Assay Detail
Binding
CHEMBL4774494
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Inhibition of Menin-MLL protein-protein interaction (unknown origin) preincubated for 1 hr in presence of FLSN-MLL4-43 peptide followed by compound addition and measured after 1 hr by fluorescence polarization assay
10
Total Activities
10
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
Menin/Histone-lysine N-methyltransferase MLL (CHEMBL2093861) ↗| Type | PROTEIN-PROTEIN INTERACTION |
| Organism | Homo sapiens |
Publication
Covalent and noncovalent constraints yield a figure eight-like conformation of a peptide inhibiting the menin-MLL interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.93 | 8.63 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4788214 | — | — | 1 | 8.63 |
| CHEMBL4777030 | — | — | 1 | 8.34 |
| CHEMBL4782745 | — | — | 1 | 7.85 |
| CHEMBL2314823 | — | — | 1 | 7.31 |
| CHEMBL4796292 | — | — | 1 | 7.24 |
| CHEMBL4796544 | — | — | 1 | 6.25 |
| CHEMBL4788240 | — | — | 1 | 6.18 |
| CHEMBL4795122 | — | — | 1 | 6.11 |
| CHEMBL4794800 | — | — | 1 | 5.91 |
| CHEMBL4797084 | — | — | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4788214 | — | IC50 | = | 2.35 | nM | 8.63 |
| CHEMBL4777030 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4782745 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2314823 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4796292 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4796544 | — | IC50 | = | 569.0 | nM | 6.25 |
| CHEMBL4788240 | — | IC50 | = | 657.0 | nM | 6.18 |
| CHEMBL4795122 | — | IC50 | = | 777.0 | nM | 6.11 |
| CHEMBL4794800 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL4797084 | — | IC50 | = | 3588.0 | nM | 5.45 |