Assay Detail
Binding
CHEMBL664631
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Inhibitory activity against Cyclin E-cyclin-dependent kinase 2 in enzymatic assay by measuring phosphorylation of RbING
60
Total Activities
60
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
Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 60 | 6.60 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL306856 | — | — | 1 | 8.40 |
| CHEMBL74637 | — | — | 1 | 8.22 |
| CHEMBL306748 | — | — | 1 | 8.10 |
| CHEMBL73832 | — | — | 1 | 8.05 |
| CHEMBL76390 | — | — | 1 | 8.00 |
| CHEMBL308479 | — | — | 1 | 7.66 |
| CHEMBL308541 | — | — | 1 | 7.64 |
| CHEMBL73485 | — | — | 1 | 7.24 |
| CHEMBL73751 | — | — | 1 | 7.19 |
| CHEMBL74883 | — | — | 1 | 7.17 |
| CHEMBL72754 | — | — | 1 | 7.17 |
| CHEMBL307150 | — | — | 1 | 7.16 |
| CHEMBL74289 | — | — | 1 | 7.12 |
| CHEMBL308116 | — | — | 1 | 7.12 |
| CHEMBL72607 | — | — | 1 | 7.07 |
| CHEMBL73718 | — | — | 1 | 7.05 |
| CHEMBL310260 | — | — | 1 | 7.00 |
| CHEMBL73343 | — | — | 1 | 6.95 |
| CHEMBL306611 | — | — | 1 | 6.95 |
| CHEMBL308252 | — | — | 1 | 6.90 |
| CHEMBL308594 | — | — | 1 | 6.68 |
| CHEMBL76499 | — | — | 1 | 6.65 |
| CHEMBL76326 | — | — | 1 | 6.58 |
| CHEMBL306367 | — | — | 1 | 6.57 |
| CHEMBL306114 | — | — | 1 | 6.50 |
| CHEMBL441258 | — | — | 1 | 6.49 |
| CHEMBL75953 | — | — | 1 | 6.48 |
| CHEMBL73742 | — | — | 1 | 6.40 |
| CHEMBL73781 | — | — | 1 | 6.37 |
| CHEMBL73764 | — | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL306856 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL74637 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL306748 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL73832 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL76390 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL308479 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL308541 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL73485 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL73751 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL74883 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL72754 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL307150 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL74289 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL308116 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL72607 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL73718 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL310260 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL73343 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL306611 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL308252 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL308594 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL76499 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL76326 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL306367 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL306114 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL441258 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL75953 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL73742 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL73781 | — | IC50 | = | 432.0 | nM | 6.37 |
| CHEMBL73764 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL73413 | — | IC50 | = | 558.0 | nM | 6.25 |
| CHEMBL76337 | — | IC50 | = | 567.0 | nM | 6.25 |
| CHEMBL308979 | — | IC50 | = | 685.0 | nM | 6.16 |
| CHEMBL72077 | — | IC50 | = | 716.0 | nM | 6.14 |
| CHEMBL312292 | — | IC50 | = | 796.0 | nM | 6.10 |
| CHEMBL268368 | STAUROSPORINE AGLYCON | IC50 | = | 897.0 | nM | 6.05 |
| CHEMBL311851 | — | IC50 | = | 902.0 | nM | 6.04 |
| CHEMBL75610 | — | IC50 | = | 928.0 | nM | 6.03 |
| CHEMBL75952 | — | IC50 | = | 942.0 | nM | 6.03 |
| CHEMBL72808 | — | IC50 | = | 972.0 | nM | 6.01 |
| CHEMBL75368 | — | IC50 | = | 978.0 | nM | 6.01 |
| CHEMBL306501 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL307152 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL75984 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL307630 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL76464 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL306034 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL306047 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL73772 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL72076 | — | IC50 | = | 1500.0 | nM | 5.82 |