Assay Detail
Binding
CHEMBL5366416
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Inhibition of PARP1 (unknown origin) using histone as substrate by ELISA
34
Total Activities
34
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
YCH1899, a Highly Effective Phthalazin-1(2<i>H</i>)-one Derivative That Overcomes Resistance to Prior PARP Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 8.68 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5401127 | — | — | 1 | 10.70 |
| CHEMBL5425729 | — | — | 1 | 9.77 |
| CHEMBL5404605 | — | — | 1 | 9.64 |
| CHEMBL5428376 | — | — | 1 | 9.62 |
| CHEMBL5425393 | — | — | 1 | 9.59 |
| CHEMBL5395197 | — | — | 1 | 9.36 |
| CHEMBL5408163 | — | — | 1 | 9.13 |
| CHEMBL5419303 | — | — | 1 | 9.07 |
| CHEMBL5425070 | — | — | 1 | 9.02 |
| CHEMBL5410501 | — | — | 1 | 9.02 |
| CHEMBL5421957 | — | — | 1 | 9.01 |
| CHEMBL5432616 | — | — | 1 | 8.90 |
| CHEMBL5429957 | — | — | 1 | 8.89 |
| CHEMBL5435418 | — | — | 1 | 8.87 |
| CHEMBL3930624 | FLUZOPARIB | 3.0 | 1 | 8.84 |
| CHEMBL5397203 | — | — | 1 | 8.72 |
| CHEMBL5427132 | — | — | 1 | 8.67 |
| CHEMBL5412306 | — | — | 1 | 8.63 |
| CHEMBL5417924 | — | — | 1 | 8.25 |
| CHEMBL5423216 | — | — | 1 | 8.21 |
| CHEMBL5436154 | — | — | 1 | 8.20 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 8.18 |
| CHEMBL5436989 | — | — | 1 | 8.13 |
| CHEMBL5433982 | — | — | 1 | 8.09 |
| CHEMBL5427638 | — | — | 1 | 8.07 |
| CHEMBL5422190 | — | — | 1 | 7.89 |
| CHEMBL5438131 | — | — | 1 | 7.87 |
| CHEMBL5436743 | — | — | 1 | 7.64 |
| CHEMBL5416682 | — | — | 1 | 7.33 |
| CHEMBL5437055 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5401127 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL5425729 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL5404605 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL5428376 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL5425393 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL5395197 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL5408163 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL5419303 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL5425070 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL5410501 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL5421957 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL5432616 | — | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL5429957 | — | IC50 | = | 1.28 | nM | 8.89 |
| CHEMBL5435418 | — | IC50 | = | 1.35 | nM | 8.87 |
| CHEMBL3930624 | FLUZOPARIB | IC50 | = | 1.46 | nM | 8.84 |
| CHEMBL5397203 | — | IC50 | = | 1.91 | nM | 8.72 |
| CHEMBL5427132 | — | IC50 | = | 2.14 | nM | 8.67 |
| CHEMBL5412306 | — | IC50 | = | 2.33 | nM | 8.63 |
| CHEMBL5417924 | — | IC50 | = | 5.67 | nM | 8.25 |
| CHEMBL5423216 | — | IC50 | = | 6.19 | nM | 8.21 |
| CHEMBL5436154 | — | IC50 | = | 6.34 | nM | 8.20 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 6.65 | nM | 8.18 |
| CHEMBL5436989 | — | IC50 | = | 7.32 | nM | 8.13 |
| CHEMBL5433982 | — | IC50 | = | 8.15 | nM | 8.09 |
| CHEMBL5427638 | — | IC50 | = | 8.49 | nM | 8.07 |
| CHEMBL5422190 | — | IC50 | = | 12.92 | nM | 7.89 |
| CHEMBL5438131 | — | IC50 | = | 13.45 | nM | 7.87 |
| CHEMBL5436743 | — | IC50 | = | 23.05 | nM | 7.64 |
| CHEMBL5416682 | — | IC50 | = | 47.35 | nM | 7.33 |
| CHEMBL5437055 | — | IC50 | = | 61.66 | nM | 7.21 |
| CHEMBL5402698 | — | IC50 | < | 0.001 | nM | - |
| CHEMBL5437176 | — | IC50 | < | 0.001 | nM | - |
| CHEMBL5425913 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL3137320 | TALAZOPARIB | IC50 | - | — | - |