Assay Detail
Binding
CHEMBL5040191
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Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay
20
Total Activities
20
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 M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 8.42 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5076146 | — | — | 1 | 8.77 |
| CHEMBL5085940 | — | — | 1 | 8.60 |
| CHEMBL5094183 | — | — | 1 | 8.57 |
| CHEMBL5081367 | — | — | 1 | 8.57 |
| CHEMBL5079678 | — | — | 1 | 8.55 |
| CHEMBL5071412 | — | — | 1 | 8.55 |
| CHEMBL5090509 | — | — | 1 | 8.54 |
| CHEMBL5079839 | — | — | 1 | 8.52 |
| CHEMBL5088651 | — | — | 1 | 8.49 |
| CHEMBL5088354 | — | — | 1 | 8.47 |
| CHEMBL5082413 | — | — | 1 | 8.46 |
| CHEMBL5075855 | — | — | 1 | 8.46 |
| CHEMBL5086858 | — | — | 1 | 8.44 |
| CHEMBL5083305 | — | — | 1 | 8.43 |
| CHEMBL5081374 | — | — | 1 | 8.42 |
| CHEMBL5087485 | — | — | 1 | 8.40 |
| CHEMBL5081163 | — | — | 1 | 8.38 |
| CHEMBL5085064 | — | — | 1 | 8.34 |
| CHEMBL5076001 | — | — | 1 | 8.16 |
| CHEMBL5084863 | — | — | 1 | 7.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5076146 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5085940 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5094183 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5081367 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5079678 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5071412 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5090509 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5079839 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5088651 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5088354 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5082413 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5075855 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5086858 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5083305 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5081374 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5087485 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5081163 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5085064 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5076001 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL5084863 | — | IC50 | = | 42.4 | nM | 7.37 |