Assay Detail
Binding
CHEMBL4612762
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Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA1 expressed in baculovirus infected Sf9 insect cells using FRET-labeled Ser/Thr 12 as substrate measured after 1 hr by Z'-lyte assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.90 | 7.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4641226 | — | — | 1 | 7.97 |
| CHEMBL4644893 | — | — | 1 | 7.96 |
| CHEMBL4648005 | — | — | 1 | 7.80 |
| CHEMBL296468 | BMS-387032 | 1.0 | 1 | 7.68 |
| CHEMBL4643057 | — | — | 1 | 7.23 |
| CHEMBL4644643 | — | — | 1 | 7.13 |
| CHEMBL4647764 | — | — | 1 | 6.92 |
| CHEMBL4633672 | — | — | 1 | 6.85 |
| CHEMBL4644198 | — | — | 1 | 6.68 |
| CHEMBL4645334 | — | — | 1 | 6.25 |
| CHEMBL4644087 | — | — | 1 | 5.85 |
| CHEMBL4636175 | — | — | 1 | 5.83 |
| CHEMBL4632815 | — | — | 1 | 5.50 |
| CHEMBL4636090 | — | — | 1 | - |
| CHEMBL4636908 | — | — | 1 | - |
| CHEMBL4637498 | — | — | 1 | - |
| CHEMBL4643754 | — | — | 1 | - |
| CHEMBL4636251 | — | — | 1 | - |
| CHEMBL4634832 | — | — | 1 | - |
| CHEMBL4649546 | — | — | 1 | - |
| CHEMBL4645503 | — | — | 1 | - |
| CHEMBL4649802 | — | — | 1 | - |
| CHEMBL4636655 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4641226 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL4644893 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4648005 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL296468 | BMS-387032 | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4643057 | — | IC50 | = | 58.8 | nM | 7.23 |
| CHEMBL4644643 | — | IC50 | = | 73.2 | nM | 7.13 |
| CHEMBL4647764 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4633672 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4644198 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL4645334 | — | IC50 | = | 561.0 | nM | 6.25 |
| CHEMBL4644087 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL4636175 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL4632815 | — | IC50 | = | 3170.0 | nM | 5.50 |
| CHEMBL4636090 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4636908 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4637498 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4643754 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4636251 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4634832 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4649546 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4645503 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4649802 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4636655 | — | IC50 | > | 10000.0 | nM | - |