Assay Detail
Functional
CHEMBL5373885
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity against human MX1 cells harbouring BRCA1 and BRCA2 assessed as inhibition of cell growth measured after 72 hrs by MTT assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MX1 |
| Confidence | 1 — Organism |
| 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 | 35 | 7.85 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5406119 | — | — | 1 | 9.19 |
| CHEMBL5423934 | — | — | 1 | 8.93 |
| CHEMBL5434732 | — | — | 1 | 8.78 |
| CHEMBL5418896 | — | — | 1 | 8.51 |
| CHEMBL5423161 | — | — | 1 | 8.44 |
| CHEMBL5437813 | — | — | 1 | 8.38 |
| CHEMBL5423072 | — | — | 1 | 8.31 |
| CHEMBL5416806 | — | — | 1 | 8.24 |
| CHEMBL5400153 | — | — | 1 | 8.18 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 8.08 |
| CHEMBL5421335 | — | — | 1 | 8.03 |
| CHEMBL5404171 | — | — | 1 | 7.98 |
| CHEMBL5406001 | — | — | 1 | 7.91 |
| CHEMBL5439635 | — | — | 1 | 7.88 |
| CHEMBL5419639 | — | — | 1 | 7.83 |
| CHEMBL5427496 | — | — | 1 | 7.78 |
| CHEMBL5421933 | — | — | 1 | 7.73 |
| CHEMBL5394020 | — | — | 1 | 7.70 |
| CHEMBL5432851 | — | — | 1 | 7.65 |
| CHEMBL5419831 | — | — | 1 | 7.63 |
| CHEMBL5397373 | — | — | 1 | 7.63 |
| CHEMBL5413070 | — | — | 1 | 7.63 |
| CHEMBL5399361 | — | — | 1 | 7.54 |
| CHEMBL5428217 | — | — | 1 | 7.51 |
| CHEMBL5414478 | — | — | 1 | 7.49 |
| CHEMBL5432860 | — | — | 1 | 7.47 |
| CHEMBL5421189 | — | — | 1 | 7.35 |
| CHEMBL5434897 | — | — | 1 | 7.34 |
| CHEMBL5408420 | — | — | 1 | 7.29 |
| CHEMBL5414994 | — | — | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5406119 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL5423934 | — | IC50 | = | 1.18 | nM | 8.93 |
| CHEMBL5434732 | — | IC50 | = | 1.67 | nM | 8.78 |
| CHEMBL5418896 | — | IC50 | = | 3.12 | nM | 8.51 |
| CHEMBL5423161 | — | IC50 | = | 3.65 | nM | 8.44 |
| CHEMBL5437813 | — | IC50 | = | 4.15 | nM | 8.38 |
| CHEMBL5423072 | — | IC50 | = | 4.88 | nM | 8.31 |
| CHEMBL5416806 | — | IC50 | = | 5.79 | nM | 8.24 |
| CHEMBL5400153 | — | IC50 | = | 6.54 | nM | 8.18 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 8.26 | nM | 8.08 |
| CHEMBL5421335 | — | IC50 | = | 9.39 | nM | 8.03 |
| CHEMBL5404171 | — | IC50 | = | 10.45 | nM | 7.98 |
| CHEMBL5406001 | — | IC50 | = | 12.43 | nM | 7.91 |
| CHEMBL5439635 | — | IC50 | = | 13.24 | nM | 7.88 |
| CHEMBL5419639 | — | IC50 | = | 14.94 | nM | 7.83 |
| CHEMBL5427496 | — | IC50 | = | 16.46 | nM | 7.78 |
| CHEMBL5421933 | — | IC50 | = | 18.58 | nM | 7.73 |
| CHEMBL5394020 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5432851 | — | IC50 | = | 22.38 | nM | 7.65 |
| CHEMBL5419831 | — | IC50 | = | 23.22 | nM | 7.63 |
| CHEMBL5397373 | — | IC50 | = | 23.22 | nM | 7.63 |
| CHEMBL5413070 | — | IC50 | = | 23.33 | nM | 7.63 |
| CHEMBL5399361 | — | IC50 | = | 28.49 | nM | 7.54 |
| CHEMBL5428217 | — | IC50 | = | 30.92 | nM | 7.51 |
| CHEMBL5414478 | — | IC50 | = | 32.6 | nM | 7.49 |
| CHEMBL5432860 | — | IC50 | = | 33.85 | nM | 7.47 |
| CHEMBL5421189 | — | IC50 | = | 44.99 | nM | 7.35 |
| CHEMBL5434897 | — | IC50 | = | 46.15 | nM | 7.34 |
| CHEMBL5408420 | — | IC50 | = | 50.98 | nM | 7.29 |
| CHEMBL5414994 | — | IC50 | = | 60.16 | nM | 7.22 |
| CHEMBL5419161 | — | IC50 | = | 61.29 | nM | 7.21 |
| CHEMBL5437947 | — | IC50 | = | 331.0 | nM | 6.48 |
| CHEMBL5393999 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL5428859 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL5395127 | — | IC50 | > | 100.0 | nM | - |