Assay Detail
Binding
CHEMBL4186847
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MLL1 binding to N-terminal His-tagged WRD5 23 deletion mutant (24 to 334 residues) (unknown origin) expressed in Escherichia coli Rosetta 2 (DE3) pLysS cells by fluorescence polarization assay
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Histone-lysine N-methyltransferase 2A (CHEMBL1293299) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Targeting protein-protein interaction between MLL1 and reciprocal proteins for leukemia therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.50 | 8.62 |
| Ki | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3883592 | — | — | 2 | 8.62 |
| CHEMBL3799591 | — | — | 2 | 8.54 |
| CHEMBL3957384 | — | — | 2 | 8.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3883592 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3799591 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3957384 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3799591 | — | Ki | < | 1.0 | nM | - |
| CHEMBL3883592 | — | Ki | < | 1.0 | nM | - |
| CHEMBL3957384 | — | Ki | < | 1.0 | nM | - |