Assay Detail
Binding
CHEMBL4683559
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Inhibition of MLL1-WDR5 interaction in human MV4-11 cells assessed as reduction in MLL1 binding to WDR5 WIN site by 5-FAM probe based fluorescence polarization assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MV4-11 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Histone-lysine N-methyltransferase 2A/WDR5 (CHEMBL3883320) ↗| Type | PROTEIN-PROTEIN INTERACTION |
| Organism | Homo sapiens |
Publication
Proton pump inhibitors selectively suppress MLL rearranged leukemia cells via disrupting MLL1-WDR5 protein-protein interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.72 | 6.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1219 | RABEPRAZOLE | 4.0 | 1 | 6.31 |
| CHEMBL10184 | — | — | 1 | 5.96 |
| CHEMBL4741681 | — | — | 1 | 5.77 |
| CHEMBL1503 | OMEPRAZOLE | 4.0 | 1 | 5.77 |
| CHEMBL1201320 | ESOMEPRAZOLE | 4.0 | 1 | 5.75 |
| CHEMBL1201863 | DEXLANSOPRAZOLE | 4.0 | 1 | 5.24 |
| CHEMBL480 | LANSOPRAZOLE | 4.0 | 1 | 5.23 |
| CHEMBL4798671 | — | — | 1 | - |
| CHEMBL4783399 | — | — | 1 | - |
| CHEMBL4789713 | — | — | 1 | - |
| CHEMBL50030 | — | — | 1 | - |
| CHEMBL4792444 | — | — | 1 | - |
| CHEMBL4741363 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1219 | RABEPRAZOLE | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL10184 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4741681 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1503 | OMEPRAZOLE | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1201320 | ESOMEPRAZOLE | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1201863 | DEXLANSOPRAZOLE | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL480 | LANSOPRAZOLE | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4798671 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4783399 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4789713 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL50030 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4792444 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4741363 | — | IC50 | > | 100000.0 | nM | - |