Assay Detail
Binding
CHEMBL5373000
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of Biotin-p53K381acK382me2 from N-terminal his6-tagged 53BP1 (1484 to 1603 residues) (unknown origin) expressed in Rosetta2 BL21 (DE3) pLysS competent cells by TR-FRET assay
37
Total Activities
37
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
Discovery of a 53BP1 Small Molecule Antagonist Using a Focused DNA-Encoded Library Screen.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 5.17 | 6.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5439383 | — | — | 1 | 6.34 |
| CHEMBL5403027 | — | — | 1 | 6.33 |
| CHEMBL5402301 | — | — | 1 | 6.07 |
| CHEMBL5431269 | — | — | 1 | 5.89 |
| CHEMBL5433157 | — | — | 1 | 5.85 |
| CHEMBL5415556 | — | — | 1 | 5.72 |
| CHEMBL5423332 | — | — | 1 | 5.66 |
| CHEMBL5440895 | — | — | 1 | 5.47 |
| CHEMBL5421180 | — | — | 1 | 5.42 |
| CHEMBL5430714 | — | — | 1 | 5.39 |
| CHEMBL5440393 | — | — | 1 | 5.30 |
| CHEMBL5397384 | — | — | 1 | 5.25 |
| CHEMBL5400477 | — | — | 1 | 5.24 |
| CHEMBL5397306 | — | — | 1 | 5.23 |
| CHEMBL5395836 | — | — | 1 | 5.18 |
| CHEMBL5428966 | — | — | 1 | 5.17 |
| CHEMBL5429915 | — | — | 1 | 5.13 |
| CHEMBL5412662 | — | — | 1 | 5.11 |
| CHEMBL5418978 | — | — | 1 | 5.09 |
| CHEMBL5438168 | — | — | 1 | 5.00 |
| CHEMBL5398002 | — | — | 1 | 5.00 |
| CHEMBL5409275 | — | — | 1 | 4.96 |
| CHEMBL5437926 | — | — | 1 | 4.92 |
| CHEMBL5439940 | — | — | 1 | 4.85 |
| CHEMBL5416576 | — | — | 1 | 4.82 |
| CHEMBL5440782 | — | — | 1 | 4.82 |
| CHEMBL5423187 | — | — | 1 | 4.75 |
| CHEMBL5431260 | — | — | 1 | 4.66 |
| CHEMBL5431898 | — | — | 1 | 4.55 |
| CHEMBL5412159 | — | — | 1 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5439383 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL5403027 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5402301 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL5431269 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5433157 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5415556 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5423332 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5440895 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL5421180 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL5430714 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL5440393 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5397384 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL5400477 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL5397306 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL5395836 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL5428966 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL5429915 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL5412662 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL5418978 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL5398002 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5438168 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5409275 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL5437926 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL5439940 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL5416576 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL5440782 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL5423187 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL5431260 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL5431898 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL5412159 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL5420747 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL5416659 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL5434158 | — | IC50 | = | 83000.0 | nM | 4.08 |
| CHEMBL5419460 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL5406735 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5441134 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5414804 | — | IC50 | > | 100000.0 | nM | - |