Assay Detail
Binding
CHEMBL3130541
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human His-tagged menin-biotinylated MLL (4 to 15) interaction after 1 hr by HTRF assay
29
Total Activities
29
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
High-affinity small-molecule inhibitors of the menin-mixed lineage leukemia (MLL) interaction closely mimic a natural protein-protein interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.16 | 7.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3126198 | — | — | 1 | 7.25 |
| CHEMBL3126196 | — | — | 1 | 7.17 |
| CHEMBL3126197 | — | — | 1 | 7.09 |
| CHEMBL3126194 | — | — | 1 | 7.05 |
| CHEMBL3126199 | — | — | 1 | 6.94 |
| CHEMBL3126200 | — | — | 1 | 6.83 |
| CHEMBL3126188 | — | — | 1 | 6.71 |
| CHEMBL3126201 | — | — | 1 | 6.71 |
| CHEMBL3126193 | — | — | 1 | 6.65 |
| CHEMBL3126190 | — | — | 1 | 6.65 |
| CHEMBL3126192 | — | — | 1 | 6.62 |
| CHEMBL3126187 | — | — | 1 | 6.57 |
| CHEMBL3126191 | — | — | 1 | 6.52 |
| CHEMBL3126185 | — | — | 1 | 6.41 |
| CHEMBL3126189 | — | — | 1 | 6.36 |
| CHEMBL3124953 | — | — | 1 | 6.28 |
| CHEMBL3126195 | — | — | 1 | 5.85 |
| CHEMBL3126186 | — | — | 1 | 5.77 |
| CHEMBL3126184 | — | — | 1 | 5.40 |
| CHEMBL3126183 | — | — | 1 | 5.39 |
| CHEMBL3126202 | — | — | 1 | 4.97 |
| CHEMBL3126182 | — | — | 1 | 4.95 |
| CHEMBL1438422 | — | — | 1 | 4.89 |
| CHEMBL3126181 | — | — | 1 | 4.82 |
| CHEMBL1348295 | — | — | 1 | 4.11 |
| CHEMBL3126180 | — | — | 1 | - |
| CHEMBL3126179 | — | — | 1 | - |
| CHEMBL17345 | — | — | 1 | - |
| CHEMBL3126203 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3126198 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3126196 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3126197 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3126194 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3126199 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL3126200 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL3126188 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL3126201 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL3126193 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL3126190 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL3126192 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL3126187 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3126191 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL3126185 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3126189 | — | IC50 | = | 436.0 | nM | 6.36 |
| CHEMBL3124953 | — | IC50 | = | 529.0 | nM | 6.28 |
| CHEMBL3126195 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3126186 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3126184 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3126183 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL3126202 | — | IC50 | = | 10800.0 | nM | 4.97 |
| CHEMBL3126182 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL1438422 | — | IC50 | = | 12800.0 | nM | 4.89 |
| CHEMBL3126181 | — | IC50 | = | 15300.0 | nM | 4.82 |
| CHEMBL1348295 | — | IC50 | = | 77000.0 | nM | 4.11 |
| CHEMBL3126180 | — | IC50 | = | 295000.0 | nM | - |
| CHEMBL3126179 | — | IC50 | = | 234000.0 | nM | - |
| CHEMBL17345 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3126203 | — | IC50 | = | 205000.0 | nM | - |