Assay Detail
Binding
CHEMBL4737441
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Inhibition of human N-terminal GST-tagged CDK2 (1 to 298 residues)/Cyclin A (174 to 432 residues) expressed in Escherichia coli Turner (DE3) cells assessed as reduction in ADP formation using PKTPKKAKKL as substrate by resorufin dye based fluorescence assay
52
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Tetrahydroindazole inhibitors of CDK2/cyclin complexes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 52 | 5.03 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4763182 | — | — | 1 | 5.82 |
| CHEMBL4778660 | — | — | 1 | 5.68 |
| CHEMBL1708376 | — | — | 1 | 5.66 |
| CHEMBL4795402 | — | — | 1 | 5.62 |
| CHEMBL1906448 | — | — | 1 | 5.58 |
| CHEMBL4751663 | — | — | 1 | 5.57 |
| CHEMBL1735186 | — | — | 1 | 5.52 |
| CHEMBL4750255 | — | — | 1 | 5.51 |
| CHEMBL4776386 | — | — | 1 | 5.44 |
| CHEMBL1905410 | — | — | 1 | 5.35 |
| CHEMBL4746245 | — | — | 1 | 5.34 |
| CHEMBL4777405 | — | — | 2 | 5.32 |
| CHEMBL4754480 | — | — | 1 | 5.31 |
| CHEMBL4799696 | — | — | 1 | 5.17 |
| CHEMBL1722444 | — | — | 1 | 5.12 |
| CHEMBL1722954 | — | — | 1 | 5.03 |
| CHEMBL1881607 | — | — | 1 | 4.98 |
| CHEMBL4753818 | — | — | 1 | 4.92 |
| CHEMBL4790330 | — | — | 1 | 4.92 |
| CHEMBL4762608 | — | — | 1 | 4.72 |
| CHEMBL4785643 | — | — | 1 | 4.68 |
| CHEMBL4793550 | — | — | 1 | 4.58 |
| CHEMBL4790476 | — | — | 1 | 4.43 |
| CHEMBL4751645 | — | — | 1 | 4.34 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 4.30 |
| CHEMBL4744387 | — | — | 1 | 4.25 |
| CHEMBL4782922 | — | — | 1 | 4.23 |
| CHEMBL4784385 | — | — | 1 | 4.01 |
| CHEMBL4760978 | — | — | 1 | - |
| CHEMBL4745490 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4763182 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4778660 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1708376 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4795402 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1906448 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4751663 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1735186 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4750255 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4776386 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1905410 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4746245 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL4777405 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4754480 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4799696 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL1722444 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL1722954 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL1881607 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL4790330 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4753818 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4762608 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4785643 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL4793550 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4777405 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL4790476 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL4751645 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL4744387 | — | IC50 | = | 56000.0 | nM | 4.25 |
| CHEMBL4782922 | — | IC50 | = | 59000.0 | nM | 4.23 |
| CHEMBL4784385 | — | IC50 | = | 97000.0 | nM | 4.01 |
| CHEMBL4795766 | — | IC50 | = | 180000.0 | nM | - |
| CHEMBL4777481 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4788692 | — | IC50 | = | 820000.0 | nM | - |
| CHEMBL4746001 | — | IC50 | = | 160000.0 | nM | - |
| CHEMBL4799375 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4747164 | — | IC50 | = | 560000.0 | nM | - |
| CHEMBL4777744 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4750473 | — | IC50 | = | 470000.0 | nM | - |
| CHEMBL4750473 | — | IC50 | = | 130000.0 | nM | - |
| CHEMBL4777750 | — | IC50 | = | 130000.0 | nM | - |
| CHEMBL4796893 | — | IC50 | = | 350000.0 | nM | - |
| CHEMBL4742154 | — | IC50 | = | 107000.0 | nM | - |
| CHEMBL4756865 | — | IC50 | = | 630000.0 | nM | - |
| CHEMBL4783158 | — | IC50 | = | 200000.0 | nM | - |
| CHEMBL4757459 | — | IC50 | = | 110000.0 | nM | - |
| CHEMBL4760978 | — | IC50 | = | 110000.0 | nM | - |
| CHEMBL4756568 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4747910 | — | IC50 | = | 230000.0 | nM | - |
| CHEMBL4756323 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4749900 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4795870 | — | IC50 | > | 1000000.0 | nM | - |