Assay Detail
Binding
CHEMBL5504735
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Inhibition of MER (unknown origin) expressed in mouse BaF3 cells co-expressing TMEM assessed as inhibition of MER-driven cell proliferation incubated for 72 hrs by MTS assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BaF3 |
| 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 | 34 | 7.59 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5542282 | — | — | 1 | 9.40 |
| CHEMBL5558074 | — | — | 1 | 9.15 |
| CHEMBL5505865 | — | — | 1 | 9.00 |
| CHEMBL5556050 | — | — | 1 | 8.92 |
| CHEMBL5559385 | — | — | 1 | 8.92 |
| CHEMBL5512537 | — | — | 1 | 8.80 |
| CHEMBL5517863 | — | — | 1 | 8.80 |
| CHEMBL5532530 | — | — | 1 | 8.68 |
| CHEMBL5558836 | — | — | 1 | 8.35 |
| CHEMBL5559274 | — | — | 1 | 8.35 |
| CHEMBL5557391 | — | — | 1 | 8.32 |
| CHEMBL5556349 | — | — | 1 | 8.30 |
| CHEMBL5555723 | — | — | 1 | 8.23 |
| CHEMBL5555377 | — | — | 1 | 8.12 |
| CHEMBL5505936 | — | — | 1 | 8.12 |
| CHEMBL5556255 | — | — | 1 | 8.09 |
| CHEMBL5532211 | — | — | 1 | 8.08 |
| CHEMBL5557044 | — | — | 1 | 7.97 |
| CHEMBL5559259 | — | — | 1 | 7.87 |
| CHEMBL5555725 | — | — | 1 | 7.13 |
| CHEMBL5558002 | — | — | 1 | 7.11 |
| CHEMBL3326006 | — | — | 1 | 7.03 |
| CHEMBL5557417 | — | — | 1 | 6.76 |
| CHEMBL5523590 | — | — | 1 | 6.67 |
| CHEMBL5542329 | — | — | 1 | 6.37 |
| CHEMBL5556531 | — | — | 1 | 6.21 |
| CHEMBL5505863 | — | — | 1 | 6.18 |
| CHEMBL5558251 | — | — | 1 | 6.15 |
| CHEMBL3809489 | BEMCENTINIB | 2.0 | 1 | 6.10 |
| CHEMBL5558655 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5542282 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5558074 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5505865 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5556050 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5559385 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5512537 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5517863 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5532530 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5558836 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL5559274 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL5557391 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL5556349 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5555723 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL5555377 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL5505936 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL5556255 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL5532211 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL5557044 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL5559259 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL5555725 | — | IC50 | = | 73.6 | nM | 7.13 |
| CHEMBL5558002 | — | IC50 | = | 77.1 | nM | 7.11 |
| CHEMBL3326006 | — | IC50 | = | 92.4 | nM | 7.03 |
| CHEMBL5557417 | — | IC50 | = | 171.7 | nM | 6.76 |
| CHEMBL5523590 | — | IC50 | = | 211.2 | nM | 6.67 |
| CHEMBL5542329 | — | IC50 | = | 428.0 | nM | 6.37 |
| CHEMBL5556531 | — | IC50 | = | 617.9 | nM | 6.21 |
| CHEMBL5505863 | — | IC50 | = | 658.3 | nM | 6.18 |
| CHEMBL5558251 | — | IC50 | = | 713.0 | nM | 6.15 |
| CHEMBL3809489 | BEMCENTINIB | IC50 | = | 788.1 | nM | 6.10 |
| CHEMBL5558655 | — | IC50 | = | 910.2 | nM | 6.04 |
| CHEMBL5512532 | — | IC50 | = | 1048.0 | nM | 5.98 |
| CHEMBL5505870 | — | IC50 | = | 1139.0 | nM | 5.94 |
| CHEMBL5517877 | — | IC50 | = | 3634.0 | nM | 5.44 |
| CHEMBL1172843 | — | IC50 | > | 10000.0 | nM | - |