Assay Detail
Binding
CHEMBL4832186
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Displacement of 10mer-Thr-FAM probe from WDR5 (unknown origin) incubated for 30 mins by fluorescence polarizaton assay
25
Total Activities
25
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 a potent MLL1 and WDR5 protein-protein interaction inhibitor with in vivo antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.31 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4845887 | — | — | 1 | 8.19 |
| CHEMBL3884329 | — | — | 1 | 8.12 |
| CHEMBL4861912 | — | — | 1 | 8.07 |
| CHEMBL4851969 | — | — | 1 | 8.05 |
| CHEMBL4869658 | — | — | 1 | 8.05 |
| CHEMBL4852951 | — | — | 1 | 7.95 |
| CHEMBL4852048 | — | — | 1 | 7.80 |
| CHEMBL4863061 | — | — | 1 | 7.80 |
| CHEMBL4852196 | — | — | 1 | 7.69 |
| CHEMBL4850959 | — | — | 1 | 7.47 |
| CHEMBL4864032 | — | — | 1 | 7.39 |
| CHEMBL4847277 | — | — | 1 | 7.25 |
| CHEMBL4868412 | — | — | 1 | 7.22 |
| CHEMBL4868706 | — | — | 1 | 7.17 |
| CHEMBL3884212 | — | — | 1 | 7.16 |
| CHEMBL4868755 | — | — | 1 | 7.14 |
| CHEMBL4847340 | — | — | 1 | 7.03 |
| CHEMBL4857312 | — | — | 1 | 7.02 |
| CHEMBL4878567 | — | — | 1 | 7.00 |
| CHEMBL4877455 | — | — | 1 | 6.90 |
| CHEMBL4852501 | — | — | 1 | 6.83 |
| CHEMBL4859991 | — | — | 1 | 6.75 |
| CHEMBL4846292 | — | — | 1 | 6.41 |
| CHEMBL4853161 | — | — | 1 | 6.35 |
| CHEMBL4866458 | — | — | 1 | 5.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4845887 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3884329 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4861912 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4851969 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4869658 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4852951 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL4852048 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL4863061 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL4852196 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL4850959 | — | IC50 | = | 33.9 | nM | 7.47 |
| CHEMBL4864032 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4847277 | — | IC50 | = | 55.6 | nM | 7.25 |
| CHEMBL4868412 | — | IC50 | = | 59.7 | nM | 7.22 |
| CHEMBL4868706 | — | IC50 | = | 67.8 | nM | 7.17 |
| CHEMBL3884212 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4868755 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4847340 | — | IC50 | = | 93.5 | nM | 7.03 |
| CHEMBL4857312 | — | IC50 | = | 95.3 | nM | 7.02 |
| CHEMBL4878567 | — | IC50 | = | 98.8 | nM | 7.00 |
| CHEMBL4877455 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4852501 | — | IC50 | = | 147.9 | nM | 6.83 |
| CHEMBL4859991 | — | IC50 | = | 179.4 | nM | 6.75 |
| CHEMBL4846292 | — | IC50 | = | 390.2 | nM | 6.41 |
| CHEMBL4853161 | — | IC50 | = | 443.8 | nM | 6.35 |
| CHEMBL4866458 | — | IC50 | = | 1036.0 | nM | 5.99 |