Assay Detail
Binding
CHEMBL3875501
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Inhibition of recombinant SUMO-fused MLL1/ASH2L/RBBP5/WDR5 complex histone methyltransferase activity (unknown origin) expressed in Escherichia coli BL21 (DE3) using 10-mer histone H3 peptide as substrate and [3H]-S-adenosyl methionine as cofactor after 2 hrs by scintillation counting method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
High-affinity small molecular blockers of mixed lineage leukemia 1 (MLL1)-WDR5 interaction inhibit MLL1 complex H3K4 methyltransferase activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 6.46 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3798088 | — | — | 1 | 6.52 |
| CHEMBL3883592 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3798088 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3883592 | — | IC50 | = | 400.0 | nM | 6.40 |