Assay Detail
Binding
CHEMBL5539300
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Inhibition of MLL1/WDR5 (unknown origin) protein-protein interaction incubated for 60 mins by HTRF analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
Discovery and Optimization of WDR5 Inhibitors via Cascade Deoxyribonucleic Acid-Encoded Library Selection Approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.42 | 8.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4588661 | — | — | 1 | 8.17 |
| CHEMBL5562523 | — | — | 1 | 8.07 |
| CHEMBL5573350 | — | — | 1 | 8.01 |
| CHEMBL5579746 | — | — | 1 | 7.95 |
| CHEMBL5572054 | — | — | 1 | 7.81 |
| CHEMBL5565914 | — | — | 1 | 7.76 |
| CHEMBL5576035 | — | — | 1 | 7.73 |
| CHEMBL5575058 | — | — | 1 | 7.60 |
| CHEMBL5572530 | — | — | 1 | 7.57 |
| CHEMBL5571097 | — | — | 1 | 7.49 |
| CHEMBL5579685 | — | — | 1 | 7.40 |
| CHEMBL5595245 | — | — | 1 | 7.39 |
| CHEMBL5592145 | — | — | 1 | 7.38 |
| CHEMBL5590145 | — | — | 1 | 7.30 |
| CHEMBL5591718 | — | — | 1 | 7.12 |
| CHEMBL5574146 | — | — | 1 | 7.07 |
| CHEMBL5579747 | — | — | 1 | 6.83 |
| CHEMBL5562904 | — | — | 1 | 6.66 |
| CHEMBL5573257 | — | — | 1 | 6.62 |
| CHEMBL5574810 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4588661 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL5562523 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL5573350 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL5579746 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL5572054 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL5565914 | — | IC50 | = | 17.2 | nM | 7.76 |
| CHEMBL5576035 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL5575058 | — | IC50 | = | 25.2 | nM | 7.60 |
| CHEMBL5572530 | — | IC50 | = | 26.9 | nM | 7.57 |
| CHEMBL5571097 | — | IC50 | = | 32.4 | nM | 7.49 |
| CHEMBL5579685 | — | IC50 | = | 39.5 | nM | 7.40 |
| CHEMBL5595245 | — | IC50 | = | 40.5 | nM | 7.39 |
| CHEMBL5592145 | — | IC50 | = | 41.6 | nM | 7.38 |
| CHEMBL5590145 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5591718 | — | IC50 | = | 75.8 | nM | 7.12 |
| CHEMBL5574146 | — | IC50 | = | 84.6 | nM | 7.07 |
| CHEMBL5579747 | — | IC50 | = | 148.7 | nM | 6.83 |
| CHEMBL5562904 | — | IC50 | = | 220.7 | nM | 6.66 |
| CHEMBL5573257 | — | IC50 | = | 239.2 | nM | 6.62 |
| CHEMBL5574810 | — | IC50 | = | 319.0 | nM | 6.50 |