Assay Detail
Binding
CHEMBL3767485
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Inhibition of CDK2/Cyclin E (unknown origin)
30
Total Activities
30
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 |
Target
Cyclin-dependent kinase 2/cyclin E1 (CHEMBL1907605) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.22 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL103355 | — | — | 1 | 8.22 |
| CHEMBL3765826 | — | — | 1 | 8.05 |
| CHEMBL424696 | — | — | 1 | 7.85 |
| CHEMBL3765564 | — | — | 1 | 7.72 |
| CHEMBL102926 | — | — | 1 | 7.49 |
| CHEMBL3765805 | — | — | 1 | 7.46 |
| CHEMBL72461 | — | — | 1 | 7.44 |
| CHEMBL3763230 | — | — | 1 | 7.42 |
| CHEMBL358057 | — | — | 1 | 7.41 |
| CHEMBL1999484 | — | — | 1 | 6.66 |
| CHEMBL372207 | — | — | 1 | 6.61 |
| CHEMBL180431 | — | — | 1 | 6.60 |
| CHEMBL360342 | — | — | 1 | 6.49 |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | 6.15 |
| CHEMBL72808 | — | — | 1 | 6.01 |
| CHEMBL3764046 | — | — | 1 | 5.99 |
| CHEMBL307630 | — | — | 1 | 5.97 |
| CHEMBL75984 | — | — | 1 | 5.97 |
| CHEMBL280867 | — | — | 1 | 5.85 |
| CHEMBL306856 | — | — | 1 | 5.68 |
| CHEMBL183511 | — | — | 1 | 5.59 |
| CHEMBL73080 | — | — | 1 | 5.54 |
| CHEMBL99842 | — | — | 1 | 5.54 |
| CHEMBL182011 | — | — | 1 | 5.36 |
| CHEMBL47302 | — | — | 1 | 5.19 |
| CHEMBL280074 | OLOMOUCINE | — | 1 | 5.15 |
| CHEMBL317445 | — | — | 1 | 5.00 |
| CHEMBL99647 | — | — | 1 | 4.02 |
| CHEMBL102622 | — | — | 1 | 4.02 |
| CHEMBL71233 | — | — | 1 | 4.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL103355 | — | IC50 | = | 6.026 | nM | 8.22 |
| CHEMBL3765826 | — | IC50 | = | 8.913 | nM | 8.05 |
| CHEMBL424696 | — | IC50 | = | 14.13 | nM | 7.85 |
| CHEMBL3765564 | — | IC50 | = | 19.05 | nM | 7.72 |
| CHEMBL102926 | — | IC50 | = | 32.36 | nM | 7.49 |
| CHEMBL3765805 | — | IC50 | = | 34.67 | nM | 7.46 |
| CHEMBL72461 | — | IC50 | = | 36.31 | nM | 7.44 |
| CHEMBL3763230 | — | IC50 | = | 38.02 | nM | 7.42 |
| CHEMBL358057 | — | IC50 | = | 38.9 | nM | 7.41 |
| CHEMBL1999484 | — | IC50 | = | 218.78 | nM | 6.66 |
| CHEMBL372207 | — | IC50 | = | 245.47 | nM | 6.61 |
| CHEMBL180431 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL360342 | — | IC50 | = | 323.59 | nM | 6.49 |
| CHEMBL14762 | SELICICLIB | IC50 | = | 707.95 | nM | 6.15 |
| CHEMBL72808 | — | IC50 | = | 977.24 | nM | 6.01 |
| CHEMBL3764046 | — | IC50 | = | 1023.29 | nM | 5.99 |
| CHEMBL307630 | — | IC50 | = | 1071.52 | nM | 5.97 |
| CHEMBL75984 | — | IC50 | = | 1071.52 | nM | 5.97 |
| CHEMBL280867 | — | IC50 | = | 1412.54 | nM | 5.85 |
| CHEMBL306856 | — | IC50 | = | 2089.3 | nM | 5.68 |
| CHEMBL183511 | — | IC50 | = | 2570.4 | nM | 5.59 |
| CHEMBL73080 | — | IC50 | = | 2884.03 | nM | 5.54 |
| CHEMBL99842 | — | IC50 | = | 2884.03 | nM | 5.54 |
| CHEMBL182011 | — | IC50 | = | 4365.16 | nM | 5.36 |
| CHEMBL47302 | — | IC50 | = | 6456.54 | nM | 5.19 |
| CHEMBL280074 | OLOMOUCINE | IC50 | = | 7079.46 | nM | 5.15 |
| CHEMBL317445 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL99647 | — | IC50 | = | 95499.26 | nM | 4.02 |
| CHEMBL102622 | — | IC50 | = | 95499.26 | nM | 4.02 |
| CHEMBL71233 | — | IC50 | = | 97723.72 | nM | 4.01 |