Assay Detail
Binding
CHEMBL3375263
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assay
84
Total Activities
84
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 |
Target
Ubiquitin carboxyl-terminal hydrolase 1/WD repeat-containing protein 48 (CHEMBL3430885) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationship studies of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against nonsmall cell lung cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 84 | 6.06 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3182033 | — | — | 1 | 7.30 |
| CHEMBL3185589 | — | — | 1 | 7.16 |
| CHEMBL3187668 | — | — | 1 | 7.16 |
| CHEMBL3182437 | — | — | 1 | 7.12 |
| CHEMBL3183916 | — | — | 1 | 7.10 |
| CHEMBL3182908 | — | — | 1 | 7.10 |
| CHEMBL3181856 | — | — | 1 | 7.10 |
| CHEMBL3182895 | — | — | 1 | 7.05 |
| CHEMBL3356519 | — | — | 1 | 7.00 |
| CHEMBL3181906 | — | — | 1 | 6.96 |
| CHEMBL3188490 | — | — | 1 | 6.96 |
| CHEMBL3189120 | — | — | 1 | 6.96 |
| CHEMBL3356521 | — | — | 1 | 6.92 |
| CHEMBL3183277 | — | — | 1 | 6.92 |
| CHEMBL3185384 | — | — | 1 | 6.92 |
| CHEMBL3186151 | — | — | 1 | 6.89 |
| CHEMBL3356518 | — | — | 1 | 6.85 |
| CHEMBL3187225 | — | — | 1 | 6.85 |
| CHEMBL3187391 | — | — | 1 | 6.82 |
| CHEMBL3183657 | — | — | 1 | 6.80 |
| CHEMBL3187106 | — | — | 1 | 6.75 |
| CHEMBL3356515 | — | — | 1 | 6.75 |
| CHEMBL3186327 | — | — | 1 | 6.75 |
| CHEMBL3182461 | — | — | 1 | 6.72 |
| CHEMBL3356522 | — | — | 1 | 6.72 |
| CHEMBL3187128 | — | — | 1 | 6.68 |
| CHEMBL3185465 | — | — | 1 | 6.58 |
| CHEMBL3186525 | — | — | 1 | 6.57 |
| CHEMBL3187675 | — | — | 1 | 6.55 |
| CHEMBL3356514 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3182033 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3185589 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3187668 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3182437 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3183916 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3182908 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3181856 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3182895 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3356519 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3181906 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3188490 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3189120 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3185384 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3183277 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3356521 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3186151 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3356518 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3187225 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3187391 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3183657 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3187106 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3356515 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3186327 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3182461 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3356522 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3187128 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3185465 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3186525 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3187675 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3356514 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3188392 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3186898 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3356517 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL3356520 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL3183116 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL3184137 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3189092 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL3182829 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL3184172 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL3183200 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3187556 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3184249 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3188647 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3188953 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3356111 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3187140 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3184785 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3356110 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3356109 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3187834 | — | IC50 | = | 2900.0 | nM | 5.54 |