Assay Detail
Binding
CHEMBL3801642
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Binding affinity to human poly His-tagged WDR5 (1 to 334 residues) expressed in Escherichia coli BL21(DE3)-V2R-pRARE2 cells by surface plasmon resonance analysis
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 14 | 6.98 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3798846 | — | — | 1 | 7.52 |
| CHEMBL3799608 | — | — | 1 | 7.52 |
| CHEMBL3799704 | — | — | 1 | 7.40 |
| CHEMBL3798198 | — | — | 1 | 7.40 |
| CHEMBL3799127 | — | — | 1 | 7.40 |
| CHEMBL3799275 | — | — | 1 | 7.30 |
| CHEMBL3799840 | — | — | 1 | 7.30 |
| CHEMBL3800054 | — | — | 1 | 7.30 |
| CHEMBL3797967 | — | — | 1 | 6.68 |
| CHEMBL3798578 | — | — | 1 | 6.48 |
| CHEMBL3797611 | — | — | 1 | 6.47 |
| CHEMBL2337032 | — | — | 1 | 6.42 |
| CHEMBL3800271 | — | — | 1 | 6.41 |
| CHEMBL3798573 | — | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3798846 | — | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL3799608 | — | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL3799704 | — | Kd | = | 40.0 | nM | 7.40 |
| CHEMBL3798198 | — | Kd | = | 40.0 | nM | 7.40 |
| CHEMBL3799127 | — | Kd | = | 40.0 | nM | 7.40 |
| CHEMBL3799275 | — | Kd | = | 50.0 | nM | 7.30 |
| CHEMBL3799840 | — | Kd | = | 50.0 | nM | 7.30 |
| CHEMBL3800054 | — | Kd | = | 50.0 | nM | 7.30 |
| CHEMBL3797967 | — | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL3798578 | — | Kd | = | 330.0 | nM | 6.48 |
| CHEMBL3797611 | — | Kd | = | 340.0 | nM | 6.47 |
| CHEMBL2337032 | — | Kd | = | 380.0 | nM | 6.42 |
| CHEMBL3800271 | — | Kd | = | 390.0 | nM | 6.41 |
| CHEMBL3798573 | — | Kd | = | 720.0 | nM | 6.14 |