Assay Detail
Binding
CHEMBL665281
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Inhibitory activity against Cyclin E-cyclin-dependent kinase 2 by measuring phosphorylation of RbING substrate
21
Total Activities
21
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 E (CHEMBL2094126) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.03 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL62253 | — | — | 1 | 6.85 |
| CHEMBL545295 | — | — | 1 | 6.80 |
| CHEMBL126087 | — | — | 1 | 6.75 |
| CHEMBL416056 | — | — | 1 | 6.58 |
| CHEMBL301515 | — | — | 1 | 6.24 |
| CHEMBL304428 | — | — | 1 | 6.17 |
| CHEMBL268368 | STAUROSPORINE AGLYCON | — | 1 | 6.05 |
| CHEMBL124620 | — | — | 1 | 5.82 |
| CHEMBL341110 | — | — | 1 | 5.79 |
| CHEMBL341035 | — | — | 1 | 5.73 |
| CHEMBL53856 | — | — | 1 | 5.71 |
| CHEMBL7463 | GF-109203 | — | 1 | 4.99 |
| CHEMBL266487 | RO-316233 | — | 1 | 4.93 |
| CHEMBL339948 | — | — | 1 | - |
| CHEMBL127852 | — | — | 1 | - |
| CHEMBL302234 | — | — | 1 | - |
| CHEMBL123777 | — | — | 1 | - |
| CHEMBL124033 | — | — | 1 | - |
| CHEMBL293898 | — | — | 1 | - |
| CHEMBL124072 | — | — | 1 | - |
| CHEMBL16958 | STAUROSPORINONE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL62253 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL545295 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL126087 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL416056 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL301515 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL304428 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL268368 | STAUROSPORINE AGLYCON | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL124620 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL341110 | — | IC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL341035 | — | IC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL53856 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL7463 | GF-109203 | IC50 | = | 10180.0 | nM | 4.99 |
| CHEMBL266487 | RO-316233 | IC50 | = | 11690.0 | nM | 4.93 |
| CHEMBL339948 | — | IC50 | < | 60.0 | nM | - |
| CHEMBL127852 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL302234 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL123777 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL124033 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL293898 | — | IC50 | > | 200.0 | nM | - |
| CHEMBL124072 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL16958 | STAUROSPORINONE | IC50 | > | 1000.0 | nM | - |