Assay Detail
Binding
CHEMBL1109145
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Inhibition of CDK2/Cyclin A assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Cyclin-dependent kinase 2/cyclin A (CHEMBL2094128) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 | 7.24 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1094401 | — | — | 1 | 8.70 |
| CHEMBL1099105 | — | — | 1 | 8.70 |
| CHEMBL1099106 | — | — | 1 | 8.70 |
| CHEMBL559845 | — | — | 1 | 8.70 |
| CHEMBL1097429 | — | — | 1 | 8.52 |
| CHEMBL1098060 | — | — | 1 | 8.52 |
| CHEMBL1094477 | — | — | 1 | 8.52 |
| CHEMBL1094322 | — | — | 1 | 8.40 |
| CHEMBL1095709 | — | — | 1 | 8.30 |
| CHEMBL1095448 | — | — | 1 | 8.30 |
| CHEMBL1094811 | — | — | 1 | 8.30 |
| CHEMBL1097424 | — | — | 1 | 8.22 |
| CHEMBL1095771 | — | — | 1 | 8.15 |
| CHEMBL1097022 | — | — | 1 | 8.15 |
| CHEMBL1094402 | — | — | 1 | 8.15 |
| CHEMBL1095132 | — | — | 1 | 7.85 |
| CHEMBL1094400 | — | — | 1 | 7.82 |
| CHEMBL1095457 | — | — | 1 | 7.77 |
| CHEMBL562104 | — | — | 1 | 7.72 |
| CHEMBL1098058 | — | — | 1 | 7.52 |
| CHEMBL1094135 | — | — | 1 | 7.39 |
| CHEMBL1094735 | — | — | 1 | 7.34 |
| CHEMBL1095717 | — | — | 1 | 7.09 |
| CHEMBL559639 | — | — | 1 | 7.09 |
| CHEMBL1098057 | — | — | 1 | 6.98 |
| CHEMBL1094478 | — | — | 1 | 6.85 |
| CHEMBL1094810 | — | — | 1 | 6.68 |
| CHEMBL1098059 | — | — | 1 | 6.60 |
| CHEMBL1097071 | — | — | 1 | 6.51 |
| CHEMBL1094408 | NMS-1286937 | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1094401 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL559845 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1099106 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1099105 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1097429 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1098060 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1094477 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1094322 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1095709 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1095448 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1094811 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1097424 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1097022 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1094402 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1095771 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1095132 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1094400 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1095457 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL562104 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1098058 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1094135 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL1094735 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL559639 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL1095717 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL1098057 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL1094478 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL1094810 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL1098059 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL1097071 | — | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL1094408 | NMS-1286937 | IC50 | = | 355.0 | nM | 6.45 |
| CHEMBL1095772 | — | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL1094820 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL1094488 | — | IC50 | = | 571.0 | nM | 6.24 |
| CHEMBL563150 | — | IC50 | = | 574.0 | nM | 6.24 |
| CHEMBL1097373 | — | IC50 | = | 1037.0 | nM | 5.98 |
| CHEMBL1094816 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL1097374 | — | IC50 | = | 1121.0 | nM | 5.95 |
| CHEMBL1099104 | — | IC50 | = | 1263.0 | nM | 5.90 |
| CHEMBL1094817 | — | IC50 | = | 1347.0 | nM | 5.87 |
| CHEMBL1094484 | — | IC50 | = | 1448.0 | nM | 5.84 |
| CHEMBL1096095 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1094815 | — | IC50 | = | 2746.0 | nM | 5.56 |
| CHEMBL563028 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL1094821 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1094822 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1096028 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1095716 | — | IC50 | > | 10000.0 | nM | - |