5558002 | — | — | 1 | 6.75 |
| CHEMBL3809489 | BEMCENTINIB | 2.0 | 1 | 6.20 |
| CHEMBL5557417 | — | — | 1 | - |
| CHEMBL5512532 | — | — | 1 | - |
| CHEMBL5558655 | — | — | 1 | - |
| CHEMBL5542329 | — | — | 1 | - |
| CHEMBL5523590 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5532211 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5517863 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5512537 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5557391 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5558074 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3326006 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5314429 | TAMNORZATINIB | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL5558836 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL5559385 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL5505865 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5555377 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL5556050 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL5557044 | — | IC50 | = | 23.5 | nM | 7.63 |
| CHEMBL5532530 | — | IC50 | = | 34.1 | nM | 7.47 |
| CHEMBL5505936 | — | IC50 | = | 34.8 | nM | 7.46 |
| CHEMBL5542282 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5555723 | — | IC50 | = | 45.1 | nM | 7.35 |
| CHEMBL5556349 | — | IC50 | = | 59.4 | nM | 7.23 |
| CHEMBL5559274 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5559259 | — | IC50 | = | 178.4 | nM | 6.75 |
| CHEMBL5558002 | — | IC50 | = | 177.6 | nM | 6.75 |
| CHEMBL3809489 | BEMCENTINIB | IC50 | = | 636.5 | nM | 6.20 |
| CHEMBL5557417 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5512532 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5558655 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5542329 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5523590 | — | IC50 | > | 1000.0 | nM | - |