Assay Detail
Functional
CHEMBL1109150
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Antiproliferative activity against human A2780 cells assessed as intracellular ATP level after 72 hrs by luminometry
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A2780 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 47 | 6.03 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1094408 | NMS-1286937 | — | 1 | 8.05 |
| CHEMBL1099106 | — | — | 1 | 7.40 |
| CHEMBL1094322 | — | — | 1 | 7.30 |
| CHEMBL1099105 | — | — | 1 | 7.05 |
| CHEMBL1094401 | — | — | 1 | 7.00 |
| CHEMBL1095717 | — | — | 1 | 6.84 |
| CHEMBL1097429 | — | — | 1 | 6.60 |
| CHEMBL1094735 | — | — | 1 | 6.51 |
| CHEMBL559845 | — | — | 1 | 6.30 |
| CHEMBL1094402 | — | — | 1 | 6.26 |
| CHEMBL1095771 | — | — | 1 | 6.17 |
| CHEMBL1095716 | — | — | 1 | 6.12 |
| CHEMBL1094477 | — | — | 1 | 6.10 |
| CHEMBL1098058 | — | — | 1 | 6.05 |
| CHEMBL1094135 | — | — | 1 | 6.03 |
| CHEMBL1095448 | — | — | 1 | 5.98 |
| CHEMBL1097424 | — | — | 1 | 5.83 |
| CHEMBL1094811 | — | — | 1 | 5.78 |
| CHEMBL1095132 | — | — | 1 | 5.71 |
| CHEMBL1098060 | — | — | 1 | 5.59 |
| CHEMBL562104 | — | — | 1 | 5.58 |
| CHEMBL1095709 | — | — | 1 | 5.56 |
| CHEMBL1098059 | — | — | 1 | 5.55 |
| CHEMBL1097022 | — | — | 1 | 5.54 |
| CHEMBL1094810 | — | — | 1 | 5.46 |
| CHEMBL559639 | — | — | 1 | 5.42 |
| CHEMBL1097373 | — | — | 1 | 5.41 |
| CHEMBL1098057 | — | — | 1 | 5.33 |
| CHEMBL1094820 | — | — | 1 | 5.23 |
| CHEMBL1094478 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1094408 | NMS-1286937 | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1099106 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1094322 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1099105 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1094401 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1095717 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL1097429 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1094735 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL559845 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1094402 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1095771 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL1095716 | — | IC50 | = | 762.0 | nM | 6.12 |
| CHEMBL1094477 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL1098058 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL1094135 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL1095448 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL1097424 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL1094811 | — | IC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL1095132 | — | IC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL1098060 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL562104 | — | IC50 | = | 2630.0 | nM | 5.58 |
| CHEMBL1095709 | — | IC50 | = | 2750.0 | nM | 5.56 |
| CHEMBL1098059 | — | IC50 | = | 2790.0 | nM | 5.55 |
| CHEMBL1097022 | — | IC50 | = | 2920.0 | nM | 5.54 |
| CHEMBL1094810 | — | IC50 | = | 3490.0 | nM | 5.46 |
| CHEMBL559639 | — | IC50 | = | 3820.0 | nM | 5.42 |
| CHEMBL1097373 | — | IC50 | = | 3930.0 | nM | 5.41 |
| CHEMBL1098057 | — | IC50 | = | 4710.0 | nM | 5.33 |
| CHEMBL1094820 | — | IC50 | = | 5850.0 | nM | 5.23 |
| CHEMBL1094478 | — | IC50 | = | 6860.0 | nM | 5.16 |
| CHEMBL1095457 | — | IC50 | = | 7540.0 | nM | 5.12 |
| CHEMBL1094816 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL1097071 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1094400 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL563028 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1099104 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1095772 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1094484 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1094815 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1094817 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1096095 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1094488 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1094821 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1094822 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1097374 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1096028 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL563150 | — | IC50 | > | 10000.0 | nM | - |