Assay Detail
Binding
CHEMBL5373883
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant PARP1 expressed in Escherichia coli BL21(DE3) incubated for 1 hr by ELISA assay
36
Total Activities
36
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 Quinazoline-2,4(1<i>H</i>,3<i>H</i>)-dione Derivatives Containing a Piperizinone Moiety as Potent PARP-1/2 Inhibitors─Design, Synthesis, <i>In Vivo</i> Antitumor Activity, and X-ray Crystal Structure Analysis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 8.37 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5403305 | — | — | 1 | 9.03 |
| CHEMBL5423072 | — | — | 1 | 8.99 |
| CHEMBL5439635 | — | — | 1 | 8.85 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 8.68 |
| CHEMBL5437813 | — | — | 1 | 8.68 |
| CHEMBL5393999 | — | — | 1 | 8.62 |
| CHEMBL5421335 | — | — | 1 | 8.62 |
| CHEMBL5397373 | — | — | 1 | 8.61 |
| CHEMBL5418896 | — | — | 1 | 8.60 |
| CHEMBL5437947 | — | — | 1 | 8.57 |
| CHEMBL5394020 | — | — | 1 | 8.56 |
| CHEMBL5416806 | — | — | 1 | 8.54 |
| CHEMBL5406001 | — | — | 1 | 8.52 |
| CHEMBL5404171 | — | — | 1 | 8.52 |
| CHEMBL5419831 | — | — | 1 | 8.46 |
| CHEMBL5423934 | — | — | 1 | 8.44 |
| CHEMBL5432860 | — | — | 1 | 8.43 |
| CHEMBL5408420 | — | — | 1 | 8.42 |
| CHEMBL5421933 | — | — | 1 | 8.42 |
| CHEMBL5406119 | — | — | 1 | 8.41 |
| CHEMBL5395127 | — | — | 1 | 8.38 |
| CHEMBL5428859 | — | — | 1 | 8.36 |
| CHEMBL5432851 | — | — | 1 | 8.33 |
| CHEMBL5423161 | — | — | 1 | 8.31 |
| CHEMBL5419161 | — | — | 1 | 8.31 |
| CHEMBL5428217 | — | — | 1 | 8.30 |
| CHEMBL5413070 | — | — | 1 | 8.12 |
| CHEMBL5434732 | — | — | 1 | 8.05 |
| CHEMBL5421189 | — | — | 1 | 8.05 |
| CHEMBL5419639 | — | — | 1 | 8.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5403305 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL5423072 | — | IC50 | = | 1.02 | nM | 8.99 |
| CHEMBL5439635 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 2.09 | nM | 8.68 |
| CHEMBL5437813 | — | IC50 | = | 2.08 | nM | 8.68 |
| CHEMBL5393999 | — | IC50 | = | 2.39 | nM | 8.62 |
| CHEMBL5421335 | — | IC50 | = | 2.38 | nM | 8.62 |
| CHEMBL5397373 | — | IC50 | = | 2.46 | nM | 8.61 |
| CHEMBL5418896 | — | IC50 | = | 2.54 | nM | 8.60 |
| CHEMBL5437947 | — | IC50 | = | 2.71 | nM | 8.57 |
| CHEMBL5394020 | — | IC50 | = | 2.72 | nM | 8.56 |
| CHEMBL5416806 | — | IC50 | = | 2.85 | nM | 8.54 |
| CHEMBL5406001 | — | IC50 | = | 3.03 | nM | 8.52 |
| CHEMBL5404171 | — | IC50 | = | 3.02 | nM | 8.52 |
| CHEMBL5419831 | — | IC50 | = | 3.45 | nM | 8.46 |
| CHEMBL5423934 | — | IC50 | = | 3.67 | nM | 8.44 |
| CHEMBL5432860 | — | IC50 | = | 3.76 | nM | 8.43 |
| CHEMBL5421933 | — | IC50 | = | 3.79 | nM | 8.42 |
| CHEMBL5408420 | — | IC50 | = | 3.81 | nM | 8.42 |
| CHEMBL5406119 | — | IC50 | = | 3.86 | nM | 8.41 |
| CHEMBL5395127 | — | IC50 | = | 4.18 | nM | 8.38 |
| CHEMBL5428859 | — | IC50 | = | 4.33 | nM | 8.36 |
| CHEMBL5432851 | — | IC50 | = | 4.68 | nM | 8.33 |
| CHEMBL5423161 | — | IC50 | = | 4.92 | nM | 8.31 |
| CHEMBL5419161 | — | IC50 | = | 4.86 | nM | 8.31 |
| CHEMBL5428217 | — | IC50 | = | 5.06 | nM | 8.30 |
| CHEMBL5413070 | — | IC50 | = | 7.59 | nM | 8.12 |
| CHEMBL5434732 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5421189 | — | IC50 | = | 8.88 | nM | 8.05 |
| CHEMBL5419639 | — | IC50 | = | 9.75 | nM | 8.01 |
| CHEMBL5400153 | — | IC50 | = | 9.85 | nM | 8.01 |
| CHEMBL5414478 | — | IC50 | = | 9.85 | nM | 8.01 |
| CHEMBL5427496 | — | IC50 | = | 11.81 | nM | 7.93 |
| CHEMBL5399361 | — | IC50 | = | 15.52 | nM | 7.81 |
| CHEMBL5414994 | — | IC50 | = | 17.05 | nM | 7.77 |
| CHEMBL5434897 | — | IC50 | = | 17.2 | nM | 7.76 |