Assay Detail
ADMET
CHEMBL4605124
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery and SARs of 5-Chloro-N4-phenyl-N2-(pyridin-2-yl)pyrimidine-2,4-diamine Derivatives as Oral Available and Dual CDK 6 and 9 Inhibitors with Potent Antitumor Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 53 | 5.90 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4633452 | — | — | 1 | 7.52 |
| CHEMBL4640779 | — | — | 1 | 7.13 |
| CHEMBL4635295 | — | — | 1 | 6.72 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 6.56 |
| CHEMBL4636440 | — | — | 1 | 6.19 |
| CHEMBL4633128 | — | — | 1 | 6.15 |
| CHEMBL4639071 | — | — | 1 | 6.14 |
| CHEMBL4635619 | — | — | 1 | 5.92 |
| CHEMBL4644673 | — | — | 1 | 5.80 |
| CHEMBL4639504 | — | — | 1 | 5.69 |
| CHEMBL4639374 | — | — | 1 | 5.57 |
| CHEMBL3656841 | — | — | 1 | 5.46 |
| CHEMBL4641577 | — | — | 1 | 5.43 |
| CHEMBL4645068 | — | — | 1 | 5.32 |
| CHEMBL4645060 | — | — | 1 | 5.21 |
| CHEMBL4640477 | — | — | 1 | 5.21 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | 5.06 |
| CHEMBL4635117 | — | — | 1 | 5.04 |
| CHEMBL4638665 | — | — | 1 | - |
| CHEMBL4646636 | — | — | 1 | - |
| CHEMBL4641040 | — | — | 1 | - |
| CHEMBL4637112 | — | — | 1 | - |
| CHEMBL4647703 | — | — | 1 | - |
| CHEMBL4645755 | — | — | 1 | - |
| CHEMBL4637170 | — | — | 1 | - |
| CHEMBL4634984 | — | — | 1 | - |
| CHEMBL4640518 | — | — | 1 | - |
| CHEMBL4638056 | — | — | 1 | - |
| CHEMBL4637253 | — | — | 1 | - |
| CHEMBL4643225 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4633452 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4640779 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4635295 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL4636440 | — | IC50 | = | 643.0 | nM | 6.19 |
| CHEMBL4633128 | — | IC50 | = | 701.0 | nM | 6.15 |
| CHEMBL4639071 | — | IC50 | = | 718.0 | nM | 6.14 |
| CHEMBL4635619 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL4644673 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL4639504 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL4639374 | — | IC50 | = | 2680.0 | nM | 5.57 |
| CHEMBL3656841 | — | IC50 | = | 3460.0 | nM | 5.46 |
| CHEMBL4641577 | — | IC50 | = | 3690.0 | nM | 5.43 |
| CHEMBL4645068 | — | IC50 | = | 4840.0 | nM | 5.32 |
| CHEMBL4640477 | — | IC50 | = | 6230.0 | nM | 5.21 |
| CHEMBL4645060 | — | IC50 | = | 6110.0 | nM | 5.21 |
| CHEMBL189963 | PALBOCICLIB | IC50 | = | 8750.0 | nM | 5.06 |
| CHEMBL4635117 | — | IC50 | = | 9180.0 | nM | 5.04 |
| CHEMBL4641071 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4634775 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4633552 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4641351 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4642835 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4645749 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4637543 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4644616 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4638083 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4639998 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4647610 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4637738 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4634448 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4638082 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4634365 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4648038 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4647698 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4639926 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4642485 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4647649 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4643225 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4637253 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4638056 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4640518 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4634984 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4637170 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4645755 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4647703 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4637112 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4641040 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4646636 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4638665 | — | IC50 | > | 10000.0 | nM | - |